||4-Guanidinobutanoate (4-Guanidinobutanoate, gamma-Guanidinobutyric acid, gamma-Guanidinobutanoate) is a normal metabolite present in low concentrations.
||G-1 is a nonsteroidal and selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with Ki of 11 nM.
||G007-LK is a potent and selective tankyrase inhibitor with IC50 of 46 nM and 25 nM for TNKS1/2, respectively.
||G15 is a cell-permeable high affinity and selective G-protein coupled estrogen receptor 1 (GPER, GPR30) antagonist with an affinity of approximately 20 nM that displays no affinity for ERα and ERβ at concentrations up to 10 μM.
||G150 is a potent and highly selective human cyclic GMP-AMP synthase (cGAS) inhibitor with IC50 of 10.2 nM.
||G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.
||G244-LM is a potent and specific tankyrase 1/2 inhibitor that inhibits Wnt signaling.
||G6PDi-1 is an effective inhibitor of glucose-6-phosphate dehydrogenase (G6PD). G6PDi-1 depletes NADPH and decreases inflammatory cytokine production.
||GABAA receptor agent 1
||GABAA receptor agent 1 is a high affinity ligand for GABAA receptor that exerts potent anticonvulsant activity.
||Gabapentin is a GABA analogue, used to treat seizures and neuropathic pain.
||Gabapentin HCl is a GABA analogue, used to treat seizures and neuropathic pain.
||GABARAPL2 Rabbit Recombinant mAb
||GABARAPL2 Rabbit Recombinant mAb detects endogenous level of total GABARAPL2.
||Gabexate Mesylate is a serine protease inhibitor with IC50 of 0.19 μM which is used therapeutically in the treatment of pancreatitis and disseminated intravascular coagulation.
||Gadobutrol (Gadovist, Gadavist) is a non-ionic macrocyclic gadolinium-based contrast agent (GBCA) that is usedfor tissue contrast enhancement in magnetic resonance imaging (MRI).
||Gadodiamide (GDD, Omniscan) is a widely used magnetic resonance imaging (MRI) contrast agent with a high renal toxicity.
||Gadodiamide Hydrate, a nonionic Gd3+ chelate, is frequently injected i.v. into magnetic resonance imaging (MRI) to enhance contrast.
||Gadopentetate Dimeglumine (Gadopentetic acid dimeglumine, Gd-DTPA, Meglumine gadopentetate), a complex of gadolinium with a chelating agent, diethylenetriamine penta-acetic acid, is an extracellular intravenous contrast agent used in magnetic resonance imaging.
||Gadoteridol (ProHance, SQ-32692, Gd-HP-DO3A) is a nonionic contrast agent for magnetic resonance imaging (MRI).
||Gadoxetate is a paramagnetic gadolinium-containing contrast agent in which its salt form, gadoxetate disodium, is used for intravenous injection.
||GAK inhibitor 49
||GAK inhibitor 49 is a potent, ATP-competitive and selective inhibitor of cyclin G associated kinase (GAK) with Ki of 0.54 nM and IC50 of 56 nM. GAK inhibitor 49 also binds to RIPK2.
||GAL-021 is a new intravenous BKCa-channel blocker.
||Galangin (3,5,7-trihydroxyflavone; Norizalpinin), a naturally occuring flavonoid found in herbs, is a well-known antioxidant and also an inhibitor of CYP1A1 activity and an agonist/antagonist of the aryl hydrocarbon receptor.
||Galangin 3-methyl ether
||Galangin 3-methyl ether (3-O-Methylgalangin, 3-Methylgalangin), isolated from Lychnophora markgravii aerial parts, shows strong antibacterial and antifungal effects.
||Galanthamine (Galantamine, Nivalin, Razadyne, Razadyne ER, Reminyl, Lycoremine) is a phenanthrene alkaloid and a reversible, competitive acetylcholinesterase inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase. It is studied as a treatment for Alzheimer's disease and other central nervous system disorders.
||Galanthamine is an AChE inhibitor with IC50 of 0.35 μM, exhibits 50-fold selectivity against butyryl-cholinesterase.
||Galeterone (TOK-001) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.
||Galicaftor (ABBV-2222, GLPG2222) is a potent corrector of CFTR for the treatment of Cystic Fibrosis (CF).
||Gallamine Triethiodide is a cholinergic receptor blocker with an IC50 of 68.0 ± 8.4 μM.
||Gallein (Pyrogallol phthalein) is an inhibitor of G protein βγ (G beta-gamma complex, Gβγ) subunit interaction with PI3 kinase. Gallein inhibits β-ionone effects and exhibits anti-tumor activity. Gallein can be used as a biological stain.
||Gallic acid (3,4,5-Trihydroxybenzoic acid, Gallate, Benzoic acid), known as powerful antioxidants, is an organic acid found in a variety of foods and herbs.
||Gallic acid trimethyl ether
||Gallic acid trimethyl ether (Eudesmic acid, Tri-O-methylgallic acid, Benzoic acid, 3,4,5-Trimethoxybenzoic acid) is an O-methylated trihydroxybenzoic acid that is found in olive.
||Gallocyanine (Solid Violet) is a histological dye used in solution with an iron alum mordant as a hematoxylin substitute in the H&E stain. It has a role as a fluorochrome and a histological dye.
||Galloflavin (NSC 107022) is a novel inhibitor of lactate dehydrogenasee (LDH) with Ki values of 5.46 μM and 15.06 μM for LDH-A and LDH-B, respectively.
||Galunisertib (LY2157299) is a potent TGFβ receptor I (TβRI) inhibitor with IC50 of 56 nM in a cell-free assay. Phase 2/3.
||Gambogenic Acid, identified from Gamboge, is an inhibitor of the FGFR signaling pathway in erlotinib-resistant non-small-cell lung cancer (NSCLC) and exhibits anti-tumor effects. Gambogenic acid acts is also an effective inhibitor of EZH2 that specifically and covalently binds to Cys668 within the EZH2-SET domain, and triggers EZH2 ubiquitination.
||Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.
||Gamithromycin (ML-1709460) is a new macrolide antibiotic that is only registered for use in cattle to treat respiratory disorders such as bovine respiratory disease.
||Gamma-oryzanol (GO), a nutriactive phytochemical naturally occurring in crude rice bran oil, is an antioxidant compound used to treat hyperlipidemia, disorders of menopause and to increase the muscle mass. γ-Oryzanol is a potent DNA methyltransferases (DNMTs) inhibitor in the striatum of mice. γ-Oryzanol significantly inhibits the activities of DNMT1 (IC50=3.2 μM), DNMT3a (IC50=22.3 μM).
||Ganciclovir (BW 759)
||Ganciclovir (RS-21592, BW-759, 2'-Nor-2'-deoxyguanosine) is an antiviral drug for feline herpesvirus type-1 with IC50 of 5.2 μM in a cell-free assay.
||Ganciclovir Sodium (RS-21592, Cytovene IV, BW 759, 2'-Nor-2'-deoxyguanosine) is the sodium salt form of ganciclovir, a synthetic, antiviral, purine nucleoside analog with antiviral activity, especially against cytomegalovirus (CMV).
||Gandotinib (LY2784544) is a potent JAK2 inhibitor with IC50 of 3 nM, effective in JAK2V617F, 8- and 20-fold selective versus JAK1 and JAK3. Phase 2.
||Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.
||GANT61 (NSC 136476) is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 induces apoptosis and activates protective autophagy in LX-2 cells.
||Gap 26, a connexin mimetic peptide that composeds of residue no. 63-75 of the extracellular loop 1 of connexin 43 (Cx43), is a gap junction inhibitor. Gap 26 blocks photoliberating inositol-1,4,5-trisphosphate triggers ATP release.
