inhibitor of mcl1

MIM1 (Inhibitor of Mcl-1) 是一种骨髓细胞因子 1 抑制剂。

S63845 是一种选择性骨髓细胞白血病 1（MCL1) 抑制剂，结合人 MCL1的 Kd 值为 0.19 nM。

AZD-5991 Racemate是 AZD-5991 的外消旋体。(Rac)-AZD-5991是一种新型的Mcl-1 抑制剂，FRET 实验中IC50 <3 nM，在AML细胞系中诱导BCL2,BCL-XL, CMYC和MCL1的上调。

Mcl1-IN-11 (Compound G) is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.06 and 4.2 μM, respectively.

Mcl1-IN-12 has anti-tumor activity.It is a selective Mcl-1 inhibitor, less potent at Bcl-2, with Kis of 0.29 and 3.1 μM, respectively.

Mcl1-IN-4 is an inhibitor of Mcl1 ( IC50:0.2 μM).

Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.

Tapotoclax (AMG-176) 是一种具有口服活性 MCL1 抑制剂，可用于研究髓系细胞白血病。

Mcl1-IN-3 is an Mcl1 inhibitor. It has an IC50 and Ki of 0.67 and 0.13 μM, respectively.

CLZ-8 (Mcl1-IN-8) 是具有口服活性的 Mcl-1-PUMA （p53 上调细胞凋亡介质）抑制剂，具有辐射防护能力。CLZ-8 可改善辐射诱导的 HUVEC 细胞损伤并减少细胞凋亡计数，抑制辐射诱导的过表达 PUMA。

AZ5576 racemate is a racemic mixture of AZ5576 isomers. AZ5576 is a potent, highly selective, and orally bioavailable inhibitor of Cdk9 that inhibits Cdk9 enzyme activity with an IC50 <5nM and decreases phosphorlyation of Ser2-RNAPII in cells with an IC50 of 96nM. In the MLL-fusion containing acute myeloid leukemia (AML) line, MV411, short-term treatment with AZ5576 led to a rapid dose-dependent decrease in pSer2-RNAPII with concomitant loss of Mcl1 mRNA and protein, resulting in the cleavage and activation of caspase 3 and loss of cell viability.

BRD-810 作为一种MCL1高选择性抑制剂，通过与 MCL1 的 BH3 沟结合，有效阻断促凋亡蛋白的隔离，进而在 MCL1 依赖性细胞系中迅速诱导半胱天冬酶(caspase)激活。在血液肿瘤和实体瘤模型中，BRD-810 展现出显著的抗肿瘤活性。

TC11 (1H-Isoindole-1,3(2H)-dione, 5-amino-2-[2,6-bis(1-methylethyl)phenyl]-TC11) 是一种有效的肿瘤细胞增殖抑制剂，并通过激活 caspase-3、8 和 9 诱导细胞凋亡。在长时间有丝分裂阻滞期间，它诱导 MCL1降解导致凋亡。它作为苯酞酰亚胺衍生物在结构上与免疫调节药物相关。