mcl-1-in-3

Bcl-2 Mcl-1-IN-3 是一种 Bcl-2 Mcl-1 抑制剂，作用于 Mcl-1 (Ki: 0.14 μM) 和 Bcl-2 (Ki: 0.23 μM)，能够用于研究癌症。

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

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。

MCL-1 BCL-2-IN-3 is a selective and potent Mcl-1 and Bcl-2 dual inhibitor with IC50s of 5.95 and 4.78 μM, respectiely.

Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay).

AZD5991是一种针对血液癌症治疗的高效选择性Mcl-1抑制剂。作为经过合理设计的大环形化合物，AZD5991对Mcl-1有亚纳摩尔级的亲和力。该化合物主要抑制诱导性髓系白血病细胞分化蛋白（myeloid cell leukemia-1; Mcl-1; Bcl2-L-3），具有潜在的促凋亡和抗肿瘤活性。使用时，AZD5991与Mcl-1结合，从而阻止Mcl-1与某些促凋亡蛋白的结合及其失活，进而促进过表达Mcl-1的细胞发生凋亡。

3’-Me Meayamycin D 是一种靶向 SF3B1 和 PHF5A 的剪接调节剂，能够影响 pre-mRNA 的剪接，并下调 MCL-1 的表达。在癌细胞 HCT116、SW48、A549、DMS53 和 DMS114 中，它可抑制细胞增殖，GI50 范围为 4.6-7.2 nM。此化合物在小鼠体内具有良好的血浆稳定性，半衰期为 16 小时。

UNBS-1450 is a sodium channel antagonist. UNBS-1450 is a hemi-synthetic cardenolide derived from 2″-oxovorusharin, it is effective against various cancer cell types with an excellent differential toxicity. At low nanomolar concentrations, UNBS-1450 induce

Potent and selective BTK Degrader (IC50 = 5.1 nM); degrades BTK in a proteasome- and CRBN-dependent manner. Suppresses BTK signaling and proliferation in mantle cell lymphoma (MCL) cells by degrading BTK, IKFZ1, and IKFZ3 (3 validated targets in B-cell malignancies). Also degrades Ibrutinib (Cat. No. 6813) -resistant C481S-BTK mutant cancer cells. Exhibits no binding against a panel of 468 kinases at 1 μM. Reduces tumor burden and extends survival in lymphoma patient-derived xenograft models.

A-1208746，一种MCL-1抑制剂，其Ki值为0.454 nM。该化合物能够激活caspase-3 -7，诱发H929细胞的细胞凋亡(apoptosis)，并降低线粒体膜电位。此外，A-1208746与Navitoclax共同使用时，可以在癌症研究中发挥协同效应。