BMI-1

抑制剂选择性比较

BMI-1产品

所有产品(5) BMI-1抑制剂(5)

目录号	产品描述	文献引用	实验数据
S7372	PTC-209 PTC-209是一种有效的选择性BMI-1抑制剂，在HEK293T细胞系中IC50为0.5 μM，并导致癌症起始细胞(CICs)的不可逆减少。	Exp Ther Med, 2021, 21(6):619 J Biol Chem, 2020, 10.1074/jbc.RA119.010655 Cell Cycle, 2020, 1-15	Immunoblot analysis of BMI-1 and H2AK119Ub levels following 72 h treatment with 10 µM PTC-209. β-actin and total H2A served as loading controls.
S8820	Unesbulin (PTC596) Unesbulin (PTC596)是第二代BMI-1抑制剂，可加速BMI-1的降解。PTC596 可下调 MCL-1 并诱导p53依赖性的线粒体的凋亡。处理套细胞淋巴瘤细胞72小时，IC50为68-340 nM。
S5315	PRT4165 PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.	Leukemia, 2021, 10.1038/s41375-021-01121-8 Leukemia, 2021, 10.1038/s41375-021-01121-8 Genome Res, 2019, 29(10):1659-1672
S7539	PTC-209 HBr PTC-209 HBr 是PTC-209的氢溴酸盐 , 这是一种强效的选择性的BMI-1抑制剂，其IC50为0.5 μM, 可以不可逆的减少癌起始细胞(CICs)。	Cell Cycle, 2018, 17(10):1199-1211 J Hematol Oncol, 2016, 10.1186/s13045-016-0247-4 Oncotarget, 2016, 7(1):745-58	b Reduced viability 96 h post treatment was observed in all MM cell lines in a dose-dependent manner, but not in BMSCs or PBMCs (c). d Downregulation of CCND1 and MYC as well as upregulation of CDNK1A and CDKN1B was noted 5 h post treatment. e Deregulation of proliferation-associated genes translated into a significant increase of cells in the G1 phase and concurrent decrease in the S and G2M phase of the cell cycle 24 h post treatment. *P < 0.001, P < 0.01 and *P < 0.05 vs DMSO control
S8662	PTC-028 PTC-028是一种具有生物口服活性的化合物，能够通过翻译后修饰减少BMI-1水平。

目录号	产品描述	文献引用	实验数据
S7372	PTC-209 PTC-209是一种有效的选择性BMI-1抑制剂，在HEK293T细胞系中IC50为0.5 μM，并导致癌症起始细胞(CICs)的不可逆减少。	Exp Ther Med,2021, 21(6):619 J Biol Chem,2020, 10.1074/jbc.RA119.010655 Cell Cycle,2020, 1-15	Immunoblot analysis of BMI-1 and H2AK119Ub levels following 72 h treatment with 10 µM PTC-209. β-actin and total H2A served as loading controls.
S8820	Unesbulin (PTC596) Unesbulin (PTC596)是第二代BMI-1抑制剂，可加速BMI-1的降解。PTC596 可下调 MCL-1 并诱导p53依赖性的线粒体的凋亡。处理套细胞淋巴瘤细胞72小时，IC50为68-340 nM。
S5315	PRT4165 PRT4165 is a Bmi1/Ring1A inhibitor with an IC50 of 3.9 µM in the cell-free assay and also inhibits PRC1-mediated H2A ubiquitylation in vivo and in vitro.	Leukemia,2021, 10.1038/s41375-021-01121-8 Leukemia,2021, 10.1038/s41375-021-01121-8 Genome Res,2019, 29(10):1659-1672
S7539	PTC-209 HBr PTC-209 HBr 是PTC-209的氢溴酸盐 , 这是一种强效的选择性的BMI-1抑制剂，其IC50为0.5 μM, 可以不可逆的减少癌起始细胞(CICs)。	Cell Cycle,2018, 17(10):1199-1211 J Hematol Oncol,2016, 10.1186/s13045-016-0247-4 Oncotarget,2016, 7(1):745-58	b Reduced viability 96 h post treatment was observed in all MM cell lines in a dose-dependent manner, but not in BMSCs or PBMCs (c). d Downregulation of CCND1 and MYC as well as upregulation of CDNK1A and CDKN1B was noted 5 h post treatment. e Deregulation of proliferation-associated genes translated into a significant increase of cells in the G1 phase and concurrent decrease in the S and G2M phase of the cell cycle 24 h post treatment. *P < 0.001, P < 0.01 and *P < 0.05 vs DMSO control
S8662	PTC-028 PTC-028是一种具有生物口服活性的化合物，能够通过翻译后修饰减少BMI-1水平。

Tags: BMI-1 inhibitor | BMI-1 modulator | BMI-1 chemical