Chemical Structure : MI-238
货号: PC-49852Not For Human Use, Lab Use Only.
MI-238 (MI 238) is a potent and specific Mcl-1 inhibitor with Ki of 0.45 uM to human Mcl-1 protein in FP assays, disrupts the association of Mcl-1 with BH3-only proteins.
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MI-238 (MI 238) is a potent and specific Mcl-1 inhibitor with Ki of 0.45 uM to human Mcl-1 protein in FP assays, disrupts the association of Mcl-1 with BH3-only proteins.
MI-238 is docked into Mcl-1 BH3 binding groove and proximal to the BH1 domain of Mcl-1.
MI-238 disrupts Bak/Mcl-1 interaction in a dose-dependent manner in vitro, directly binds to Mcl-1 and inhibits Mcl-1 anti-apoptotic function.
MI-238 treatment (20 uM) induced apoptosis in 50.1 ± 1.1% of parental H1299 cells, but not Mcl-1 deficient H1299 cells, caused caspase 3 cleavage, effectively induced apoptosis in AML cells.
MI-238 synergized with venetoclax to induce apoptosis in AML cells, and the combination of MI-238 and venetoclax potently inhibited the development of AML in murine model.
分子量 | 497.93 | |
分子式 | C29H20ClNO5 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Tianming Zhao, et al. Mol Med. 2023 Jan 19;29(1):10.
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