Gap 27 is a synthetic connexin-mimetic peptide and acts as a gap junction inhibitor. Gap 27 is highly effective in interrupting co-operative cell-cell interactions, such as the synchronous beating of embryonic cardiomyocytes.
||Gap19 is a nonapeptide derived from the cytoplasmic loop (CL) of Cx43 and acts as a selective connexin 43 (Cx43) hemichannel blocker. Gap19 blocks Cx43 hemichannels without inhibiting gap junctions (GJs) at IC50 of 6.5 μM when applied intracellulary.
||GAPDH Rabbit Recombinant mAb
GAPDH Rabbit Recombinant mAb detects endogenous levels of total GAPDH.
||Gardenoside is a natural compound extracted from Gardenia fruits, with hepatoprotective properties. Gardenoside inhibits TNF-α, IL-1β, IL-6 and NFκB activation. Gardenoside also has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis. Gardenoside suppresses the pain in rats model of chronic constriction injury by regulating the P2X3 and P2X7 receptors.
||Garenoxacin (T-3811ME, BMS-284756) is a novel des-F(6) quinolone that has been shown to be effective in vitro against a wide range of clinically important pathogens, including gram-positive and gram-negative aerobes and anaerobes.
||GART Rabbit Recombinant mAb
||GART Rabbit Recombinant mAb detects endogenous level of total GART.
||Gastrodenol (Bismuth tripotassium dicitrate) is used to treat certain conditions caused by too much acid being produced in the stomach, such as stomach ulcers and ulcers of the upper part of the intestine (duodenal ulcers).
||Gastrodin (Gastrodine), an anti-inflammatory polyphenol extracted from Chinese natural herbal Gastrodia elata Blume., benefits neurodegenerative diseases.
||GATA1 Rabbit Recombinant mAb
||GATA1 Rabbit Recombinant mAb detects endogenous level of GATA1.
||GATA2/3 Rabbit Recombinant mAb
||GATA2/3 Rabbit Recombinant mAb detects endogenous levels of total GATA2/3.
||GATA4-NKX2-5-IN-1 (3i-1000) is a potent, dose-dependent inhibitor of the GATA4–NKX2-5 transcriptional synergy with IC50 of 3 μM. GATA4-NKX2-5-IN-1 exhibits no activity on the protein kinases involved in the regulation of GATA4 phosphorylation, and it modulates the hypertrophic agonist-induced cardiac gene expression.
||Gatifloxacin (AM-1155, CG5501, BMS-206584) is an antibiotic of the fourth-generation fluoroquinolone family, and inhibits the bacterial enzymes DNA gyrase and topoisomerase IV.
||Gatifloxacin (AM-1155, CG5501, BMS-206584, PD135432) hydrochloride is a potent fluoroquinolone antibiotic with broad-spectrum antibacterial activity. Gatifloxacin hydrochloride inhibits bacterial type II topoisomerases with IC50 of 13.8 μg/ml and 0.109 μg/ml for S. aureus topoisomerase IV and E. coli DNA gyrase, respectively.
||Gboxin is an inhibitor of oxidative phosphorylation in cancer cells. Gboxin inhibits the activity of F0F1 ATP synthase. It specifically inhibits the growth of primary mouse and human glioblastoma cells but not that of mouse embryonic fibroblasts or neonatal astrocytes.
||GC376 is a 3CLpro (3C-like protease) inhibitor with IC50 of ~ 1.11 μM for the PEDV 3CLpro. GC376 is active against the 3CLpro of multiple coronaviruses, including SARS-CoV.
||GC7 (N1-guanyl-1,7-diaminoheptane) Sulfate is an inhibitor of deoxyhypusine synthase (DHPS). GC7 inhibits Neuroblastoma (NB) cell proliferation in a dose-dependent manner, through induction of the cell cycle inhibitor p21 and reduction of total and phosphorylated Rb proteins.
||GCLC Rabbit Recombinant mAb
||GCLC Rabbit Recombinant mAb detects endogenous level of total GCLC.
||GCN2 Rabbit Recombinant mAb
||GCN2 Rabbit Recombinant mAb detects endogenous level of total GCN2.
||GCN2iB is an ATP-competitive serine/threonine-protein kinase general control nonderepressible 2 (GCN2) inhibitor with IC50 of 2.4 nM.
||GDC-0152 is a potent antagonist of XIAP-BIR3, ML-IAP-BIR3, cIAP1-BIR3 and cIAP2-BIR3 with Ki of 28 nM, 14 nM, 17 nM and 43 nM in cell-free assays, respectively; less affinity shown to cIAP1-BIR2 and cIAP2-BIR2. Phase 1.
||GDC-0349 (RG-7603) is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
||GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM.
||GDC-0623 (G-868) is a potent and ATP-uncompetitive MEK1 inhibitor with Ki of 0.13 nM. Phase 1.
||GDC-0879 (AR-00341677) is a novel, potent, and selective B-Raf inhibitor with IC50 of 0.13 nM in A375 and Colo205 cells with activity against c-Raf as well; no inhibition known to other protein kinases.
||GDC046 (Compound 3) is a potent, selective, and orally bioavailable inhibitor of TYK2 with Ki of 4.8 nM, 83.8 nM, 27.6 nM and 253 nM for TYK2, JAK1, JAK2, and JAK3, respectively.
||GDNF Rabbit Recombinant mAb
||GDNF Rabbit Recombinant mAb detects endogenous level of total GDNF.
||GeA-69 is a cell-permeable, selective allosteric inhibitor targeting macrodomain 2 (MD2) of poly-adenosine-diphosphate-ribose polymerase 14 (PARP14) with Kd of 860 nM.
||Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM in cell-free assays, respectively. Phase 2.
||Gefapixant (AF-219, MK-7264, R1646, RG-1646, RO 4926219) is an orally active small molecule antagonist of human P2X3 receptor with IC50 of about 30 nM, 100–250 nM for recombinant hP2X3 homotrimers and hP2X2/3 heterotrimeric receptors, respectively. Gefapixant has shown promise for the treatment of refractory and unexplained chronic cough.
||Gefarnate (Geranyl farnesylacetate) is a synthetic compound used for the treatment of gastric ulcers.
||Gefitinib (ZD-1839, Iressa) is an EGFR inhibitor for Tyr1173, Tyr992, Tyr1173 and Tyr992 in the NR6wtEGFR and NR6W cells with IC50 of 37 nM, 37nM, 26 nM and 57 nM, respectively. Gefitinib promotes autophagy and apoptosis of lung cancer cells via blockade of the PI3K/AKT/mTOR pathway.
||Gefitinib (ZD1839) is an EGFR inhibitor with IC50s of 15.5 nM and 823.3 nM for WT EGFR and EGFR (858R/T790M), respectively.
||Gefitinib-based PROTAC 3
||Gefitinib-based PROTAC 3 which conjugates an EGFR binding element to a VHL ligand via a linker induces degradation of EGFR and mutants with DC50 of 11.7 nM and 22.3 nM in HCC827(Exon 19 del) and H3255 (L858R) cells, respectively.
||Geldanamycin (NSC 122750)
||Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.
||Gelsemine, a principal alkaloid from Gelsemium sempervirens Ait., is a highly toxic compound and may be a glycine receptor agonist with significantly higher binding affinity for some of these receptors than its native agonist, glycine.
||Gemcabene (PD-72953), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity.
||Gemcitabine (LY-188011, NSC 613327), a nucleic acid synthesis inhibitor, is a very potent and specific deoxycytidine analogue, used as chemotherapy. Gemcitabine induces a potent p53-dependent apoptosis.
||Gemcitabine (LY-188011) HCl
||Gemcitabine (LY-188011, NSC 613327) HCl is a DNA synthesis inhibitor with IC50 of 50 nM, 40 nM, 18 nM and 12 nM in PANC1, MIAPaCa2, BxPC3 and Capan2 cells, respectively.
||Gemfibrozil (CI-719) is an activator of peroxisome proliferator-activated receptor-alpha (PPARα), used for the treatment of hypercholesterolemia and hypertriglyceridemia.
