product results for Drug Repurposing for Anticancer Indications
Searches related to Drug Repurposing for Anticancer Indications :
- Inhibitors (173)
- Compound Libraries (10)
- Natural Products (16)
- Kit Products (1)
Catalog No. Product Name Information Product Use Citations Product Validations S1267 Vemurafenib (PLX4032) Vemurafenib (PLX4032, RG7204) is a novel and potent inhibitor of B-RafV600E with IC50 of 31 nM in cell-free assay. 10-fold selective for B-RafV600E over wild-type B-Raf in enzymatic assays and the cellular selectivity can exceed 100-fold. Vemurafenib (PLX4032, RG7204) induces autophagy.
The regressing tumour microenvironment stimulates the outgrowth, infiltration and metastasis of drug-resistant clones. b, Bioluminescent signal of drug-resistant A375RTGL cells in vemurafenib-sensitive, A375 tumours, treated with vehicle or vemurafenib for 5 days (vehicle, n = 36; vemurafenib, n = 15 tumours). D, day. c, EdU incorporation in A375R-TGL cells in A375/A375R-TGL tumours treated with vehicle or vemurafenib for 4 days, as determined by FACS (vehicle, n = 8; vemurafenib, n = 6 tumours). d, Bioluminescent signal of A375R-TGL tumours alone, treated with vehicle or vemurafenib for 5 days (vehicle, n 5 38; vemurafenib, n = 15 tumours). e, Bioluminescent signal of TGLexpressing drug-resistant cancer cells (A375R, M249R4, PC9 and H2030) in drug-sensitive tumours (Colo800, LOX, UACC62, M249, H3122 and HCC827) treated with vehicle or drugs (vemurafenib, crizotinib and erlotinib) for 5 days (n (from left to right on the graph) = 6, 7, 12, 12, 9, 9, 25, 26, 9, 12, 12, 12, 16 and 11 tumours). f, Spontaneous lung metastasis by A375R cells in mice bearing A375/A375R-TGL tumours treated with vehicle or vemurafenib (10 days), visualized by BLI (n = 4).
S2457 Clindamycin HCl Clindamycin HCl inhibits protein synthesis by acting on the 50S ribosomal, used for the treatment of bacterial infections.
S3196 Azacyclonol Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.
S7057 LY2874455 LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.
A: Overall structure of LY2874455/FGFR4 complex. B: The diagram of LY2874455. C: Fo-Fc omit map of LY2874455 in the FGFR4/LY2874455 complex. The electron density is superimposed with the final model. D: The DFG motif conformation of FGFR4. Active ApoFGFR4 DFG-in conformation is shown in blue (PDB: 4QQT); FGFR4/Ponatinib DFG-out conformation is shown in yellow (PDB: 4UXQ); FGFR4/BLU9931 DFG-in conformation is shown in pink (PDB: 4XCU); FGFR4/LY2874455 DFG-in conformation is shown in grey (this work). LY2874455 is highlighted in brown.
S8179 BI-7273 BI-7273 is a potent, selective, and cell-permeable BRD9 BD inhibitor with IC50s of 19 nM and 117 nM for BRD9 and BRD7 respectively in alpha assay.
S4798 Benfotiamine Benfotiamine is a synthetic S-acyl derivative of thiamine (vitamin B1) and has been investigated for the treatment and prevention of Diabetic Nephropathy and Diabetes Mellitus, Type 2. Benfotiamine suppresses oxidative stress-induced NF-κB activation and prevents the bacterial endotoxin-induced inflammation.
S6233 Tartaric acid Tartaric acid is a white crystalline organic acid that occurs naturally in many plants, most notably in grapes. It has several applications for industrial and pharmaceutical use.
S6529 New NIH-12848 NIH-12848 is a specific PI5P4Kγ inhibitor with an IC50 of approximately 1 μM but does not inhibit the α and β PI5P4K isoforms at concentrations up to 100 μM.
S0000 New Cav 2.2 blocker 1 Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM.
S0494 New SM 324405 SM-324405 is a potent selective agonist of TLR7 with EC50 of 50 nM and antedrug characteristics.
S0706 New ISRIB ISRIB is an integrated stress response inhibitor and an experimental drug which reverses the effects of eIF2α phosphorylation with IC50 of 5 nM.
S7281 JIB-04 JIB-04 is a pan-selective Jumonji histone demethylase inhibitor with IC50 of 230, 340, 855, 445, 435, 1100, and 290 nM for JARID1A, JMJD2E, JMJD3, JMJD2A, JMJD2B, JMJD2C, and JMJD2D in cell-free assays, respectively.
G, Western blot analyses to monitor the amount of H3K9me3 in the presence of rhein and MMS (upper panel) and under the treatment of JIB-04 (lower panel).
S7337 SH-4-54 SH-4-54 is a potent STAT inhibitor with KD of 300 nM and 464 nM for STAT3 and STAT5, respectively.
Expression of indicated proteins in PRL-stimulated INS-1 cells without (control, white bars) or with (black bars) STAT inhibitor (SH-4-54).
S4566 DL-Panthenol DL-panthenol is a racemic mixture of D and L form of panthenol,a provitamin of B5.
S8190 CPI-637 CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor with IC50 values of 0.03 μM and 0.051μM for CBP and EP300 respectively in TR-FRET assay. It is highly selective against other bromodomains, displaying substantial biochemical activity only against BRD9.
S5501 Hydrocortisone acetate Hydrocortisone Acetate is the synthetic acetate salt form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive properties.
S5739 Nebivolol Nebivolol is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and also for left ventricular failure.
S0001 New GSK137647A GSK137647A is a selective FFA4 agonist with pEC50 of 6.3, 6.2, and 6.1 for human, Mouse and Rat FFA4, respectively.
S0495 New BI-671800 BI-671800 is a highly specific and potent antagonist of chemoattractant receptor-homologous molecule on Th2 cells (DP2/CRTH2) with IC50 of 4.5 nM and 3.7 nM for PGD2 binding to CRTH2 in hCRTH2 and mCRTH2 transfected cells, respectively. BI-671800 has potential for the treatment of poorly controlled asthma.
S1268 IC-87114 IC-87114 is a selective PI3Kδ inhibitor with IC50 of 0.5 μM in a cell-free assay, 58-fold more selective for PI3Kδ than PI3Kγ, and over 100-fold more selective than PI3Kα/β.
S1653 Tretinoin Tretinoin, which is a ligand for both the retinoic acid receptor (RAR) and the retinoid X receptor (RXR), can induce granulocytic differentiation and apoptosis in acute promyelocytic leukemia (APL) cells.
HL60 differentiation measured by expression of CD11b (flow cytometry) after a single dose exposure to HH1 or MC180295 for 4 days. 1 mM ATRA and high concentrations of DMSO (1.25%) were used as positive controls.
