product results for Drug Repurposing for Anticancer Indications

Searches related to Drug Repurposing for Anticancer Indications :

Catalog No. Product Name Information Product Use Citations Product Validations
S1267 Vemurafenib (PLX4032, RG7204) 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.
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.
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.
S6233 New 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.
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.
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.
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 New Hydrocortisone acetate Hydrocortisone Acetate is the synthetic acetate salt form of hydrocortisone, a corticosteroid with anti-inflammatory and immunosuppressive properties.
S5739 New Nebivolol Nebivolol is a β1 receptor blocker with nitric oxide-potentiating vasodilatory effect used in treatment of hypertension and also for left ventricular failure.
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.
S2459 Clozapine Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.
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).
S4567 Eprodisate disodium Eprodisate Disodium is the orally available disodium salt form of Eprodisate, a small-molecule, orally bioavailable, inhibitor of AA-amyloid fibrillogenesis.
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 New Cefminox Sodium Cefminox Sodium is the sodium salt form of cefminox, a semi-synthetic, second-generation, beta-lactamase-stable cephalosporin with antibacterial activity.
S9363 New Coumarin 151 Coumarin 151 is a fluorescent tracer used for the detection of proteinases.
S5741 New Quetiapine Quetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.
S6235 New 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.
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.
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.
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.
S5223 Phenylpiracetam Phenylpiracetam is a central nervous system stimulant and nootropic agent belonging to the racetam family of drugs.
S5361 New Bendazac Bendazac is a non-steroidal anti-inflammatory drug that delays the cataractogenic process. It may act by preventing protein denaturation.
S5269 J147 J147, a curcumin derivative, is a potent neurogenic and neuroprotective compound developed for the treatment of neurodegenerative conditions associated with aging.
S5753 New Setipiprant(ACT-129968, KYTH-105) 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 New 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.
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.
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.
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 New 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.
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.
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.
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 New 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.
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.
S5620 New 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.
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.
S5306 Forchlorfenuron (KT-30, 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.
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.
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 New 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 New 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 New 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 New Terephthalic acid Terephthalic acid, a raw material for polyethylene terephthalate (PET) production, is one of the most important chemicals in petrochemical industry.
S1009 Dactolisib (BEZ235, NVP-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.
S4920 b-AP15 b-AP15 is a deubiquitinases inhibitor for 19S proteasomes activity of Ub-AMC cleavage with IC50 of 2.1 μM.
S5328 New 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 New Lodoxamide Tromethamine Lodoxamide Tromethamine is the tromethamide salt form of lodoxamide, a synthetic mast cell stabilizing compound with anti-inflammatory activity.
S5872 New 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 New 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
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.
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.
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.
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.
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 New 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 New 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.
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.
S8125 Pamapimod (R-1503, Ro4402257) 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 New Fingolimod Fingolimod is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
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.
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.
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 New Lazertinib (YH25448,GNS-1480) 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 New 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.
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
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.
S4579 Resorcinol Resorcinol is a chemical compound that serves as an antiseptic,an disinfectant, and a chemical intermediate for the production of many other pharmaceuticals.
S8762 New dBET6 dBET6 is a highly cell-permeable degrader of BET bromodomains with an IC50 of 14 nM for BRD4 binding.
S1290 Celastrol Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
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 New Benzoic aldehyde Benzaldehyde is an organic compound that is frequently used in industry for chemical synthesis.
S8609 New 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.
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.
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.
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.
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 New 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 New 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 New 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 New Ammonium formate Ammonium Formate is the ammonium salt of formic acid. It is widely used in various organic reactions.
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.
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.
S5006 Teprenone Teprenone, an acylic polyisoprenoid, that is known as tetraprenylacetone or geranylgeranylacetone, is an anti-ulcer drug, clinically used for gastritis.
S9452 New 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.
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.
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. First S6K1-specific inhibitor to be reported.
S7323 New 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 New 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.
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.
S7076 T0901317 T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively.
S7304 CPI-203 CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
S3632 Trichloroisocyanuric acid Trichloroisocyanuric acid (TCCA) is a safe and efficient reagent, useful for chlorination and oxidation reactions.
S5272 New 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 New 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 New 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.
S1508 Alprostadil Alprostadil is used as a drug in the treatment of erectile dysfunction and has vasodilatory properties. It is a Prostaglandin Analog and Prostaglandin E1 Agonist.
