TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM. 了解更多
Yool Lee, .et al. Time-of-day specificity of anticancer drugs may be mediated by circadian regulation of the cell cycle, Sci Adv, 2021, 7
Naoki Shiraishi, .et al. Heat shock protein 90 as a molecular target for therapy in oral squamous cell carcinoma: Inhibitory effects of 17?DMAG and ganetespib on tumor cells, Oncol Rep, 2020, 448-458 PMID: 33416122
Sisunatovir, also known as RV521, is a highly potent fusion inhibitor with efficacy against a panel of clinical isolates of RSV-A and RSV-B viruses. 了解更多
Caroverine hydrochloride is a potent, competitive and reversible antagonist of NMDA and AMPA glutamate receptor. Caroverine hydrochloride is also an antioxidant and calcium-blocking agent that exhibits vasorelaxant action. Caroverine hydrochloride can be used for the research of inner ear tinnitus. 了解更多
ML-095 is an inhibitor of PLAP (IC50 = 3.7 μM) that demonstrates high selectivity against the related alkaline phosphatases, TNAP and IAP (IC50s > 100 μM). 了解更多
SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity. 了解更多
Glucagon is a peptide hormone, produced by alpha cells of the pancreas. It works to raise the concentration of glucose in the bloodstream. Its effect is opposite that of insulin, which lowers the glucose. 了解更多
Wei Y, .et al. SUMO-Targeted DNA Translocase Rrp2 Protects the Genome from Top2-Induced DNA Damage, Mol Cell, 2017, Jun 1;66(5):581-596.e6 PMID: 28552615
Mohácsik P, .et al. A Transgenic Mouse Model for Detection of Tissue-Specific Thyroid Hormone Action, Endocrinology, 2018, Feb 1;159(2):1159-1171 PMID: 29253128
Pencheva N, .et al. Broad-spectrum therapeutic suppression of metastatic melanoma through nuclear hormone receptor activation., Cell., 2014, 156(5):986-1001 PMID: 24581497
Bin Dong, .et al. High-fructose diet downregulates long-chain acyl-CoA synthetase 3 expression in liver of hamsters via impairing LXR/RXR signaling pathway, J Lipid Res., 2013, May; 54(5): 1241-1254. PMID: 23427282
Hiroki Ozawa, .et al. Targeting AURKA in treatment of peritoneal tumor dissemination in gastrointestinal cancer, Transl Oncol, 2022, Feb;16:101307 PMID: 34902741
Cong Li, .et al. AMG 925 is a dual FLT3/CDK4 inhibitor with the potential to overcome FLT3 inhibitor resistance in acute myeloid leukemia., Mol Cancer Ther., 2015, Feb;14(2):375-83. PMID: 25487917
Pirita Pekkonen, .et al. KSHV viral cyclin interferes with T-cell development and induces lymphoma through Cdk6 and Notch activation in vivo, Cell Cycle, 2014, Dec 1; 13(23): 3670-3684 PMID: 25483078
Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay. 了解更多
UK-371804 is a potent and selective urokinase-type plasmogen activator (uPA) inhibitor with excellent enzyme potency (Ki=10 nM) and selectivity profile (4000-fold versus tPA and 2700-fold versus plasmin). 了解更多
AVN-101 is a very potent 5-HT7 receptor antagonist, with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors. It is a milti-target drug candidate for the treatment of CNS disorders. 了解更多
MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively).
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Acecainide, also known as N-acetylprocainamide and ASL 601, is the N-acetylated metabolite of procainamide. Acecainide is a Class III antiarrhythmic agent. It can be given either intravenously or orally, and is eliminated primarily by renal excretion. 了解更多
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