S2459 Clozapine Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
Michaelis-Menten plots illustrate the effects of PGD, individual radix paeonia (Pr) and radix glycyrrhiza (Gr) preparations, and the two individual preparations in combination on the formation of N-demethyl-clozapine (A) and clozapine-N-oxide (B) in the human liver microsomes. Serial concentration of clozapine was coincubated in the presence of herbal preparations. The absence of herbal preparations serves as control (CON).
S7285 NMS-873 NMS-873 is an allosteric and specific p97 inhibitor with IC50 of 30 nM that demonstrates potent selectivity for VCP/p97 compared to a panel of other AAA ATPases, Hsp90, and 53 additional analyzed kinases (IC50s >10 μM).
(E) The mDPC level induced by HN2 in the presence of MG132 or NMS-873. MG132 or NMS-873 were added for 3 h after HN2 exposure and then replaced by normal medium until 24 h.
S4567 Eprodisate disodium Eprodisate Disodium is the orally available disodium salt form of Eprodisate, a small-molecule, orally bioavailable, inhibitor of AA-amyloid fibrillogenesis.
Fostamatinib inhibits activation of Syk and BTK BCWM.1 and MWCL-1 cells treated with either vehicle or fostamatinib at the indicated concentrations for two hours were harvested and lysed, and protein extracts were analyzed by Western blotting. The activation status of Syk (A, B) and BTK (C) was probed with phospho-specific antibodies using β-Actin as well as the levels of total, non-phosphorylated Syk and BTK as controls. Data shown are representative of one of three independent experiments.
S5224 Adrafinil Adrafinil is a mild central nervous system stimulant drug directly affecting CNS function. It is used to relieve excessive sleepiness and inattention in elderly patients.
S5352 Cefminox Sodium Cefminox Sodium is the sodium salt form of cefminox, a semi-synthetic, second-generation, beta-lactamase-stable cephalosporin with antibacterial activity.
S9363 Coumarin 151 Coumarin 151 is a fluorescent tracer used for the detection of proteinases.
S5741 Quetiapine Quetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine have moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.23, 5.74, 7.54, 5.55.
S6235 Sodium dehydroacetate Sodium dehydroacetate is the sodium salt of dehydroacetic acid, a fungicide and bactericide that is commonly used as a food preservative. Sodium dehydroacetate is a preservative that is used in the formulation of cosmetics and personal care products in order to extend the shelf-life by preventing microbial contamination.
S8832 New Branebrutinib (BMS-986195) Branebrutinib (BMS-986195) is a potent inhibitor of BTK with IC50 values of 0.1 nM, 0.9 nM, 1.5 nM, 5 nM for BTK, TEC, BMX, TXK, respectively.
S0496 New PF-04995274 PF-04995274 is a potent, high-affinity, orally active and partial agonist of serotonin 4 receptor (5-HT4R) with EC50 range of 0.26-0.47 nM and Ki range of 0.15-0.46 nM for human 5-HT4A/4B/4D/4E. PF-04995274 has EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E and Ki of 0.30 nM for rat 5-HT4S. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
S0708 New CGK733 CGK733 is a potent inhibitor of ATM/ATR that can be used for the research of cancer.
S1003 Linifanib (ABT-869) Linifanib (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Phase 3.
(B and C) KMCH-1 cells were plated alone (monoculture) or together with PDGF-BB-secreting LX-2 cells (co-culture) in a transwell insert co-culture system (KMCH-1 cells in the bottom wells and LX-2 cells in the inserts; 1:1 ratio) for 2 days. Cells were treated as indicated with vehicle, rhTRAIL (10 ng/ml for 6 h on day 2), rhTRAIL plus imatinib [rhTRAIL:10 ng/ml for 6 h on day 2; Imatinib: 5 μmol/L for 24 h (day2)], or rhTRAIL plus linifanib [rhTRAIL: 10 ng/ml for 6 h on day 2; Linifanib:0.5 μmol/L for 24 h (day2)]. After rhTRAIL treatment for 6 h,KMCH-1 cells were analysed for apoptotic nuclear morphology by DAPI-staining (B) and for DNA fragmentation by transferasemediated dUTP nick end labelling assay (C) with quantification of apoptotic nuclei by fluorescence microscopy.
S1683 Ipratropium Bromide Ipratropium Bromide is an antagonist of M3 type muscarinic acetylcholine receptors, used for the treatment of chronic obstructive pulmonary disease (COPD).
S2460 Pramipexole Pramipexole is a partial/full D2S, D2L, D3, D4 receptor agonist with a Ki of 3.9, 2.2, 0.5 and 5.1 nM for D2S, D2L, D3, D4 receptor, respectively.
S3005 Paroxetine HCl Paroxetine HCl is an antidepressant drug of the SSRI type.
S8071 UNC0638 UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets.
S7282 NMS-E973 NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases.
(D) Representative images of paraffin-embedded tumor sections were analyzed by active caspase-3 staining. (E) Representative images of paraffin-embedded tumor sections analyzed by TUNEL staining.
S3621 Pazufloxacin mesylate Pazufloxacin Mesylate, also known as Pazucross and T-3762, is a quinolone antibacterial agent used for the intravenous therapy of several infections.
S5361 Bendazac Bendazac is a non-steroidal anti-inflammatory drug that delays the cataractogenic process. It may act by preventing protein denaturation.
S0497 New JNJ-42165279 JNJ-42165279 is an inhibitor of FAAH with IC50 of 70 nM and 313 nM for hFAAH and rFAAH, respectively.
S5269 J147 J147, a curcumin derivative, is a potent neurogenic and neuroprotective compound developed for the treatment of neurodegenerative conditions associated with aging.
S5753 Setipiprant(ACT-129968) Setipiprant(ACT-129968, KYTH-105) is a selective, orally available antagonist of the prostaglandin D2 receptor 2 (DP2) that that has been shown to have greater specificity for DP2 (CRTH2) than for DP1.
S5871 Trans-Tranilast Trans-Tranilast is an antiallergic drug, used to treat bronchial asthma, allergic rhinitis and atopic dermatitis.
S2462 Donepezil HCl Donepezil is a specific and potent AChE inhibitor for bAChE and hAChE with IC50 of 8.12 nM and 11.6 nM , respectively.
Donepezil-mediated eACh activity in vitro. After being cultured in serum-free EBM-2, HUVECs were treated with donepezil at a concentration of 10 umol/L for 24 hours. E and F: Representative images (x 400 magnification) of anti-ChAT and -VAChT immunofluorescence. Scale bar: 50 um. ChAT indicates choline acetyltransferase; eACh, endothelium-derived acetylcholine; EBM-2, endothelial basal medium 2; HUVECs, human umbilical vein endothelial cells; PCR, polymerase chain reaction; VAChT, vesicular acetylcholine transporter.
S3207 Iopromide Iopromide is a low osmolar, non-ionic X-ray contrast agent for intravascular administration. It functions as a contrast agent by opacifying blood vessels in the path of flow of the contrast agent, permitting radiographic visualization of the internal structures until significant hemodilution occurs.