Gemigliptin (Zemiglo, LC15-0444) is a potent, selective and long-acting dipeptidyl peptidase 4 (DPP 4) inhibitor with a Ki of 7.25 nM. Gemigliptin shows at least >23,000-fold selectivity for DPP-4 over various proteases and peptidases, including DPP-8, DPP-9, and fibroblast activation protein (FAP)-α.
||GNE-6776 is a potent, non-covalent, selective and orally bioavailable inhibitor of USP7 with IC50 of 1.34 μM and 0.61 μM for full length USP7 and USP7 catalytic domain, respectively.
||Geneticin (G418 Sulfate)
||Geneticin (G418 Sulfate), an aminoglycoside antibiotic, is an elongation inhibitor of 80 S ribosomes that blocks polypeptide synthesis by inhibiting the elongation step in both prokaryotic and eukaryotic cells.
||Genipin 1-O-beta-D-gentiobioside (GG, Genipin 1-β-D-gentiobioside, Genipin 1-gentiobioside, Genipin 1-β-gentiobioside, Genipin gentiobioside) is a bioactive iridoid glycoside isolated from Gardenia jasminoides Ellis (Zhizi in Chinese) that exhibits hepatoprotective, anti-inflammatory, antioxidant, and antithrombotic activities.
||Geniposide is an iridoid glycoside isolated from the fruit of Gardenia jasminoides Ellis.
||Genistein (NPI 031L)
||Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM.
||Genistin (Genistoside, Genistine, Genistein 7-glucoside, Genistein glucoside) is an isoflavone found in a number of dietary plants like soy and kudzu. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of Estrogen Receptor α (ERα) signaling pathway.
||Genkwanin (Apigenin 7-methyl ether) is one of the major non-glycosylated flavonoids in herbs. It has a variety of pharmacological effects including anti-inflammatory, anti-bacterial, antiplasmodial, radical scavenging, chemopreventive and inhibiting 17β-Hydroxysteroid dehydrogenase type 1 activities.
||Gentamicin is a widely used antibiotic in the intensive care unit (ICU). Gentamicin, an aminoglycoside, is an inhibitor of protein synthesis.
||Gentamycin Sulfate (NSC-82261, SCH9724) is a broad-spectrum, aminoglycoside antibiotic used for cell culture which inhibits protein synthesis in sensitive organisms.
||Gentiopicroside (GE, Gentiopicrin), a naturally occurring iridoid glycoside, inhibits CYP2A6 and CYP2E1 with IC50 values of 21.8μg/ml and 594μg/ml, respectively in human liver microsomes, and dose not inhibit CYP2C9, CYP2D6, CYP1A2 or CYP3A4 activities.
||Gentisic acid (2,5-dihydroxybenzoic acid, 5-Hydroxysalicylic acid, Hydroquinonecarboxylic acid, DHB), an active metabolite of salicylic acid degradation, has a broad spectrum of biological activity, such as anti-inflammatory, antirheumatic and antioxidant properties.
||Genz-123346 free base
||Genz-123346 is an inhibitor of GL1 synthase that blocks the conversion of ceramide to GL1, the first step in the biosynthesis of gangliosides and other glycosphingolipids.
||Genz-644282 is a non-camptothecin topoisomerase I (Topo I) inhibitor that demonstrates potent cytotoxic activity with a median IC50 of 1.2 nM (range 0.2 nM-21.9 nM). Genz-644282 can be used in cancer research.
||Geraniin, a hydrolysable polyphenol derived from Nephelium lappaceum L. fruit rind, has been shown to possess significant antioxidant activity in vitro.The IC50 values of TNF-α release inhibition were 43 μM for geraniin.
||Geraniol is a terpene alcohol occurring in the essential oils of several aromatic plants used in the flavour and fragrance industries. It also exhibits insecticidal and repellent properties and used as a natural pest control agent exhibiting low toxicity.
||Geranyl acetate (Geraniol acetate, Geranyl ethanoate) is a natural organic compound that is used primarily as a component of perfumes for creams and soaps and as a flavoring ingredient. Geranyl acetate exhibits anti-cancer effects by inducing cell apoptosis.
||Germacrone, a major activity component found in Curcuma zedoaria oil product, shows anti-inflammatory, antiandrogenic, and antimicrobial activities.
||Gestodene (SH B 331) is a progestogen hormonal contraceptive.
||GET73 (Gamma hydroxybutyric acid analogue, GET 73, GHB analogue) regulates hippocampal Aminoacidergic transmission possibly via an allosteric modulation of mGlu5 receptor.
||GFB-8438 is a novel, potent, and subtype selective TRP channel subfamily C (TRPC) inhibitor that is equipotent against TRPC4 and TRPC5 with IC50 of 0.18 μM and 0.29 μM, and shows excellent selectivity against TRPC6, other TRP family members , NaV 1.5, as well as limited activity against the hERG channel.
||GFP Rabbit Recombinant mAb
||GFP Rabbit Recombinant mAb detects endogenous level of total GFP.
||GGTI 298 TFA salt
||GGTI 298 is a geranylgeranyltransferase I inhibitor with ability to arrest human tumor cells in the G1 phase of the cell cycle and induce apoptosis.
||GI254023X (GI 4023, SRI028594) is a selective inhibitor of ADAM10 with 100-fold selectivity for ADAM10 over ADAM17. The IC50 values for recombinant ADAM10 amd ADAM17 are 5.3 nM and 541 nM, respectively.
||Gibberellic acid (Gibberellin, Gibberellin A3, GA3, GA), a plant hormone stimulating plant growth and development, is a tetracyclic di-terpenoid compound.
||Gibberellins A4/A7 (Gibberellin A4 and A7) is the Gibberellin A4 Mixture With Gibberellin A7. Gibberellins A4/A7 promotes internode elongation & breaks certain dormancies in seeds. Gibberellins A4/A7 is an endogenous plant growth regulator, promotes the growth and elongation of cells.
||GIBH-130 is an effective neuroinflammation inhibitor. GIBH-130 significantly suppresses the IL-1β secretion by activated microglia with IC50 of 3.4 nM.
||Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).
||Gimeracil is an inhibitor of dihydropyrimidine dehydrogenase, which inhibits the early step in homologous recombination for double strand breaks repair.
Ginkgetin is a biflavone from Ginkgo biloba leaves with anti-cancer, anti-inflammatory, anti-microbial, anti-adipogenic, and neuroprotective activities.
||Ginkgolic acid, toxic phenolic compounds present in the fruits and leaves of Ginkgo biloba L., is a potent sumoylation inhibitor also reported to inhibit histone acetylation transferase (HAT).
||Ginkgolic Acid (C13:0)
||Ginkgolic Acid (C13:0) is a natural anticariogenic agent in Ginkgo biloba L. that exhibits antimicrobial activity against S. mutans and suppresses the specific virulence factors associated with its cariogenicity. Ginkgolic acid is a potent sumoylation inhibitor and reported to inhibit histone acetylation transferase (HAT).
||Ginkgolic acid C17:1
||Ginkgolic acid C17:1 (GAC 17:1) inhibits constitutive activation of STAT3 through the abrogation of upstream JAK2 and Src. Ginkgolic acid C17:1 can induce the substantial expression of PTEN and SHP-1. Ginkgolic acid C17:1 induces apoptosis of tumor cells.
||Ginkgolide A (BN52020) is an extract from in Ginkgo biloba and a g-aminobutyric acid (GABA) antagonist with a Ki of 14.5 μM.
||Ginkgolide B (BN52021) is a PAFR antagonist with IC50 of 3.6 μM.
||Ginkgolide C (BN-52022), isolated from Ginkgo biloba leaves, is a flavone reported to have multiple biological functions, from decreased platelet aggregation to ameliorating Alzheimer disease. It is an activator of MMP-9.
||Ginkgolide J is a minor constituent of terpene trilactone mixture of Ginkgo biloba leaves extract that inhibits GlyR-operated channels with IC50 of 2.0 μM. Ginkgolide J also inhibits cell death of rodent hippocampal neurons caused by Aβ1–42. Ginkgolide J exhibits anti‑inflammatory activity.
