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CAS NO. |
Products Name |
1338545-07-5 |
OTS964 |
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OTS964 is a potent TOPK inhibitor with an IC50 value of 28 nM. IC50 value: 28 nM Target: TOPK in vitro: OTS964 is a dimethylated derivative of OTS514. OTS964 can inhibit TOPK kinase activity with high affinity and selectivity. TOPK (T-lymphokine-activated killer cell-originated protein kinase) is a protein that is found in a wide range of human cancers and is believed to work as an oncogene, promoting tumor growth. OTS964 inhibits the growth of TOPK-positive cells with low IC50 values [A549 (31 nM), LU-99 (7.6 nM), DU4475 (53 nM), MDA-MB-231 (73 nM), T47D (72 nM), Daudi (25 nM), UM-UC-3 (32 nM), HCT-116(33nM), MKN1(38nM), MKN45(39nM), HepG2(19nM), MIAPaca-2 (30 nM), and 22Rv1 (50 nM)]. [1] in vivo: OTS964 is a potent and selective TOPK inhibitor with potential anticancer activity. OTS964 inhibits TOPK kinase activity with high affinity and selectivity. Similar to the knockdown effect of TOPK small interfering RNAs (siRNAs), OTS964 causes a cytokinesis defect and the subsequent apoptosis of cancer cells in xenograft models of human lung cancer |
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1821908-48-8 |
SGC2085 |
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SGC2085 is a potent and selective coactivator associated arginine methyltransferase 1 (CARM1) inhibitor with an IC50 of 50 nM. |
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1437321-24-8 |
CEP-40783 |
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CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively. |
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1356962-34-9 |
HG-14-10-04 |
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HG-14-10-04 is a potent and specific ALK inhibitor with IC50 of 20 nM. IC50 value: 20 nM Target: ALK More information can be found in the following Patent, Example 10 Preparation of substituted pyrimidinamines as ALK kinase inhibitors By Aquila, Brian; Kamhi, Victor; Peng, Bo; Pontz, Timothy; Saeh, Jamal Carlos; Thakur, Kumar; Yang, Bin From U.S. Pat. Appl. Publ. (2012), US 20120028924 A1 20120202 |
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1356962-20-3 |
AZD3463 |
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AZD-3463 is an ALK/IGF1R inhibitor which overcomes multiple mechanisms of acquired resistance to crizotinib. IC50 Value: Target: ALK/IGF1R |
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1450824-22-2 |
TD139 |
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TD139 is a novel high-affinity inhibitor of the galectin-3 carbohydrate binding domain with a Kd of 14 nM |
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1177827-73-4 |
AP-III-a4 |
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ENOblock(AP-III-a4) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo. IC50 value: 0.576 uM [1] Target: enolase Enolase is a component of the glycolysis pathway and a “moonlighting” protein, with important roles in diverse cellular processes that are not related to its function in glycolysis. However, small molecule tools to probe enolase function have been restricted to crystallography or enzymology. In this study, we report the discovery of the small molecule “ENOblock”, which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity. ENOblock was isolated by small molecule screening in a cancer cell assay to detect cytotoxic agents that function in hypoxic conditions, which has previously been shown to induce drug resistance. Further analysis revealed that ENOblock can inhibit cancer cell metastasis in vivo. Moreover, an unexpected role for enolase in glucose homeostasis was revealed by in vivo analysis. Thus, ENOblock is the first reported enolase inhibitor that is suitable for biological assays. This new chemical tool may also be suitable for further study as a cancer and diabetes drug candidate. A Unique Small Molecule Inhibitor of Enolase Clarifies Its Role in Fundamental Biological Processes By Jung, Da-Woon; Kim, Woong-Hee; Park, Si-Hwan; Lee, Jinho; Kim, Jinmi; Su, Dongdong; Ha, Hyung-Ho; Chang, Young-Tae; Williams, Darren R. From ACS Chemical Biology (2013), 8(6), 1271-1282 |
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1162656-22-5 |
MCB-613 |
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MCB-613 is a potent, pan steroid receptor coactivator (SRC) stimulator. Target: SRC in vitro: MCB-613 exerts the greatest activation of SRC-1 in the primary screen, is confirmed to be a strong activator of all three SRCs. MCB-613 can super-stimulate SRCs' transcriptional activity. MCB-613 increases SRCs' interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). MCB-613 selectively and reversibly binds to the RID of SRC-3, and selectively kills cancer cells including MCF-7 (breast), PC-3 (prostate), H1299 (lung), and HepG2 (liver) cells, without toxicity to mouse primary hepatocytes and mouse embryonic fibroblasts (MEFs). MCB-613 also increases SRCs' interactions with other coactivators and markedly induces ER stress coupled to the generation of reactive oxygen species (ROS). [1] in vivo: In an MCF-7 breast cancer mouse xenograft model, MCB-613 (20 mg/kg, i.p.) significantly and dramatically inhibits the growth of the tumor while causing no obvious animal toxicity and body weight less. [1] |
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1489389-18-5 |
CCT245737 |
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CCT245737 is a potent, ATP-competitive CHK1 inhibitor with an IC50 of 30-220 nM. target:CHK1; IC 50: 30-220nM; In vitro: CCT245737 shows <50% inhibition at 10 μM for 85/121 kinases, representing a selectivity for CHK1 inhibition of >5000-fold over these enzymes. [1] CCT245737 enhanced gemcitabine antitumor activity to a greater degree than for higher doses of either agent alone, without increasing toxicity. [2] In vivo: CCT2457374 shows an increase in plasma and tumoconcentrations between 3-100 mg/kg po. [1 |
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1174428-47-7 |
SF2523 |
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SF2523 is a highly selective and potent inhibitor of PI3Kα and BRD4 with IC50 values of 16 and 241 nM for PI3Kα and BD1, respectively |
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