S8030 Plerixafor (AMD3100) Plerixafor (AMD3100) is a chemokine receptor antagonist for CXCR4 and CXCL12-mediated chemotaxis with IC50 of 44 nM and 5.7 nM in cell-free assays, respectively.
BLI of NSG mice engrafted with BV173, treated with no therapy (control), plerixafor: 1 mg/kg IP daily, ESKM 100 ug twice weekly, and a combination of ESKM and plerixafor. (A) Logarithmic plot of BLI of leukemia growth measured weekly. Error bars are 5-95% confidence intervals. There was a small but not significant difference between ESKM and combination treated group. (B) End of therapy (day 34) BLI.
S7204 Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium Fosbretabulin (Combretastatin A4 Phosphate (CA4P)) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Phase 3.
Real-time hemodynamic changes in the tumor upon administration of CA4P. Panel A shows the MRI anatomical reference of the tumor, followed by sO2 maps of a slice of brain showing the largest cross section of the tumor at time points 0, 1, 4 and 6 h. post CA4P administration. Panel B shows the real-time sO2 changes in the tumor and contralateral brain occurring immediately post CA4P administration over 1 hour in a representative animal. SD is represented by lighter shades on the graph. Panel C shows the real-time sO2 changes in the tumor and contralateral brain occurring immediately post CA4P administration (n = 4). Panel D shows the quantification of hypoxia in tumors using CAIX as a marker at times 0 (n = 3), 1 (n = 4) and 6 h. (n = 3) post CA4P administration. Unpaired t-test showed statistically significant difference in CAIX staining at 1 hour post CA4P administration compared to 0 and 6 hours. ** ‐ P > 0.01. Black dotted circle and Red full circle denote the ROIs drawn at the tumor and contralateral brain respectively to compute the sO2.
S4570 Halothane Halothane is a general inhalation anesthetic used for induction and maintenance of general anesthesia.
S8575 A2AR antagonist 1 A2AR antagonist 1 is a potent A2AR (Adenosine A2A Receptor) antagonist with Ki values of 4 nM and 264 nM for A2AR and A1R, respectively.
S5537 Tizanidine Tizanidine is an imidazoline derivative and a centrally acting α2 adrenergic agonist used as a muscle relaxant for therapy of acute muscle spasms and chronic spasticity.
S1006 Saracatinib (AZD0530) Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Phase 2/3.
C and D, in vivo subcutaneous tumor growth curves (C) and tumor weight quantification of intersected subcutaneous tumor tissues (D) of Huh7 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n =18). *, P < 0.05. E and F,in vivo subcutaneous tumor growth curves (E) and tumor weight quantification of intersected subcutaneous tumor tissues (F) of SK-Hep1 cells after stable LHBs expression under saracatinib treatment (25 mg/kg body weight daily for 4 weeks; n = 18). *, P < 0.05.
S1281 Aniracetam Aniracetam is a nootropics and neuroprotective drug.
S3008 Zaltoprofen Zaltoprofen is an inhibitor of COX-1 and COX-2 for treatment of arthritis.
S7060 PP1 PP1 is a potent and selective Src inhibitor for Lck/Fyn with IC50 of 5 nM/ 6 nM.
Three days postinfection, the permeability of ANDV- and mock-infected endothelial cell monolayers was determined as described for inhibitors at indicated times in the presence or absence of the kinase inhibitor PP1. The percent change in FITC-dextran over controls is presented as a measure of EC monolayer permeability. Data are derived from two independent experiments performed in triplicate with comparable results.
S7565 WH-4-023 WH-4-023 is a potent and orally active Lck/Src inhibitor with IC50s of 2 nM and 6 nM in cell-free assays, respectively. Exhibits >300-fold selectivity against p38α and KDR. Also potently inhibits SIK (IC50 values are 10, 22 and 60 nM for SIK 1, 2 and 3 respectively) and displays selectivity over a range of closely related kinases.
(G-I) WB analysis of total LCK, LCK Y505, and Src Y416 expression in ALL-SIL, CCRF-CEM, and TALL-1. Cells were treated with DMSO only (Ctrl), dasatinib, bosutinib, nintedanib, or WH-4-023 overnight at the compound concentrations corresponding to the GI50 at 48 hr. Bos, bosutinib; Das, dasatinib; Nint, nintedanib; WH, WH-4-023.
S4571 Hexylresorcinol Hexylresorcinol is an organic compound with local anaesthetic, antiseptic and anthelmintic properties, is a potent inhibitor of mushroom tyrosinase. The IC50 values of hexylresorcinol for monophenolase is 1.24 μM and for diphenolase is 0.85 μM.
S3997 Oxaceprol Oxaceprol is an anti-inflammatory drug used in the treatment of osteoarthritis.
S6245 N-Acetylglutamic acid N-Acetylglutamic acid is the first intermediate involved in the biosynthesis of arginine in prokaryotes and simple eukaryotes and a regulator in the process known as the urea cycle that converts toxic ammonia to urea for excretion from the body in vertebrates.
S6746 New APD668 APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively.
S0500 New Purvalanol B Purvalanol B (NG-95) is a potent and selective inhibitor of cyclin-dependent kinase (CDK) with IC50 of 6 nM, 6 nM, 9 nM and 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively.
S2467 Famciclovir Famciclovir is a guanine analogue antiviral drug used for the treatment of various herpesvirus infections.
S7008 PP2 PP2, a Src family kinase inhibitor, potently inhibits Lck/Fyn with IC50 of 4 nM/5 nM in cell-free assays, ~100-fold less potent to EGFR, inactive for ZAP-70, JAK2 and PKA.
Inhibition of PLCG1 phosphorylation by the silencing of DopEcR, ErGPCR, and Gq and the addition of inhibitors of RTK and Src. 5 µM SU6668 (RTK inhibitor) and 20 µM PP2 (Src inhibitor) were added to the cells for 30 min treatment before the 20E stimulation.
S5620 NSI-189 NSI-189, a small molecule with enhanced neurogenic activity, is a potential antidepressant for the treatment of major depressive disorder (MDD), cognitive impairment and neurodegeneration.
S6520 New WHI-P180 WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET and kinase insert domain receptor (KDR), respectively.
S0007 New RO 5028442 (RG7713) RG7713 (RO5028442) is a highly potent and selective Brain-Penetrant Vasopressin 1a (V1a) receptor antagonist with Ki of 1 nM and 39 nM for hV1a and mV1a, respectively.
S1283 Asenapine maleate Asenapine maleate is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder.
S3000 Carbazochrome sodium sulfonate (AC-17) Carbazochrome sodium sulfonate (AC-17) is an antihemorrhagic for use in the treatment of hemorrhoids.
S4004 Ethambutol 2HCl Ethambutol is a bacteriostatic antimycobacterial agent, which obstructs the formation of cell wall by inhibiting arabinosyl transferases.
S7291 TAK-632 TAK-632 is a potent pan-Raf inhibitor with IC50 of 8.3 nM and 1.4 nM for B-Raf(wt) and C-Raf in cell-free assays, respectively, showing less or no inhibition against other tested kinases.