S2751 Milciclib (PHA-848125) Milciclib (PHA-848125) is a potent, ATP-competitive CDK inhibitor for CDK2 with IC50 of 45 nM. It is >3-fold more selective for CDK2 than CDK1, 2, 4, 5, and 7. Phase 2.
S7540 SB273005 SB273005 is a potent integrin inhibitor with Ki of 1.2 nM and 0.3 nM for αvβ3 receptor and αvβ5 receptor, respectively.
S7687 GSK269962A HCl GSK269962 is a selective ROCK(Rho-associated protein kinase) inhibitor with IC50 values of 1.6 and 4 nM for ROCK1 and ROCK2, respectively.
S7639 3PO 3PO is a small-molecule inhibitor of PFKFB3 with an IC50 of 22.9 μM for recombinant human PFKFB3 protein and does not inhibit PFK-1 activity. It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.
S5265 New TBB TBB (4,5,6,7-tetrabromobenzotriazole) is a selective cell-permeable CK2 inhibitor with IC50 values of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively.
S9212 New Melamine Melamine is a widely-used intermediate, mainly employed as a raw material for producing melamine resin and is a chemical most often found in plastic materials.
S1488 Naratriptan HCl Naratriptan HCl is a triptan agent that is used for the treatment of migraine headaches.
S2752 HER2-Inhibitor-1 HER2-Inhibitor-1 is an analog of ARRY-380. ARRY-380 is a potent and selective HER2 inhibitor with IC50 of 8 nM, equipotent against truncated p95-HER2, 500-fold more selective for HER2 versus EGFR.
S8641 New Nec-1s (7-Cl-O-Nec1) Nec-1s is a stable variant of Necrostatin-1. It is a more specific RIPK1 inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.
S4931 Propiverine hydrochloride Propiverine is an anticholinergic drug used for the treatment of overactive bladder and urinary incontinence.
S5248 New Apatinib Apatinib is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM and 13 nM for VEGFR-2 and Ret, respectively.
S8770 New Lanifibranor(IVA-337) Lanifibranor (IVA-337) is a moderately potent and well balanced pan PPAR agonist with EC50 values of 1537 nM, 866 nM and 206 nM for hPPARα, hPPARδ and hPPARγ, respectively.
S1022 Ridaforolimus (Deforolimus, MK-8669) Ridaforolimus (Deforolimus, MK-8669) is a selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. Phase 3.
S2181 Ixazomib Citrate (MLN9708) Ixazomib Citrate (MLN9708) immediately hydrolyzed to MLN2238, the biologically active form, on exposure to aqueous solutions or plasma. MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Phase 3.
S5130 Taurocholic acid sodium salt hydrate Taurocholic acid, a bile salt formed in the liver, is the product of conjugation of cholic acid with taurine that is involved in the emulsification of lipids. Its sodium salt is the chief ingredient of the bile of carnivorous animals.
S4932 Proxyphylline Proxyphylline is a derivative of theophylline which is used as a bronchodilator and for its cardiovascular properties. It selectively antagonizes A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 µM for platelets).
S5283 TMB-PS TMB-PS is a chromogenic reagent for the detection of hydrogen peroxide e.g. in the enzymatic analysis of body fluids.
S5266 New Stiripentol Stiripentol is a third-generation anti-epileptic drug that enhances GABAergic neurotransmission. It is an inhibitor of cytochrome P450.
S7965 New PLX8394 PLX8394 is a next-generation, orally available, small-molecule BRAF inhibitor with IC50 values of 3.8 nM, 14 nM and 23 nM for BRAF(V600E), WT BRAF and CRAF respectively. It has potential antineoplastic activity.
S1518 Ibuprofen Lysine Ibuprofen Lysine is a non-steroidal anti-inflammatory drug.
S2830 Clindamycin Clindamycin inhibits protein synthesis by acting on the 50S ribosomal, used for the treatment of bacterial infections.
S5765 New Sodium Dehydrocholate Sodium Dehydrocholate is a semisynthetic bile acid made from cholic acid. It has been used for stimulation of biliary lipid secretion.
S2001 Elvitegravir (GS-9137, JTK-303) Elvitegravir (GS-9137, JTK-303) is an HIV integrase inhibitor for HIV-1 IIIB, HIV-2 EHO and HIV-2 ROD with IC50 of 0.7 nM, 2.8 nM and 1.4 nM in cell-free assays, respectively.