||Ginsenoside F1, a pharmaceutical component of ginseng, is known to have antiaging, antioxidant, anticancer, and keratinocyte protective effects. Ginsenoside F1 exhibits competitive inhibition of the activity of CYP3A4 with Ki values of 67.8 ± 16.2 μM. Ginsenoside F1 also exhibited a weaker inhibition of the activity of CYP2D6.
||Ginsenoside Rb1 (Gypenoside Ⅲ) is a protopanaxadiol that has diverse in vitro and in vivo effects, including neuroprotective, anti-inflammatory, and anti-obesity actions. Ginsenoside Rb1, a main constituent of the root of Panax ginseng, inhibits Na+, K+-ATPase activity with IC50 of 6.3±1.0 μM. Ginsenoside also inhibits IRAK-1 activation and phosphorylation of NF-κB p65. Ginsenoside Rb1 reduces the expressions of TLR3, TLR4 and TRAF-6, and down-regulates the levels of TNF-α, IFN-β and iNOS.
||Ginsenoside Rb2 (Ginsenoside C) is a ginsenoside found in Panax ginseng that has a role as a plant metabolite, an antiviral agent and a hypoglycemic agent.
||Ginsenoside Rb3, extracted from the plant Panax ginseng, plays important roles in cardiovascular diseases, including myocardial ischemia-reperfusion (I/R) injury. Ginsenoside Rb3 (0.1-10 μM) is tested for inhibition of tumor necrosis factor-α (TNF)-induced nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) luciferase reporter activity using a human kidney 293T cell-based assay. Ginsenoside Rb3 shows the significant activity with an IC50 of 8.2 μM. Ginsenoside Rb3 also inhibits the induction of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS) messenger Ribonucleic acid (mRNA) in a dose-dependent manner after HepG2 cells have been treated with TNF-α (10 ng/mL).
||Ginsenoside Rd (Panaxoside Rd, Sanchinoside Rd), a minor ginseng saponin, has several pharmacological activities such as immunosuppressive activity, anti-inflammatory activity, immunological adjuvant, anti-cancer activity and wound-healing activity. Ginsenoside Rd inhibits TNFα-induced NF-κB transcriptional activity with an IC50 of 12.05±0.82 μM in HepG2 cells. Ginsenoside Rd inhibits expression of COX-2 and iNOS mRNA. Ginsenoside Rd also inhibits Ca2+ influx. Ginsenoside Rd inhibits CYP2D6, CYP1A2, CYP3A4, and CYP2C9, with IC50s of 58.0±4.5 μM, 78.4±5.3 μM, 81.7±2.6 μM, and 85.1±9.1 μM, respectively.
||Ginsenoside Re (Ginsenoside B2, Panaxoside Re, Sanchinoside Re, Chikusetsusaponin Ivc), an extract from Panax notoginseng, is a major ginsenoside in ginseng and belongs to 20(S)-protopanaxatriol group. It has diverse in vitro and in vivo effects, including vasorelaxant, antioxidant, antihyperlipidemic, and angiogenic actions. Ginsenoside Re decreases the β-amyloid protein (Aβ). Ginsenoside Re plays a role in antiinflammation through inhibition of JNK and NF-κB.
||Ginsenoside Rg1 (Ginsenoside A2, Panaxoside A, Panaxoside Rg1, Sanchinoside C1, Sanchinoside Rg1), one of the major active components of ginseng, is identified as a protopanaxatriol-type and has pharmacological actions such as neuroprotective and anti-tumor effects on various cancer types. Ginsenoside Rg1 reduces cerebral Aβ levels and NF-κB nuclear translocation.
||Ginsenoside Ro (Chikusetsusaponin V), one of the high-abundance saponins in ginseng, is widely used as a dietary supplement and has many health-promoting effects.
||Givinostat (ITF2357) is a potent HDAC inhibitor for maize HD2, HD1B and HD1A with IC50 of 10 nM, 7.5 nM and 16 nM in cell-free assays. Phase 2.
||GJ-103 is an active analog of GJ072 which is a read-through compound (RTC). Chemical-induced read through of premature stop codons might be exploited as a potential treatment strategy for genetic disorders caused by nonsense mutations.
||GJ103 sodium salt
||GJ103 sodium salt is an active analog of GJ072 (a read-through compound).
||GK921 is a transglutaminase 2 (TGase 2) inhibitor with an IC50 of 8.93 μM under a modified assay condition.
||Glabridin (Q-100692, KB-289522, LS-176045), one of the active phytochemicals in licorice extract, binds to and activates the ligand binding domain of PPARγ, as well as the full length receptor. It is also a GABAA receptor positive modulator promoting fatty acid oxidation and improving learning and memory.
||Glasdegib (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2.
Glatiramer acetate is a synthetic copolymer composed of a random mixture of four amino acids that modifies the immune response.
Glaucocalyxin A is a biologically active ent-kauranoid diterpenoid isolated from Rabdosia japonica var. glaucocalyx with antitumor and anti-inflammatory activity. Glaucocalyxin A induces G2/M cell cycle arrest and apoptosis through the PI3K/Akt pathway in human bladder cancer cells.
||Glecaprevir is a hepatitis C virus (HCV) nonstructural (NS) protein 3/4A protease inhibitor that targets the the viral RNA replication. It displays IC50 values ranging from 3.5 to 11.3 nM for clinical isolates of HCV genotypes 1a, 1b, 2a, 2b, 3a, 4a, 5a, and 6a.
||Gliclazide is a whole-cell beta-cell ATP-sensitive potassium currents blocker with an IC50 of 184 nM.
||Glimepiride is a potent Kir6.2/SUR inhibitor with IC50 of 3.0 nM, 5.4 nM, and 7.3 nM for SUR1, SUR2A and SUR2B, used in the treatment of type 2 diabetes mellitus.
||Glipizide (CP-28720) is used to treat high blood sugar levels caused by a type of diabetes mellitus called type 2 diabetes.
||Gliquidone (Glurenorm) is an ATP-sensitive K+ channel antagonist with IC50 of 27.2 nM.
||GLPG0634 analogue is a selective JAK1 inhibitor with IC50 of 10 nM, 28 nM, 810 nM, and 116 nM for JAK1, JAK2, JAK3, and TYK2, respectively. Phase 2.
||GLPG1837 (ABBV-974) is a novel CFTR potentiator with an EC50 value of 3 nM for F508del, showing enhanced efficacy on CFTR mutants harboring class III mutations compared to Ivacaftor.
||Glucagon Acetate stimulates glycogenolysis in the liver, used as an antihypoglycemic and as an adjunct in gastrointestinal radiography.
||Glucocorticoid Receptor Rabbit Recombinant mAb
||Glucocorticoid Receptor Rabbit Recombinant mAb detects endogenous level of total glucocorticoid receptor.
||Gluconolactone is a naturally occurring polyhydroxy acid with metal chelating, moisturizing and antioxidant activity.
||Glucosamine (2-amino-2-deoxy-D-glucose) is an amino sugar and a prominent precursor in the biochemical synthesis of glycosylated proteins and lipids. It is commonly used as a treatment for osteoarthritis. Glucosamine（GS） treatment selectively downregulates HIF-1α at the protein level in YD-8 cells via interference of production of the citric acid cycle metabolites.
||Glucosamine (2-Amino-2-deoxy-glucose, Chitosamine) is a natural constituent of glycosaminoglycans in the cartilage matrix and synovial fluid, also presents in the shells of shellfish, animal bones, bone marrow, and fungi. Glucosamine is commonly used as a treatment for osteoarthritis, although its acceptance as a medical therapy varies.
||Glucosamine sulfate (D-Glucosaminesulfate, D-Glucosamine sulphate) is a dietary supplement commonly used in the treatment of osteoarthritis. It is a type of glycosaminoglycan, which is a naturally occurring major component of joint cartilage and joint fluid.
||Glucosyl-vitexin (Glucosylvitexin), the major C-glycosylflavone present in millet, inhibits thyroid peroxidase (TPO) activity.
||Glumetinib (SCC244) is a potent and highly selective c-Met inhibitor with an IC50 of 0.42 ± 0.02 nmol/L. Glumetinib has greater than 2,400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, and TyrO3.
||GluR2 Rabbit Recombinant mAb
||GluR2 Rabbit Recombinant mAb detects endogenous level of total GluR2.
||GLUT3 Rabbit Recombinant mAb
||GLUT3 Rabbit Recombinant mAb detects endogenous level of total GLUT3.
||Glutamine Metabolism Compound Library
||A unique collection of 439 glutamine metabolism related compounds used for high throughput screening (HTS) and high content screening (HCS).
||Glutamine Synthetase Rabbit Recombinant mAb
||Glutamine Synthetase Rabbit Recombinant mAb detects endogenous level of total Glutamine Synthetase.