Graph showing a concentration-dependent response of hypoxia-induced HIF-1α-NanoLuc activity to RAS-RAF-MEK-ERK pathway inhibitors: GDC-0994, PD-184352, selumetinib, TAK632, trametinib, and vemurafenib.
S5306 Forchlorfenuron (CPPU) Forchlorfenuron is a synthetic cytokinin that inhibits septins and exhibits anti-parasitic, anticancer, and anti-angiogenic activities.
S1008 Selumetinib (AZD6244) Selumetinib (AZD6244) is a potent, highly selective MEK inhibitor with IC50 of 14 nM for MEK1 and Kd value of 530 nM for MEK2. It also inhibits ERK1/2 phosphorylation with IC50 of 10 nM, no inhibition to p38α, MKK6, EGFR, ErbB2, ERK2, B-Raf, etc. Phase 3.
Stimulation response of p37d-expressing cells. (c) Western blot of 5 min serum stimulated HEK-293 cells stably expressing p37d, p110d or control, with the presence of inhibitors as indicated at the top.
S7292 RG2833 (RGFP109) RG2833 (RGFP109) is a brain-penetrant HDAC inhibitor with IC50 of 60 nM and 50 nM for HDAC1 and HDAC3 in cell-free assays, respectively.
The cells were treated with 1 μM RG2833 (HDAC1/3 inhibitor), 2 μM RGFP966 (HDAC3 inhibitor), 1 μM TSA (pan-HDAC inhibitor), or vehicle for 16 h in serum-free medium. Cell lysates were analysed by Western blotting for expression of SREBP-2 activated fragment, HMG-CoA reductase and APP. Shown are representative blots and quantifications with means ± SEM of the indicated number of independent experiments performed in duplicate. *p < 0.05; **p < 0.01; n.s., not significant in one-sample t-test.
S4935 Asunaprevir Asunaprevir is an orally bioavailable inhibitor of the hepatitis C virus enzyme serine protease NS3 that is necessary for protein processing required for viral replication.
S5048 Fosfomycin Disodium Fosfomycin is a bactericidal, low-molecular weight, broad-spectrum antibiotic, with putative activity against several bacteria, including multidrug-resistant Gram-negative bacteria, by irreversibly inhibiting an early stage in cell wall synthesis.
S5527 Salmeterol Salmeterol is a long-acting beta2-adrenergic receptor agonist with Ki value of 1.5 nM for WT β2AR and shows very high selectivity for the WT β2AR(β1Ki/β2Ki ratio of approximately 1500).
S5673 Mivacurium chloride Mivacurium chloride is a rapid, non-depolarising, neuromuscular blocking agent of short duration, used therefore as anesthetic, to provide skeletal muscle relaxation in minor surgical operations, in emergency surgical procedures of short to intermediate duration and during intubation of the trachea.
S8750 NGI-1(ML414) NGI-1 is an aminobenzamide-sulfonamide compound that targets both oligosaccharyltransferase (OST) isoforms and therefore may exhibit antiviral activity against flaviviruses.
S6251 Terephthalic acid Terephthalic acid, a raw material for polyethylene terephthalate (PET) production, is one of the most important chemicals in petrochemical industry.
S0009 New Asimadoline Asimadoline is a potent κ opioid receptor agonist with IC50 of 5.6 nM and 1.2 nM for guinea pig and human recombinant κ opioid receptor, respectively.
S0717 New Varenicline dihydrochloride Varenicline dihydrochloride is a partial agonist of α4β2 nicotinic acetylcholine receptor. Varenicline dihydrochloride is a prescription medication used for smoking cessation.
S1009 Dactolisib (BEZ235) Dactolisib (BEZ235, NVP-BEZ235) is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively. Inhibits ATR with IC50 of 21 nM in 3T3TopBP1-ER cell.
Three-dimensional responses of MCF7/IGF-1R cells to TAM (1 μM), E2 and IGF-1. Compared to parental MCF7 cells (a), MCF7/IGF-1R cells (b) in three-dimensional (3D) culture formed bigger acini in response to IGF-1 stimulation and displayed significant TAM resistance when treated with TAM (1 μM) + E2 + IGF-1, which was removable by kinase inhibitors BMS-536924, U0126 and BEZ235 (c). Cells (10,000/well) were seeded in 96-well plates. Acini were formed on 100% Matrigel and cultured for 14 days in starving medium containing 2% Matrigel and 5% charcoal/dextran-stripped fetal bovine serum with the treatments as indicated. Concentrations used: TAM (1 μM), E2 (1 nM) and IGF-1 (100 ng/mL). Confocal image original magnification, × 20. Red, rhodamine phalloidin (actin). Blue, Hoechst blue stain. Results are representative of two individual experiments.
S4920 b-AP15 b-AP15 is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.
A USP14 inhibitor directly inhibits OSCC cell proliferation and triggers apoptosis. (A-D) OSCC cells were treated with indicated doses of b-AP15 for 24 h. (A) Cell proliferation was monitored by CCK8 assay. b-AP15 dramatically decreased cancer cells viability in a dose-dependent manner (p < 0.01). All values represented means ± SD of three independent experiments and each was performed in triplicate. (B, C) Flow cytometry analysis indicated that b-AP15 triggered significant apoptosis of OSCC cells (p < 0.01). Data were obtained in more than three independent experiments. (D) Apoptosis-related proteins were examined by western blot analysis. Inhibition of USP14 with b-AP15 induced a massive increase of ubiquitinated proteins, which then triggered apoptosis of cancer cells, activating caspase 3 to induce cleavage of caspase 3 and PARP.
S5328 Gamithromycin Gamithromycin is a new macrolide antibiotic that is only registered for use in cattle to treat respiratory disorders such as bovine respiratory disease.
S5674 Lodoxamide Tromethamine Lodoxamide Tromethamine is the tromethamide salt form of lodoxamide, a synthetic mast cell stabilizing compound with anti-inflammatory activity.
S5872 Estradiol dipropionate Estradiol dipropionate (17-Beta-Estradiol-3,17-Dipropionate) is a semisynthetic, steroidal estrogen which has been used in hormone therapy for menopausal symptoms and low estrogen levels in women and in the treatment of gynecological disorders.
S6252 3-Hydroxypicolinic acid 3-Hydroxy picolinic acid is a picolinic acid derivative and is a member of the pyridine family. It is used as a matrix for nucleotides in MALDI mass spectrometry analyses
S0010 New Ralinepag Ralinepag is a potent, orally bioavailable and non-prostanoid prostacyclin (IP) receptor agonist with EC50 of 8.5 nM, 530 nM and 850 nM for human IP receptor, rat IP receptor and human DP1 receptor, respectively.
S0504 New SU14813 SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.
S1010 Nintedanib (BIBF 1120) Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.