S2599 L-Thyroxine L-Thyroxine is a synthetic form of thyroxine and a hormone replacement drug.
S2842 SAR131675 SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.
S7311 Q-VD-Oph Q-VD-Oph is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9.
S7875 NVP-CGM097 NVP-CGM097 is a highly potent and selective MDM2 inhibitor with Ki value of 1.3 nM for hMDM2 in TR-FRET assay. It binds to the p53 binding-site of the Mdm2 protein, disrupting the interaction between both proteins, leading to an activation of the p53 pathway.
S5401 New Tegaserod Maleate Tegaserod Maleate is a hydrogen maleate salt form of tegaserod, which is a 5-HT4 receptor partial agonist and binds with high affinity to 5-HT4 receptors. It has limited affinity for 5-HT1 receptors and no appreciable affinity for other 5-HT receptors, muscarinic, adrenergic, dopaminergic or opiate receptors.
S5239 New Paroxetine mesylate Paroxetine Mesylate is the mesylate salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties.
S6281 New Sodium Thiocyanate Sodium Thiocyanate, one of the main sources of the thiocyanate anion, is used as a precursor for the synthesis of pharmaceuticals and other specialty chemicals.
S1515 Pracinostat (SB939) Pracinostat (SB939) is a potent pan-HDAC inhibitor with IC50 of 40-140 nM with exception for HDAC6. It has no activity against the class III isoenzyme SIRT I. Phase 2.
S2487 Mycophenolic acid Mycophenolic acid is a potent IMPDH inhibitor and the active metabolite of an immunosuppressive drug, used to prevent rejection in organ transplantation.
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.
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.
S3994 Methyl Cholate Methyl Cholate is methyl ester form of Cholic acid that is a primary bile acid mainly produced by the liver.
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.
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.
S5578 Cadaverine Cadaverine is a foul-smelling diamine formed by bacterial decarboxylation of lysine that occurs during protein hydrolysis during putrefaction of animal tissue.
S9385 Ligustilide Ligustilide is the most abundant bioactive ingredient in Rhizoma Chuanxiong, a Chinese medicinal herb commonly used for the treatment of cardiovascular ailments.
S9214 Jujuboside B Jujuboside B, one of the saponins isolated from the seeds of Zizyphus jujuba var. spinosa, is used in traditional chinese medicine for treating cardiovascular diseases and neurodegenerative diseases.
K1020 PI3K/Akt/mTOR Pathway Inhibitor Kit A unique collection of 9 inhibitors for the study of PI3K/Akt/mTOR Pathway Inhibitor Kit.
K1030 EGFR Pathway Inhibitor Kit A unique collection of 15 inhibitors for the study of EGFR Pathway Inhibitor Kit.
K1040 FGFR Pathway Inhibitor Kit A unique collection of 13 inhibitors for the study of FGFR Pathway Inhibitor Kit.
K1050 IGF Pathway Inhibitor Kit A unique collection of 12 inhibitors for the study of IGF Pathway Inhibitor Kit.
K1060 JAK/STAT Pathway Inhibitor Kit A unique collection of 11 inhibitors for the study of JAK/STAT Pathway Inhibitor Kit.
L3800 Drug Repurposing Library A unique collection of 2837 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 and Clinical Compound Library A unique collection of 2582 preclinical and clinical compounds for high throughput screening (HTS) and high content screening (HCS).
L1700-Ⅱ Bioactive Compound Library-Ⅱ (Provided by Pfizer) A unique collection of 7000 bioactive compounds for high throughput screening (HTS) and high content screening (HCS).
L4000 Neuronal Signaling Compound Library A unique collection of 1115 small molecule compounds with biological activity used for neurologic research and associated assays
L4500 Human Endogenous Metabolite Compound Library 400 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 1091 small molecules with biological activity used for Immunology/Inflammation research and associated assays.
L2800 PI3K/Akt Inhibitor Library A unique collection of 174 small molecule inhibitors used for PI3K/Akt/mTOR pathway research.
L2500 Protease Inhibitor Library A unique collection of 229 small molecule inhibitors used for chemical genomics, high-throughput screening (HTS), and high content screening (HCS).
L2900 Anti-diabetic Compound Library A unique collection of 155 small molecules for exploring the development of diabetes.
L3000 Anti-cancer Compound Library A unique collection of 1931 anti-cancer compounds for multiple cancers: Breast Cancer, Leukemia, Lung Cancer, Lymphoma, etc.