Glutaric acid (GA) is an attractive C5 dicarboxylic acid with wide applications in the biochemical industry.
||Glutathione (Isethion, Tathion) acts as an antioxidant, a free radical scavenger and a detoxifying agent. It is a tripeptide comprised of three amino acids (cysteine, glutamic acid, and glycine) present in most mammalian tissue.
||GLX351322 is a NADPH oxidase 4 (NOX4) inhibitor. GLX351322 inhibits hydrogen peroxide production from tetracycline inducible NOX4-overexpressing cells with IC50 of 5 μM.
||Gly-Phe β-naphthylamide (Gly-Phe beta-naphthylamide) is a substrate of cathepsin C that accumulates within the lysosome. Gly-Phe-β-naphthylamide can inhibit the cathepsin-dependent activation of caspase-8.
||Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.
||Glycerol (Glycerin) is a clear, colourless and viscous liquid that can be used as emollient, solvent or sweetening agent. Glycerol changes the separation characteristics of polyacrylamide nucleoprotein gels.
||Glycerol phenylbutyrate (GT4P, HPN-100M, Ravicti) is a nitrogen-binding agent and acts as a sigma-2 (σ2) receptor ligand with a pKi of 8.02. Glycerol phenylbutyrate is a prodrug in which phenylbutyrate (PBA) is released from the glycerol backbone by lipases in the gastrointestinal tract.
||Glycerol Tri-n-octanoate (Glycerol trioctanoate, Glycerol tricaprylate, Trioctanoin, Tricaprylin) is a well-known raw material largely used in cosmetic products.
||Glycerol tributyrate (Tributyrin) is a triglyceride that may inhibit cell growth and induce cell differentiation.
||Glycerol trilinoleate (Trilinolein) is a triacylglycerol and has been reported to provide a number of beneficial effects including reducing thrombogenicity and arrhythmias and increasing erythrocyte deformability. It is also an antioxidant.
||Glyceryl monocaprate (Monocaprin)
||Monocaprin (Glyceryl caprate) is a 1-monoglyceride of capric acid that has antimicrobial activity against enveloped viruses, certain bacteria, and the yeast Candida albicans.
||Glyceryl tridecanoate (Tricaprin) is an orally available precursor of decanoic acid with potential antiandrogen and antihyperglycemic properties.
||Glycine (2-Aminoacetic acid, Aminoacetic acid, Glycocoll) is a non-essential, non-polar, non-optical, glucogenic amino acid that is primarily found in gelatin and silk fibroin. It is involved in the body's production of DNA, phospholipids and collagen, and in release of energy.
||Glycitin (Glycitein-7-β-O-glucoside), a natural isoflavone isolated from legumes, has antibacterial, antiviral and estrogenic activities and may exerts preventative effects on alcoholism, cardiovascular and cerebrovascular diseases and some types of cancer.
||Glycochenodeoxycholic acid (Glycochenodeoxycholate, Chenodeoxycholylglycine, Glycine chenodeoxycholate) is a bile salt formed in the liver from chenodeoxycholate and glycine. It acts as a detergent to solubilize fats for absorption. Glycochenodeoxycholic acid
||Glycochenodeoxycholic acid sodium salt
||Glycochenodeoxycholic acid is a bile salt formed in the liver from chenodeoxycholic acid and glycine, usually found as the sodium salt. It acts as a detergent to solubilize fats for absorption and is itself absorbed.
||Glycocholic acid (Cholylglycine, Glycocholate) is a natural secondary bile acid involved in the emulsification of fats.
||Glycodeoxycholic acid sodium salt
||Glycochenodeoxycholic acid (GCDC, Glycodeoxycholate, Deoxycholylglycine) is a bile salt that is used as an anionic detergent to solubilize lipids.
||Glycogen synthase Rabbit Recombinant mAb
||Glycogen synthase Rabbit Recombinant mAb detects endogenous level of total glycogen synthase.
Glycolaldehyde dimer (2,5-Dihydroxy-1,4-dioxane, 1,4-Dioxane-2,5-diol, DD) is an active endogenous metabolite that appears moderate absorbent and fluorescent, when it reacts with glycine (Gly)/ammonium sulfate (AS).
||Glycolic acid (dicarbonous acid, hydroxyacetic acid, hydroacetic acid) is the smallest alpha-hydroxy acid. Due to its excellent capability to penetrate skin, glycolic acid is often used in skin care products, most often as a chemical peel. Glycolic acid is an inhibitor of tyrosinase, suppressing melanin formation and lead to a lightening of skin colour.
||Glycolysis Compound Library
||A unique collection of 396 glycolysis related compounds used for high throughput screening(HTS) and high content screening(HCS).
||Glycophorin A (CD235a) Rabbit Recombinant mAb
||Glycophorin A (CD235a) Rabbit Recombinant mAb detects endogenous level of total Glycophorin A (CD235a).
||Glycopyrrolate (Glycopyrronium, Robinul, Gastrodyn) is a muscarinic antagonist used as an antispasmodic, in some disorders of the gastrointestinal tract, and to reduce salivation with some anesthetics.
||Glycoursodeoxycholic acid (Ursodeoxycholyl Glycine, Glycine ursodeoxycholic acid) is an acyl glycine and a bile acid-glycine conjugate. It is a secondary bile acid produced by the action of enzymes existing in the microbial flora of the colonic environment.
||Glycyl-l-leucine is a dipeptide that appears to be a common substrate for glycyl-leucine dipeptidase.
||Glycyl-L-valine (H-Gly-Val-OH, Glycylvaline) is a dipeptide composed of glycine and valine. It is an incomplete breakdown product of protein digestion or protein catabolism.
||Glycylglycine (Diglycine, Diglycocoll, Glycine dipeptide), the simplest peptide made of two glycine molecules, is usually used in the synthesis of more complicated peptides.
||Glycyrrhetinic acid is a triterpenoid aglycone component of the natural product glycyrrhizinic acid and possesses remarkable anti-proliferative and apoptosis-inducing activity in various cancer cell lines.
||Glycyrrhizin (NSC 167409)
||Glycyrrhizin (NSC 167409, Glycyrrhizic Acid) is a direct HMGB1(high mobility group box 1) inhibitor that inhibits HMGB1-dependent inflammatory molecule expression and oxidative stress; modulates P38 and P-JNK but not p-ERK signalling; Also inhibits 11 beta-hydroxysteroid dehydrogenase and monoamine oxidase (MAO).
||Glyoxylic acid monohydrate
Glyoxylic acid monohydrate (2,2-Dihydroxyacetic acid) is an atmospherically relevant ketoacid.
||GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
||GMBS is a cross-linker with heterobifunction.
||GMX1778 (CHS828) is a potent and specific inhibitor of nicotinamide phosphoribosyltransferase (NAMPT) with IC50 and Kd of < 25 nM and 120 nM, respectively. GMX1778 induces programmed cell death with apoptotic features. Phase 1.
||GNE-0877 is a highly potent and selective leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 0.7 nM.
||GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with an IC50 of 4 nM for PI3Kα and Kiapp of 21 nM for mTOR.
||GNE-490 is a highly selective pan-PI3K inhibitor that demonstrates selectivity over mTOR.
||GNE-493 (compound 5) is a potent, selective and orally available dual inhibitor of pan-PI3-kinase and mTOR with IC50 of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR, respectively.
||GNE-617 is a highly potent inhibitor of NAMPT activity with an IC50 of 5 nM.
||GNE-781 (compound 19) is an orally active, highly potent and selective bromodomain inhibitor of cyclic adenosine monophosphate response element binding protein (CBP) with IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50 of 6.2 nM and 5100 nM, respectively. GNE-781 exhibits antitumor activity.
||GNF-6231 is a potent, orally active and selective Porcupine inhibitor with IC50 of 0.8 nM.