Effect of BIBF 1120 on the accumulation of doxorubicin (Dox) and rhodamine 123. The accumulations of doxorubicin a, b and rhodamine 123 c, d were measured by flow cytometric analysis as described in "Materials and Methods". The results are presented as fold change in fluorescence intensity relative to control MDR cells. Columns, means of triplicate determinations; bars, SDs. **P<0.01 versus control group
S1286 Budesonide Budesonide is a glucocorticoid steroid for the treatment of asthma, non-infectious rhinitis.
S1703 Divalproex Sodium Divalproex Sodium, consisting of a compound of sodium valproate and valproic acid in a 1:1 molar relationship in an enteric coated form, is a HDAC inhibitor, used in the treatment for epilepsy.
Divalproex sodium increases the level of acetylated histone H3 level in ataxin-3-transfected HEK293 cells. Normal (15CAG) or expanded (77CAG) ataxin-3-transfected cells were treated with divalproex sodium (Selleck chemical, 0.3 mmol/L in DMSO, (+)) or with DMSO alone (−) 48 h after transfection. The cells were treated with divalproex sodium or DMSO over 6, 12, and 24 h. The Western blot was probed with antiacetylated histone H3, antihistone H3, and antiataxin-3. Antibodies include antihistone H3 and antiataxin-3 are used as controls. The x-axis shows the different treatment group. The y-axis represents the acetylated histone H3 values normalized to histone H3. Error bars represent the standard error of the mean. Data represent three independent experiments (n = 3). The data with a normal distribution were analyzed with Student’s t-test. *P < 0.05
S2572 Streptomycin sulfate Streptomycin sulfate is a sulfate salt of streptomycin that is a protein synthesis inhibitor.
S2840 Apalutamide (ARN-509) Apalutamide (ARN-509) is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.
ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: 20.0±5.5nM (ONC1-13B), 30.8±7.7nM (MDV3100), 38.4nM (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), 7.9uM (ONC1-13B), 16.3uM (MDV3100).
S7295 Apabetalone (RVX-208) Apabetalone (RVX-208) is a potent BET bromodomain inhibitor with IC50 of 0.510 μM for BD2 in a cell-free assay, about 170-fold selectivity over BD1. Phase 2.
Bromodomain 1 or 2 of BET family proteins is involved in 3T3-L1 adipogenesis. (A) LY294002, RVX208 and JQ1 were applied to differentiating 3T3-L1 from day 2 to day 6. Phenyl acetate (PA), known as a PPAR-γ agonist was used as a positive control. Cells were labeled with ORO (Bar=50nm). (B) Schematic representation of specificity of each chemical inhibitor for Bromodomain BD1 and 2 and quantitative analysis of ORO staining. The IDMR treatment without drugs (CTL) was used to define 100%. Data are reported as means ± sd (n=3); *** p<0.001 vs IDM control; ### p<0.001 vs IDMR control (-)-JQ1); +++ p<0.01 vs IDM of each condition; ns, non significant.
S4836 Nilutamide Nilutamide is a nonsteroidal antiandrogen (NSAA) with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). It is used in the treatment of prostate cancer.
S8727 Atuveciclib (BAY-1143572) Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.
S8679 BTK inhibitor 1 (Compound 27) BTK inhibitor 1 (compound 27) is an inhibitor of BTK with an IC50 of 0.11 nM for Btk and inhibits B cell activation in hWB with an IC50 of 2 nM.
S6644 New Radiprodil (RGH-896) Radiprodil (RGH-896) is a NR2B-selective NMDA receptor antagonist, initially developed for the treatment of neuropathic pain.
S1011 Afatinib (BIBW2992) Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively. Afatinib induces autophagy.
Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay.
S1287 Bumetanide Bumetanide (Bumex) is a loop diuretic of the sulfamyl category to treat heart failure. Bumetanide is a selective Na+-K+-Cl- cotransporter 1 (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively.
S8125 Pamapimod Pamapimod (R-1503, Ro4402257) is a novel, selective inhibitor of p38 mitogen-activated protein kinase. It inhibits p38α and p38β enzymatic activity with IC50 values of 0.014±0.002 and 0.48± 0.04 microM, respectively with no activity against p38delta or p38gamma isoforms.
S5073 Donepezil Donepezil is a piperidine based, potent, specific, non-competitive and reversible inhibitor of acetylcholinesterase (AChE) used for the treatment of mild to moderate dementia of the Alzheimer's type.
S5950 Fingolimod Fingolimod is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
S6543 New ZD-4190 ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.
S6638 New AMG-333 AMG-333 is a potent and highly selective antagonist of TRPM8 with IC50 values of 13 nM and 30 nM for human TRPM8 and rat TRPM8.
S0720 New PNU 282987 PNU 282987 is a potent agonist of α7-containing neuronal nicotinic acetylcholine receptors (nAChRs) with Ki of 26 nM for the rat receptor. PNU 282987 has negligible activity against α1β1γδ and α3β4 nAChRs as well as a panel of monoamine, muscarinic, glutamate, and GABA receptors, except 5-HT3 with Ki of 930 nM.
S1012 BMS-536924 BMS-536924 is an ATP-competitive IGF-1R/IR inhibitor with IC50 of 100 nM/73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1/2.
A, cell viability reduction. TC1889 cells were treated with pharmacological inhibitors against IGF-1R (NVP and BMS), as well as a neutralizing IGF-1R antibody (aIR3) and cell viability was assessed using MTT-assays. Mouse IgG1 antibody was employed as a reference control for the effects of aIR3 at respective concentrations. Assays were performed in sextuple. Data are expressed as the mean SD (n 3). B, induction of cell death. TC1889 cells were treated with pharmacological inhibitors against IGF-1R as well as a neutralizing IGF-1R antibody and cell death was evaluated by FACS-analyses following PI-staining. Data are expressed as the mean SD (n =3).
S2602 Acemetacin Acemetacin is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
S3114 Vitamin C Vitamin C is a water-soluble vitamin indicated for the prevention and treatment of scurvy.
S7298 AZ5104 AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor with IC50 of <1 nM, 6 nM, 1 nM, and 25 nM for EGFR (L858R/T790M), EGFR (L858R), EGFR (L861Q), and EGFR (wildtype), respectively. Phase 1.
S7918 Bromodeoxyuridine (BrdU) Bromodeoxyuridine (BrdU) is a nucleoside analog that competes with thymidine for incorporation into DNA, and used in the detection of proliferating cells.
Immunofluorescence microphotographs of proliferating ARPE-19 cell with BrdU (red) and DAPI (blue) staining after ARPE-19 cells were untreated or treated with AF (1.0 μM) in the absence or presence of EGF (100ng/ml) for 24 hours and then subjected to BrdU labeling for 4 hours, followed by immunostaining with anti-BrdU antibody and DAPI. Scale bar = 20μm.
S4578 Tyloxapol Tyloxapol is a nonionic liquid polymer of the alkyl aryl polyether alcohol type, used as a surfactant to aid liquefaction, removal of mucopurulent and bronchopulmonary secretions. It also blocks plasma lipolytic activity, and thus the breakdown of triglyceride-rich lipoproteins.
