| CAS NO. |
Products Name |
| 30827-99-7 |
AEBSF HCL |
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| AEBSF is a water soluble, irreversible serine protease inhibitor; inhibits proteases like chymotrypsin, kallikrein, plasmin, thrombin, and trypsin. |
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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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| 947620-48-6 |
E6005 |
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| RVT-501 (E6005) is a selective phosphodiesterase 4 (PDE4PDE4) inhibitor with an IC50 of 2.8 nM. |
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| 1190221-43-2 |
TM5441 |
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| TM5441 is a plasminogen activator inhibitor-1 (PAI-1); inhibits several tumor cell lines with IC50 values between 9.7 and 60.3 μM. |
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| 1361224-53-4 |
AMG-3969 |
more... |
| AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM. |
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| 1361224-53-4 |
AMG-3969 |
more... |
| AMG-3969 is a potent glucokinase-glucokinase regulatory protein interaction (GK-GKRP) disruptor with an IC50 of 4 nM. |
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| 357263-13-9 |
BMS378806 |
more... |
| BMS-378806 is a potent HIV-1 attachment inhibitor that interferes with CD4-gp120 interactions. BMS-378806 selectively inhibits the binding of HIV-1 gp120 to the CD4 receptor with EC50 of 0.85-26.5 nM in virus. |
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| 928134-65-0 |
LCI699 |
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| Osilodrostat (LCI699) is a potent inhibitor of human 11β-hydroxylase and aldosterone synthase with IC50 values of 2.5 and 0.7 nM, respectively. |
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| 1000025-07-9 |
Vadadustat |
more... |
| Vadadustat is a novel, titratable, oral hypoxia-inducible factor prolyl hydroxylase (HIF-PH) inhibitor in development for the treatment of anemia. |
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| 300657-03-8 |
BMS309403 |
more... |
| BMS-309403 is a potent, selective and cell-permeable inhibitor of fatty acid binding protein 4 (FABP4) with a Ki of less than 2 nM. |
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