GNF-PF-3777 (8-Nitrotryptanthrin) is a selective human indoleamine 2,3-dioxygenase 2 (hIDO2) inhibitor which significantly reduces IDO2 activity with Ki of 0.97 μM.
||GNF351 is a potent antagonist of aryl hydrocarbon receptor (AHR). GNF351 interacts directly with the AHR ligand binding pocket and competes with a well-characterized photoaffinity AHR ligand for binding to the AHR with IC50 of 62 nM.
||Go 6983 (GOE 6983, Gö 6983) is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ and PKCδ with IC50 of 7 nM, 7 nM, 6 nM and 10 nM, respectively; less potent to PKCζ and inactive to PKCμ.
||GO-203 is a D-amino acid cell-penetrating peptide inhibitor of MUC1-C dimerization and thereby its oncogenic function.
||Go6976 (PD406976) is a potent PKC inhibitor with IC50 of 7.9 nM, 2.3 nM, and 6.2 nM for PKC (Rat brain), PKCα, and PKCβ1, respectively. Also a potent inhibitor of JAK2 and Flt3.
||Goitrin (DL-Goitrin, (R, S)-Goitrin, R,S-goitrin) is one of the main constituent of Radix isatidis (Banlangen) which is widely used as a traditional Chinese medicine for treating fever and removing toxic heat. Goitrin exhibits antiviral and antiendotoxin activity.
||Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.
||Goserelin is a luteinizing hormone releasing hormone (LHRH) agonist, which is used to suppress production of the sex hormones. Goserelin acetate is an injectable gonadotropin releasing hormone superagonist (GnRH agonist).
||Gossypol (BL 193) is an orally-active polyphenol isolated from cotton seeds and roots. Gossypol is a potent inhibitor of 5α-reductase 1 and 3α-hydroxysteroid dehydrogenase with IC50 of 3.33 μM and 0.52 μM in cell-free assay, respectively. Gossypol also inhibits the binding of BH3 peptide to Bcl protein with IC50 of 0.4 μM and 10 μM for Bcl-XL and Bcl-2, respectively. Gossypol induces apoptosis and cell growth inhibition in various cancer cells.
||Gossypol Acetate (Gossypol Acetic acid, Pogosin, AT101) is a polyphenolic aldehyde that permeates cells and acts as an inhibitor for several dehydrogenase enzymes such as lactate dehydrogenase, NAD-linked enzymes.
||GOT1 inhibitor 2c
||GOT1 inhibitor 2c is a non-covalent glutamate oxaloacetate transaminase 1 (GOT1) inhibitor with IC50 of 8.2 μM.
||GPCR Compound Library
||A unique collection of 1325 small molecules targeting G protein coupled receptors for high throughput screening (HTS) and high content screening (HCS).
||GPNA (L-γ-Glutamyl-p-nitroanilide) is a potent and selective inhibitor of the glutamine (Gln) transporter ASCT2(SLC1A5) with Ki of 55 µM.
||GR 103691 is a potent and selective antagonist of dopamine D3 receptor with Ki of 0.4 nM.
||GR 125743 is an antagonist of 5-HT1B/1D receptor.
||GRA Ex-25 is a glucagon receptor inhibitor with IC50 of 56 nM and 55 nM for rat and human glucagon receptors, respectively.
||Gramine (Donaxine) is a natural indole alkaloid isolated from giant reed, acts as an active adiponectin receptor (AdipoR) agonist, with IC50 of 3.2 µM and 4.2 µM for AdipoR2 and AdipoR1, respectively. Gramine is also a human and mouse β2-Adrenergic receptor (β2-AR) agonist.
||Granisetron (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy.
||Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.
||Grape Seed Extract
||Grape Seed Extract are industrial derivatives from whole grape seeds that have a great concentration of vitamin E, flavonoids, linoleic acid, and OPCs.
||Grapiprant (CJ-023,423, AT-001, AAT-007, RQ-00000007, CJ-23423) is a novel selective EP4 Prostaglandin Receptor inhibitor with Ki of 20 nM and 13 nM for rat EP4 receptor and human EP4 receptor, respectively.
||Grazoprevir anhydrous (MK5172) is a Hepatitis C Virus NS3/4A Protease inhibitor with IC50 values of 7pM, 4pM, and 62pM for HCV genotype 1a, 1B, and 4 respectively.
||GRB2 Rabbit Recombinant mAb
||GRB2 Rabbit Recombinant mAb detects endogenous level of total GRB2.
Green DND-26 is a green fluorescent dye that stains acidic compartments in live cells with excitation/emission maxima ∽504/511nm.
||Griseofulvin, a production from some strains of the mold Penicillium griseofulvumam, is able to inhibit cell mitosis by interfering with microtubule function.
||GRK2 Rabbit Recombinant mAb
||GRK2 Rabbit Recombinant mAb detects endogenous level of total GRK2.
||GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLPro)/deubiquitinase with IC50 of 0.6 μM and Ki of 0.49 μM. GRL0617 inhibits SARS-CoV viral replication in Vero E6 cells with EC50 of 15 microM and has no associated cytotoxicity.
||GRP-60367 is an inhibitor of rabies virus (RABV) entry that specifically targets the RABV G protein.
||GRP-60367 hydrochloride is an inhibitor of rabies virus (RABV) entry that specifically targets the RABV G protein.
||GS-441524, a molecular precursor to a pharmacologically active nucleoside triphosphate molecule, is a potent inhibitor of feline infectious peritonitis virus (FIPV) with EC50 of 0.78 μM.
||GS-444217 (ASK1-IN-1) is a potent, selective, orally available and ATP-competitive inhibitor of ASK1 (apoptosis signal-regulating kinase 1) with IC50 of 2.87 nM.
||GS143 is a selective inhibitor of IκBα ubiquitination with IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 suppresses NF-κB activation and transcription of target genes. GS143 exhibits anti-asthma effect.
||GS967 (GS458967) is a potent and selective inhibitor of late INa with anti-arrhythmic actions.
||GSK-114 is a selective inhibitor of TNNI3 Interacting Kinase (TNNI3K) with IC50 of 25 nM. GSK-114 shows significant bias for TNNI3K over B-Raf with IC50 of 1000 nM, exceptional broad spectrum kinase selectivity and adequate oral exposure to enable its use in cellular and in vivo studies.
||GSK2837808A is a selective LDHA (lactate dehydrogenase A) inhibitor with IC50 of 2.6 nM and 43 nM for hLDHA and hLDHB, respectively.
||GSK5959 is a potent and selective BRPF1 bromodomain inhibitor with an IC50 of 80 nM and exhibits >100-fold selectivity for BRPF1 over a panel of 35 other bromodomains, including BRPF2/3 and BET family bromodomains.
||GSK J4 HCl (GSKJ4 HCl)
||GSK J4 HCl is a cell permeable prodrug of GSK J1, which is the first selective inhibitor of the H3K27 histone demethylase JMJD3 and UTX with IC50 of 60 nM in a cell-free assay and inactive against a panel of demethylases of the JMJ family.