S8353 CPI-1205 CPI-1205 is an orally available selective inhibitor of the histone lysine methyltransferase EZH2 with IC50 values of 2 nM and 52 nM for EZH2 and EZH1 respectively. It has potential antineoplastic activity.
S5147 1,3,5-Trimethylpyrazole 1,3,5-Trimethylpyrazole is an intermediate product used for chemical synthesis.
S5081 Ceforanide Ceforanide is a new cephalosporin with antibacterial activity and has a longer elimination half-life than any currently available cephalosporin.
S8724 Lazertinib Lazertinib (YH25448,GNS-1480) is a potent, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively, showing much higher IC50 values aganist ErbB2 and ErbB4.
S6257 N-Acetylglucosamine N-Acetylglucosamine is a monosaccharide that usually polymerizes linearly through (1,4)-β-linkages. It may be helpful for the treatment of autoimmune diseases.
S6544 New SR-3029 SR-3029 is a potent and selective casein kinase 1δ/1ε (CK1δ/ε) inhibitor with IC50 values of 44 and 260 nM for CK1δ and CK1ε, respectively.
S0264 New BFMO (biogenic Fe-Mn oxides) BFMO (biogenic Fe-Mn oxides, defined as a mixture of biogenic Mn oxide (BMO) and Fe oxide) could eliminate or decrease Fe(II), Mn(II), and As(III&V) species simultaneously. BFMO can be used for As removal from water containing high concentrations of Fe(II) and Mn(II).
S0721 New Ticlopidine Ticlopidine is an inhibitor of adenosine diphosphate (ADP) receptor and an antiplatelet drug in the thienopyridine family.
S1512 Tadalafil Tadalafil is a PDE-5 inhibitor with IC50 of 1.8 nM in a cell-free assay. Tadalafil is at least 9000 times more selective for PDE5 than most of the other families of PDEs, with the exception of PDE11. It can partial inhibits PDE11
β-Catenin levels in 293T cells treated with PDE5 inhibitor in the presence or absence of Wnt3a. (a) Tadalafil reduced β-catenin protein levels. Immunofluorescence and confocal images of 293T cells treated with dimethyl sulfoxide (DMSO) or tadalafil at 10 uM in the presence or absence of recombinant Wnt3a for 24 h.
S7297 Osimertinib (AZD9291) Osimertinib (AZD9291) is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR in LoVo cells, respectively. Phase 3.
Western blot analysis for total (t-) and phosphorylated (p-) EGFR, AKT, ERK1/2, and β actin in H1975 parental and resistant (COR#3, AZDR#1) cells.
S8762 dBET6 dBET6 is a highly cell-permeable degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding.
S0015 New WNK-IN-11 WNK-IN-11 is an allosteric With-No-Lysine (WNK) kinase inhibitor with IC50 of 4 nM for WNK1.
S1290 Celastrol Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
SK-BR-3, A549, HCT-116 and BT-474 cells were incubated with or without X66 for 1 h before exposed to GM, celastrol or MG132 for 8 h. Cell lysates were analyzed by Western blot with indicated antibodies.
S3116 Sulfathiazole Sulfathiazole is an organosulfur compound that has been used as a short-acting sulfa drug.
S4011 Ampiroxicam Ampiroxicam is a nonselective cyclooxygenase inhibitor uesd as anti-inflammatory drug.
S3617 (20S)-Protopanaxatriol (20S)-Protopanaxatriol(g-PPT), a neuroprotective metabolite of ginsenoside, protopanaxatriol (g-PPT), is a functional ligand for both GR and ERbeta and could modulate endothelial cell functions through the glucocorticoid receptor (GR) and oestrogen receptor (ER).
S8650 BTSA1 BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.
S5035 6-Aminopenicillanic acid 6-Aminopenicillanic acid (6-APA) is the central component of penicillin β-lactam antibiotics which are generated by Penicillium. It is used as precursor for antibiotic compounds ampicillin and amoxicillin.
S5574 Benzoic aldehyde Benzaldehyde is an organic compound that is frequently used in industry for chemical synthesis.
S8609 Derazantinib(ARQ-087) Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.
S8643 New AZD5991 AZD5991 is a macrocyclic MCL-1 inhibitor with sub-nanomolar affinity for MCL-1 (Ki = 0.13 nM). The binding affinity of AZD5991 is about 25-fold lower for mouse Mcl-1 vs. human Mcl-1 but only four-fold lower for rat Mcl-1.
S0017 New Lu-135252 Darusentan is a selective endothelin A (ETA) receptor antagonist. Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics with Ki of 13 nM.
S0723 New BRL 15572 BRL 15572 is selective antagonist of 5-HT1D with around 60× selectivity over other related receptors. BRL 15572 is a useful tool for the differentiation between human 5-HT1B and 5-HT1D receptors in functional studies.
S1017 Cediranib (AZD2171) Cediranib (AZD2171) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Phase 3.
Western blots of EZH2 expression in A549, HCC461, and HCC4006 cells upon treatment with different doses of VEGFR-2-inhibitor AZD2171 (0, 5 and 10 nM). AZD2171 decreased the expression of EZH2 in HCC4006 and HCC461 cells expressing VEGFR-2 in a dose-dependent manner but did not do so in A549 cells lacking expression of VEGFR-2.
S2746 AZ 628 AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM in cell-free assays, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc.
Enzymatic activity of RIP3 from Abcam, the concentration-effect relationship of RIP3 inhibition by the tested protein kinase inhibitors and the mode of action of RIP3 inhibition by dabrafenib. The RIP3 inhibition rates of AZ628 at different concentrations were measured by the luminescent RIP3 assay. The data (mean ?SD from 3 independent experiments) were presented as the Lineweaver-Burk plots using Graphpad Prism 5.
S1216 PFI-1 (PF-6405761) PFI-1 is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.
S7667 SU5402 SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
Four FGFR inhibitors, namely PD-173074 (PD-74), PD-166866 (PD-66), SU5402 (SU54) and NVP-BGJ398 (BG-98), inhibit A673, SKNMC, POE, RDES and SKES Ewing cell growth in vitro in a dose-dependent manner, whereas normal cells (IMR90 fibroblasts) remained unaffected. PD-74 proved to be most effective in four out of five Ewing sarcoma cell lines tested. Cells were grown in 10% FBS conditions and cell proliferation was measured after 72 h using a Resazurin assay.
S4851 Tafluprost Tafluprost is a novel prostaglandin analog with a high affinity for the fluoroprostaglandin (FP) receptor PGF2α. A prostanoid selective FP receptor agonist.
S5088 Labetalone hydrochloride Labetalone hydrochloride is hydrochloride form of labetalone, a blocker of both alpha- and beta-adrenergic receptors that is used as an antihypertensive.
S8721 PDGFR inhibitor 1 PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of KIT and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth.
