mcl-1-in-9

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

A09-003 is a novel cell cycle protein-dependent kinase-9 CDK-9 inhibitor.A09-003 inhibits the proliferation of a variety of leukemia cell lines and inhibits the increase of leukemia sequence-1 protein in myeloid cells.A09-003 also induces apoptosis, decreases RNA polymerase II activity, and decreases Mcl-1 expression.

PDGFRA/CAIX/XII-IN-1 is a multi-target inhibitor targeting PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA and Ki values of 93.3 nM and 80.0 nM against CA IX and CA XII respectively. It targets and binds to the ATP-binding pocket of PDGFRA, thereby blocking the activation of downstream signaling pathways such as STAT3, AKT and ERK1/2. It induces G0/G1 phase cell cycle arrest and initiates endogenous apoptotic procedures, manifested as cleavage and activation of PARP-1, caspase-9 and caspase-3, upregulation of caspase 3/7 activity and inhibition of Mcl-1 protein expression. It exerts significant anti-proliferative effects in eosinophilic leukemia cells and can serve as a candidate tool compound for mechanism and efficacy research of leukemia.

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

Ibulocydine is a potent CDK inhibitor. Ibulocydine has high activity against Cdk7/cyclin H/Mat1 and Cdk9/cyclin T. Ibulocydine inhibited the growth of HCC cells more effectively than other Cdk inhibitors, including olomoucine and roscovitine, whereas ibulocydine as well as the other Cdk inhibitors and BMK-Y101 minimally influenced the growth of normal hepatocyte cells. Ibulocydine induced apoptosis in HCC cells, most likely by inhibiting Cdk7 and Cdk9. In vitro treatment of HCC cells with ibulocydine rapidly blocked phosphorylation of the carboxyl-terminal domain (CTD) of the large subunit of RNA polymerase II, a process mediated by Cdk7/9. Anti-apoptotic gene products such as Mcl-1, survivin, and X-linked IAP (XIAP) are crucial for the survival of many cell types, including HCC. Following the inhibition of RNA polymerase II phosphorylation, ibulocydine caused rapid down-regulation of Mcl-1, survivin, and XIAP, thus inducing apoptosis. Furthermore, ibulocydine effectively ind......

Mcl-1 Inhibitor 16 (Compound 9), a platinum-based mitochondrial-targeting agent, inhibits Mcl-1 and induces Bax/Bak-dependent apoptosis in cancer cells. This compound exhibits antitumor activity and may be utilized as a monotherapy or in combination with ABT-199 [1].