||GSK'547 is a highly selective and potent inhibitor of RIP1 (RIPK1) exhibiting a 400-fold improvement in mouse pharmacokinetic oral exposure compared with GSK'963
||GSK'872 (GSK2399872A) is a potent and selective RIP3 kinase inhibitor which binds RIP3 kinase domain with high affinity (IC50=1.8 nM) and inhibits kinase activity with IC50 of 1.3 nM. It has minimal cross-reactivity.
||GSK'963 is a chiral small-molecule inhibitor of RIP1 kinase (RIPK1) with an IC50 of 29 nM in FP binding assays. It is >10 000-fold selective for RIP1 over 339 other kinases.
||GSK 2881078 is a nonsteroidal selective modulator of androgen receptor that is potentially used for the treatment of cachexia.
||GSK2894631A is an inhibitor of hematopoietic PGD synthase (HPGDS).
||GSK-F1 is a novel potent inhibitor of phosphatidylinositol 4-kinase alpha (PI4KA).
||GSK046 (iBET-BD2) is a selective and orally active inhibitor of BET (bromodomain and extraterminal domain) with IC50 of 264 nM, 98 nM, 49 nM and 214 nM for BRD2BD2, BRD3BD2, BRD4BD2 and BRDTBD2, respectively. GSK046 exhibits immunomodulatory activity.
||GSK1016790A (GSK101) is a novel, potent activator of TRPV4 (transient receptor potential vanilloid 4) with EC50 of 34nM in choroid plexus epithelial cells.
||GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively. Phase 1.
||GSK106 is a negative control compound that can be used in binding and functional assays for PAD4 inhibitors.
||GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.
||GSK121 trifluoroacetate is a selective inhibitor of PAD4.
||GSK126 (GSK2816126A, GSK2816126) is a potent, highly selective EZH2 methyltransferase inhibitor with IC50 of 9.9 nM, >1000-fold selective for EZH2 over 20 other human methyltransferases.
||GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2.
||GSK137647A (GSK 137647) is a selective, non-carboxylic agonist of free fatty acid receptor 4 (FFA4/GPR120) with EC50 of 501 nM.
GSK1614343 is a novel selective and potent GHSR antagonist with no partial agonist properties.
||GSK180736A (GSK180736), developed as a Rho-associated, coiled-coil-containing protein kinase inhibitor, binds to GRK2(G protein-coupled receptor kinase 2) with logIC50 pf -6.6 (logIC50 -4.0 for GRK5 and >-3 for GRK1); ≥400-fold selective for GRK2 over both GRK1 and GRK5.
||GSK1838705A is a potent IGF-1R inhibitor with IC50 of 2.0 nM, modestly potent to IR and ALK with IC50 of 1.6 nM and 0.5 nM, respectively, and little activity to other protein kinases.
||GSK1904529A (GSK 4529) is a selective inhibitor of IGF-1R and IR with IC50 of 27 nM and 25 nM in cell-free assays, >100-fold more selective for IGF-1R/InsR than Akt1/2, Aurora A/B,B-Raf, CDK2, EGFR etc.
||GSK199 is a selective inhibitor of PAD4 with IC50 of 200 nM in the absence of calcium.
||GSK2193874 is an orally active, potent, and selective blocker of transient receptor potential vanilloid 4 (TRPV4) with IC50 values of 0.04 and 0.002 μM for hTRPV4 and rTRPV4, respectively.
||GSK2200150A is identified by high-throughput screening (HTS) campaign that can be used as an anti-tuberculosis (TB) agent.
||GSK2256098 is a potent, selective, reversible, and ATP competitive FAK kinase inhibitor with apparent Ki of 0.4 nM. GSK2256098 inhibits cancer cell growth and induces apoptosis.
||GSK2292767 is a potent and selective PI3Kδ inhibitor.
||GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7.Phase 2.
||GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed. GSK2606414 impairs GANT-61 induced autophagy in NB cells with MYCN amplification. GSK2606414 exacerbates ER stress-induced apoptosis in HCT116 cells while reduces the apoptosis in SIL1 KD HeLa cells.
||GSK2636771 is a potent, orally bioavailable and selective inhibitor of PI3Kβ with >900-fold selectivity over PI3Kα/PI3Kγ and >10-fold over PI3Kδ. Sensitive to PTEN null cell lines.
||GSK2643943A is an inhibitor of deubiquitylating enzyme (DUB) with IC50 of 160 nM for USP20/Ub-Rho.
||GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM in a cell-free assay, 500-fold greater against a panel of 300 kinases. GSK2656157 decreases apoptosis and inhibits excessive autophagy.
||GSK269962A HCl (GSK269962B, GSK269962) is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
||GSK2795039 is an inhibitor of NADPH oxidase 2 (NOX2) with pIC50 of 6.57 for NOX2-mediated activation of HRP/Amplex Red. GSK2795039 inhibits reactive oxygen species (ROS) production, NADPH consumption and reduces apoptosis.
||GSK2830371 is an orally active, allosteric Wip1 phosphatase inhibitor with IC50 of 6 nM.
||GSK2838232, a betulin derivative, is an inhibitor of human immune virus (HIV) maturation which is potential for the treatment of chronic HIV infection.
||GSK2879552 2HCl is a potent, selective, orally bioavailable, irreversible LSD1 inhibitor with Kiapp of 1.7 μM. Phase 1.
||GSK2981278 is a highly potent and selective inverse agonist for RORγ.
||GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase (RIPK1) inhibitor with the IC50 value of 16 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.
||GSK2983559 (compound 3)
||GSK2983559 (compound 3, RIP2 kinase inhibitor 1, RIPK2-IN-1) is a potent inhibitor of receptor interacting protein 2 (RIP2) kinase with good kinase specificity.
||GSK3 Inhibitor XIII
||GSK3 Inhibitor XIII (GSK3i XIII) is an ATP-binding site inhibitor of GSK-3.
||GSK3117391 (GSK3117391A, HDAC-IN-3) is a potent histone deacetylase (HDAC) inhibitor.
||GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities.
||GSK3179106 is a potent, selective, and gut-restricted pyridone hinge binder small molecule RET (c-RET) kinase inhibitor with a RET IC50 of 0.3 nM and is efficacious in vivo.
||GSK3368715 (EPZ019997) 3HCl
||GSK3368715 is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Kiapp vaules ranging from 1.5 to 81 nM.
||GSK343 is a potent and selective EZH2 inhibitor with IC50 of 4 nM in a cell-free assay, showing 60 fold selectivity against EZH1, and >1000 fold selectivity against other histone methyltransferases. GSK343 induces autophagy.
||GSK3685032 is a non-time-dependent, highly selective enzymatic inhibitor of DNA methyltransferase (DNMT1) with IC50 of 0.036 μM, and over 2500-fold more selective than DNMT3A/3L and DNMT3B/3L.
||GSK369796 Dihydrochloride (N-tert-butylisoquine) is an inhibitor of hERG potassium ion channel repolarization with IC50 of 7.5 μM. GSK369796 Dihydrochloride is an affordable and effective 4-aminoquinoline antimalarial.
||GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.