S5357 Safinamide Safinamide is an orally active, selective, reversible monoamine oxidase-B inhibitor with both dopaminergic and non-dopaminergic (glutamatergic) properties. The IC50 value of safinamide for MAO-B is 98 nM.
S5848 Frovatriptan Succinate Frovatriptan Succinate is the succinate salt form of frovatriptan, a synthetic triptan with serotonin (5-HT) receptor agonist activity especially for the 5-HT1B/1D receptors.
S6262 Ammonium formate Ammonium Formate is the ammonium salt of formic acid. It is widely used in various organic reactions.
S6643 New R-7050 R-7050 is a cell permeable TNF-α receptor antagonist and is 2.3-fold more selective for TNF-α-mediated signaling than for that driven by IL-1β.
S0267 New TRi-1 TRi-1 is a potent, specific and irreversible cytosolic thioredoxin reductase 1 (TXNRD1) inhibitor with IC50 of 12 nM. TRi-1 has little mitochondrial toxicity for anticancer therapy.
S0724 New CZC-25146 hydrochloride CZC-25146 hydrochloride is a potent, selective and metabolically stable LRRK2 inhibitor with IC50 of 4.76 nM and 6.87 nM for wild type LRRK2 and G2019S LRRK2, respectively.
S7688 New Ki20227 Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively.
S2769 Dovitinib (TKI-258) Dilactic Acid Dovitinib Dilactic acid (TKI258 Dilactic acid) is the Dilactic acid of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
In vitro assays on CUX1-FGFR1-expressing Ba/F3 cells. a. IL-3 deprivation of Ba/F3 cells transduced with CUX1-FGFR1 resulted in transformation to growth factor independent growth. The mean growth ±SEM of three separate measurements over four consecutive days is presented. b. The dose-response curves of CUX1-FGFR1-transduced Ba/F3 cells, treated with TKI258 and PKC412 for 48 hours in the absence or presence of IL-3 (2 ng/ml) are presented. Points represent the average results of two experiments done in triplicate plotted with the curve-fitting GraphPad Prism 5 software; bars, SD. The calculated IC50 for each inhibitor is indicated. c. Western blot analyses of CUX1-FGFR1-transformed Ba/F3 cells after treatment with PKC412 and TKI258. Phosphorylation of CUX1-FGFR1 and its downstream effectors STAT5 and RPS6K decreased with increasing inhibitor concentrations. Expression of total CUX1-FGFR1, STAT5 and RPS6K remained unaffected. d. Effect of PKC412 and TKI258 on apoptosis of CUX1-FGFR1-expressing Ba/F3 cells after treatment for 48 hours. The percentage of apoptotic plus necrotic CUX1-FGFR1-transduced Ba/F3 cells is indicated.
S2747 AMG-458 AMG 458 is a potent c-Met inhibitor with Ki of 1.2 nM, ~350-fold selectivity for c-Met than VEGFR2 in cells.
S4298 Amifostine Amifostine is the first approved radioprotective drug, used to decrease the risk of kidney problems caused by treatment with cisplatin.
S7765 Dovitinib (TKI258) Lactate Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
(c) Percent survival for the AGS cancer cell line is shown with FGFR2 inhibitors of varying specificity. (d) The KatoIII diffuse gastric cancer cell line was treated with FGFR2 inhibitors of varying specificity. The Y-axis depicts percent survival versus the X-axis with log concentrations. In all panels, error bars represent standard error of the mean. The difference in percent cell survival between KatoIII and AGS cells was statistically significant (P <0.05) at the three highest concentrations of all drugs, except Brivanib which was only significant at the highest concentration.
S5006 Teprenone Teprenone, an acylic polyisoprenoid, that is known as tetraprenylacetone or geranylgeranylacetone, is an anti-ulcer drug, clinically used for gastritis. Teprenone(Geranylgeranylacetone) is an inducer of heat shock proteins (HSPs) expression.
S9452 10-Undecenoic acid 10-Undecenoic acid, a natural or synthetic fungistatic fatty acid, is used for the preparation of active pharmaceutical ingredients, cosmetics, perfumes, antidandruff shampoos and antimicrobial powders.
S0511 New Ca2+ channel agonist 1 Ca2+ channel agonist 1 is an agonist of N-type Ca2+ channel and an inhibitor of Cdk2 with EC50 of 14.23 μM and 3.34 μM, respectively, Ca2+ channel agonist 1 is used as a potential treatment for motor nerve terminal dysfunction.
S1019 Canertinib (CI-1033) Canertinib (CI-1033) is a pan-ErbB inhibitor for EGFR and ErbB2 with IC50 of 1.5 nM and 9.0 nM, no activity to PDGFR, FGFR, InsR, PKC, or CDK1/2/4. Phase 3.
(B–C) LNCaP (B) and LNCaP-AI (C) cells were transiently transfected with sPLA2-IIa(-800)-Luc (0.5 lg). The cells were then treated with Erlotinib (20 lM), Gefitinib (20 lM), Lapatinib (20 lM), CI-1033 (8 lM), LY294002 (20 lM) and Bortezomib (20 lM) without or with EGF (100 ng/ml) for 24 h. Luciferase assay was performed according to a standard protocol with Renilla luciferase as an internal control. Data are presented as the mean (±SD) of duplicate values of a representative experiment that was independently repeated for five times.
S1293 Cilnidipine Cilnidipine is a unique L-type and N-type calcium channel blocker, used for high blood pressure treatment.
S2163 PF-4708671 PF-4708671 is a cell-permeable inhibitor of p70 ribosomal S6 kinase (S6K1 isoform) with Ki/IC50 of 20 nM/160 nM in cell-free assays, 400-fold greater selectivity for S6K1 than S6K2, and 4- and >20-fold selectivity for S6K1 than MSK1 and RSK1/2, respectively. PF-4708671 induces autophagy. First S6K1-specific inhibitor to be reported.
After treated with PF-4708671 (PF, 10 uM) and 4EGI-1 (50 uM) for 48 h, GRP78 and ATF4 in QBC939, RBE and HCCC-9810 cells were analyzed using western blot.
S7323 CHF 5074 CHF5074 is a gamma-secretase modulator that reduces Aβ42 and Aβ40 secretion. The IC50s of CHF5074 for inhibition of COX-1 and COX-2 is above 100 μmol/L.
S5037 Phenazine methosulfate Phenazine methosulfate is widely used as an intermediate electron carrier for coupling the production of NADH or NADPH to the reduction of tetrazolium salts to coloured formazans.
S5326 Dolasetron Dolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. It has minimal activity at other known serotonin receptors, and has low affinity for dopamine receptors.
S8839 New Borussertib Borussertib is a covalent-allosteric inhibitor of protein kinase Akt with an IC50 of 0.8 nM and a Ki of 2.2 nM for WT Akt.
S0269 New GSK467 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.
S1020 PD184352 (CI-1040) PD184352 (CI-1040) is an ATP non-competitive MEK1/2 inhibitor with IC50 of 17 nM in cell-based assays, 100-fold more selective for MEK1/2 than MEK5. Phase 2.
Melanoma cell viability and in vivo growth by cyclindependent kinase 2/4 inhibition. Western blot analysis for c-Jun, phosphorylated-ERK1/2 (Thr202/Tyr204) (p-ERK1/2), and total ERK1/2 protein levels was done for human melanoma cell lines treated with the BRAFV600E inhibitor GDC-0879 (1 μM), or MEK inhibitors CI-1040 (1 μM), U0126 (1 μM), and PD98059 (10 μM) for 18 hours.
S7076 T0901317 T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively.
(C) Cells were pretreated with DMSO or T0901317 (5 μM), then incubated with 100 mg/L ox-LDL for 6 h.
S7304 CPI-203 CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
S7764 New WST-8 WST-8 is a water-soluble tetrazolium salt used for assessing cell metabolic activity that produces corresponding formazan dye that absorbs at 460 nm. WST-8 is typically used as a cell viability indicator in cell proliferation assays.
S5272 Toceranib phosphate Toceranib phosphate, the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively.
S5264 L-5-Methyltetrahydrofolate calcium Calcium L-5-methyltetrahydrofolate (L-5-MTHF-Ca) is a synthetic derivative of folic acid, the predominant, naturally occurring form of folate.
S6269 Leucomalachite green Leucomalachite green is a chief metabolite of malachite green, a triphenylmethane dye. It is one of the most commonly used reagents for presumptive blood test and gives a characteristic green color in the presence of blood.
S6648 New PF-06282999 PF-06282999 is an orally bioavailable, irreversible inactivator of myeloperoxidase enzyme and is currently in clinical trials for the potential treatment of cardiovascular diseases.
Catalog No. Product Name Information Product Use Citations Product Validations S3608 Demethylzeylasteral (T-96) Demethylzeylasteral (T-96), the active component isolated from Tripterygium wilfordii Hook F., inhibits UDP-glucuronosyltransferase (UGT) isoforms UGT1A6 and UGT2B7 with immunosuppressive effects.
S3940 3'-Hydroxypterostilbene 3'-Hydroxypterostilbene (3'-HPT) is one of the active constituents of Sphaerophysa salsula and Pterocarpus marsupium which may be useful in treating different types of haematological malignancies. 3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.
S3622 Diammonium Glycyrrhizinate Diammonium glycyrrhizinate (DG), a traditional Chinese medicine (TCM), is extracted and purified from liquorices (Radix glycyrrhizae). It is known for its anti-inflammatory effects, resistance to biologic oxidation and membranous protection. DG is able to reduce inflammatory injury via suppression of NF‑κB, TNF‑α and intercellular adhesion molecule 1.
S3941 Pinocembrin Pinocembrin is a major flavonoid molecule incorporated as multifunctional in the pharmaceutical industry. Its vast range of pharmacological activities has been well researched including antimicrobial, anti-inflammatory, antioxidant, and anticancer activities.
S9190 Oroxin B Oroxin B, one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels is found to be downregulated, while PTEN was upregulated after Oroxin B treatment.
S3994 Methyl Cholate Methyl Cholate is methyl ester form of Cholic acid that is a primary bile acid mainly produced by the liver.
S3981 Sinapinic Acid Sinapinic acid, or sinapic acid is a small naturally occurring hydroxycinnamic acid which belongs to phenylpropanoid family and commonly used as matrix in MALDI mass spectrometry. Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM, and also inhibits ACE-I activity.
S3983 Caryophyllene oxide Caryophyllene oxide, an oxygenated terpenoid existed in many plant essential oil, is well known as preservative in food, drugs and cosmetics with anti-inflammatory, anti-carcinogenic and skin penetration enhancing properties.
S3996 Thioctic acid Thioctic acid (DL-α-Lipoic acid) is a cyclic disulfide antioxidant that interconverts with its reduced dithiol form.
S3998 (+)-α-Lipoic acid R(+)-α-lipoic acid, a physiological form of thioctic acid, is a strong antioxidant that relieves diabetic neuropathic symptoms. It shows superior antioxidative effects to its racemate. α-Lipoic Acid is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation.
S5455 Akebia saponin D Akebia saponin D, the most abundant constituent of the rhizome of Dipsacus asper, has been used for the treatment of lower back pain, traumatic hematoma and bone fractures.
S9203 Notopterol Notopterol is a kind of furanocoumarin that possesses anti-inflammatory, analgesic, and anticancer activities.
S3614 Lupeol Lupeol is a significant lupane-type triterpene represented in the plant, fungi and animal kingdoms with anticancer, antiprotozoal, chemopreventive and anti-inflammatory properties.
S5172 1-Triacontanol 1-Triacontanol is a fatty alcohol found in plant cuticle waxes and in beeswax. It is a growth stimulant for many plants, most notably roses.
S9208 Ginsenoside Rb3 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).
S9385 Ligustilide Ligustilide is the most abundant bioactive ingredient in Rhizoma Chuanxiong, a Chinese medicinal herb commonly used for the treatment of cardiovascular ailments.
Catalog No. Product Name Information K1020 PI3K/Akt/mTOR Pathway Inhibitor Kit Cav 2.2 blocker 1 (compound 9) is a N-type calcium channel (Cav 2.2) blocker for the treatment of pain with IC50 of 1 nM.
Catalog No. Product Name Information L3800 FDA-approved & Passed Phase I Drug Library A unique collection of 3003 drugs that are marketed around the world or have passed clinical phase 1 and can be used for high throughput screening (HTS) and high content screening (HCS).
L3900 Preclinical/Clinical Compound Library A unique collection of 2827 preclinical and clinical compounds for high throughput screening (HTS) and high content screening (HCS).
L1700-Ⅱ Bioactive Compound Library-Ⅱ A unique collection of 5309 bioactive compounds for high throughput screening (HTS) and high content screening (HCS).
L4000 Neuronal Signaling Compound Library A unique collection of 1095 small molecule compounds with biological activity used for neurologic research and associated assays
L4500 Human Endogenous Metabolite Compound Library 541 small collections of human endogenous metabolites, involving multiple metabolic pathways, which can be used for high-throughput screening, opening up new ways for humans to treat various diseases such as tumors.
L2700 Ion Channel Ligand Library A unique collection of 232 small molecule modulators used for Ion channel research.
L4100 Immunology/Inflammation Compound Library A unique collection of 1838 small molecules with biological activity used for Immunology/Inflammation research and associated assays.
L2800 PI3K/Akt Inhibitor Library A unique collection of 262 small molecule inhibitors used for PI3K/Akt/mTOR pathway research.
L2500 Protease Inhibitor Library A unique collection of 227 small molecule inhibitors used for chemical genomics, high-throughput screening (HTS), and high content screening (HCS).
L7900 Alkaloid Compound Library A unique collection of 269 alkaloid compounds used for high throughput screening(HTS) and high content screening(HCS).