GSK3987 is a potent and specific liver X receptor (LXR) dual agonist of LXRalpha and LXRbeta. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC(50)s of 40 nM.
||GSK429286A (RHO-15) is a selective inhibitor of ROCK1 and ROCK2 with IC50 of 14 nM and 63 nM, respectively.
||GSK461364 (GSK461364A) inhibits purified Plk1 with Ki of 2.2 nM in a cell-free assay. It is more than 1000-fold selective against Plk2/3. Phase 1.
||GSK467 is a cell penetrant and selective inhibitor of KDM5B (JARID1B/PLU1) with Ki of 10 nM. GSK467 shows apparent 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other JmJ family members.
||GSK4716 is a selective agonist of Estrogen-Related Orphan Nuclear Receptors ERR and ERRγ with an IC50 of 2 µM in the ERRγ FRET assay.
||GSK481 is a RIP1(Receptor Interacting Protein Kinase1, RIPK1) inhibitor. Inhibition of RIP1 has been shown to hinder cell necrotic death.
||GSK484 HCl, a benzoimidazole derivative, is a selective and reversible inhibitor of peptidylarginine deiminase 4 (PAD4) with IC50 of 50 nM in the absence of Calcium.
||GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.
||GSK583 is a highly potent and selective inhibitor of RIP2 kinase with IC50 of 5 nM. GSK583 also inhibits both TNF-α and IL-6 production with IC50 of ~200 nM in explant cultures.
||GSK591 (EPZ015866, GSK3203591) is a potent selective inhibitor of the arginine methyltransferase PRMT5 with IC50 of 4 nM.
||GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.
||GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively.
||GSK690693 is a pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects Unc-51-like autophagy activating kinase 1 (ULK1) activity, robustly inhibits STING-dependent IRF3 activation. Phase 1.
||GSK805 (JNJ 56914845, GSK-2336805) is a potent and orally bioavailable RORγt inhibitor.
||GSK8612 is a highly potent and selective inhibitor for TBK1 (Tank-binding Kinase-1) with pKd of 8.0. Within 10-fold affinity with respect to TBK1, no off-targets of GSK8612 could be identified.
||GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183. GSK923295 induces post-mitotic apoptosis. Phase 1.
||GSK962 is a negative control for GSK963 which is a highly potent and selective RIP1 inhibitor.
||GsMTx4 (Grammostola spatulata mechanotoxin 4, M-theraphotoxin-Gr1a, M-TRTX-Gr1a) is a spider venom peptide that inhibits cationic mechanosensitive channels (MSCs).
||Guadecitabine (SGI-110, S-110) is a next-generation hypomethylating agent whose active metabolite decitabine has a longer in-vivo exposure time than intravenous decitabine.
||Guaiacol (O-methoxyphenol, 2-hydroxyanisole, O-methylcatechol) is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. It is a precursor to various flavorants, such as eugenoland vanillin. Guaiacol, a phenolic compound isolated from Guaiac resin, inhibits LPS-stimulated COX-2 expression and NF-κB activation. Anti-inflammatory activity.
||Guaiazulene (Azulon, Vetivazulen) is a bicyclic sesquiterpene that is a constituent of some essential oils, mainly oil of guaiac and chamomile oil, which also serve as its commercial sources.
||Guaifenesin is an expectorant used to relieve chest congestion.
||Guanabenz (GBZ, GA, Wytensin, Wy-8678) is an orally active central alpha 2-adrenoceptor (α2 adrenergic receptor) agonist with antihypertensive action.
||Guanabenz Acetate (WY-8678) is an selective agonist of α2a-adrenergic receptor, α2b-adrenergic receptor and α2c-adrenergic receptor with pEC50 of 8.25, 7.01 and ~5, respectively.
||Guanethidine monosulfate is an antihypertensive agent that acts by inhibiting selectively transmission in post-ganglionic adrenergic nerves.
||Guanfacine Hydrochloride (Tenex, Intuniv) is a selective α2A-adrenoceptor agonist with anti-hypertensive effect.
||Guanidine HCl (Aminoformamidine), the crystalline compound of strong alkalinity formed by the oxidation of guanine, is a normal product of protein metabolism and a protein denaturant.
||Guanidinoacetic acid (Guanidino acetic acid, GAA, Glycocyamine, Guanidinoacetate), the natural precursor of creatine, is under investigation as a dietary agent. Guanidinoacetic acid exhibits potential ergogenic benefits for physically active men and women.
||Guanine is one of the four main nucleobases found in the nucleic acids DNA and RNA.
||Guanosine is a purine nucleoside comprising guanine attached to a ribose (ribofuranose) ring via a β-N9-glycosidic bond.
||Guanosine 5'-monophosphate disodium salt
||Guanosine 5′-monophosphate (GMP, 5'-Guanylic acid, guanylic acid, guanosine monophosphate) is a ribonucleoside monophospate which upon phosphorylation to GTP becomes incorporated into ribonucleic acids (RNAs) by various RNA polymerase(s).
||Guanosine 5'-triphosphate trisodium salt
Guanosine 5'-triphosphate (5'-GTP, Guanosine triphosphate, H4GTP) trisodium salt is an enhancer of myogenic cell differentiation in a murine cells. Guanosine 5'-triphosphate trisodium salt up-regulates miRNA (specifically miR133a and miR133b) and myogenic regulator factor and induces human myogenic precursor cells to release exosomes stuffed with guanosine based molecules (mainly guanosine) in the extracellular milieu.
||Gusacitinib (ASN-002) is a novel and potent dual inhibitor of spleen tyrosine kinase (SYK) and Janus kinases (JAK) with IC50 values of 5-46 nM in biochemical assays.
||Gut Microbial Metabolite Library
||A unique collection of 140 gut microbial metabolites used for high throughput screening(HTS) and high content screening(HCS).
GV-58 is a novel, selective N-type and P/Q-type Ca2+ channels agonist with IC50s of 7.21 μM and 8.81 μM, respectively.
||GW 284543 hydrochloride
||GW 284543 hydrochloride (UNC 10225170) is a selective inhibitor of MEK5.
GW 610 (NSC 721648), a simple fluorinated 2-arylbenzothiazole, shows potent and aelective inhibitory activity against lung, colon, and breast cancer cell lines.
||GW0742 is a potent and highly selective PPARβ/δ agonist, with IC50 of 1 nM, with 1000-fold selectivity over hPPARα and hPPARγ.
||GW2580 (SC-203877) is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.
||GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.
||GW406108X (GW108X) is an inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in the ATPase assay. GW406108X inhibits recombinant ULK1 kinase activity with a pIC50 of 6.37 and blocks autophagy in cells, without affecting the upstream signalling kinases mTORC1 and AMPK.
||GW4064 is an agonist of farnesoid X receptor (FXR) with EC50 of 65 nM in CV1 cell line and displays no activity at other nuclear receptors at concentrations up to 1 μM. GW4064 stimulates autophagy in MCF-7 cells.
||GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.
||GW4869 (GW69A, GW554869A) is a neutral, noncompetitive inhibitor of sphingomyelinase (SMase) with an IC50 of 1 μM. It is selective for N-SMase, and does not inhibit acid SMase at up to at least 150 μM.
||GW5074 is a potent and selective c-Raf inhibitor with IC50 of 9 nM, no effect on the activities of JNK1/2/3, MEK1, MKK6/7, CDK1/2, c-Src, p38 MAP, VEGFR2 or c-Fms is noted. GW5074 inhibits LK-induced apoptosis.
||GW604714X is a potent and selective inhibitor of mitochondrial respiration supported by pyruvate.
||GW 6471 is a potent antagonist of PPARα with IC50 of 0.24 μM.
||GW842166X is a potent and highly selective agonist of cannabinoid receptor CB2 receptor with EC50 of 63 nM, shows no significant activity at CB1 receptor. Phase 2.
||GW9662 is a selective PPAR antagonist for PPARγ with IC50 of 3.3 nM in a cell-free assay, with at least 10- to 600-fold functional selectivity in cells with PPARγ versus PPARα and PPARδ.
||Gynostemma Extract (Gynostemma Pentaphyllum, Gypenoside) is a saponins extract derived from the Gynostemma pentaphyllum.
||Gypenoside (GP) is the predominant effective component of Gynostemma pentaphyllum and possesses capacities against inflammation and oxidation.
||Gypenoside XVII (GP-17, Gynosaponin S), a ginsenoside found in Panax species, has neuroprotective effects and is widely used to prevent cardiovascular disease.GP-17 treatment predominantly up-regulating the expression of ERα but not ERβ.
||GYY4137 is a novel, water-soluble hydrogen sulfide (H2S)–releasing molecule with vasodilator and antihypertensive activity. GYY4137 shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway. GYY4137 also shows anti-inflammatory activity.
||β-Glycerophosphate sodium salt hydrate
||β-Glycerophosphate (sodium salt hydrate) is a potent protein phosphatase inhibitor.