can-508 and Multiple-Myeloma

can-508 has been researched along with Multiple-Myeloma* in 1 studies

Other Studies

1 other study(ies) available for can-508 and Multiple-Myeloma

ArticleYear
Arylazopyrazole AAP1742 inhibits CDKs and induces apoptosis in multiple myeloma cells via Mcl-1 downregulation.
    Chemical biology & drug design, 2014, Volume: 84, Issue:4

    Inhibitors of cyclin-dependent kinases 9 have been developed as potential anticancer drugs for the treatment of multiple myeloma. We have previously prepared a library of arylazo-3,5-diaminopyrazole inhibitors of CDKs. Here, we describe a novel member, AAP1742 (CDK9 inhibition with IC(50) = 0.28 μm), that reduces the viability of multiple myeloma cell lines in low micromolar concentrations. Consistent with inhibition of CDK9, AAP1742 decreases the phosphorylation of RNA polymerase II and inhibits mRNA synthesis of anti-apoptotic proteins Mcl-1, Bcl-2, and XIAP, followed by apoptosis in the RPMI-8226 cell line in a dose- and a time-dependent manner. These results are consistent with the biochemical profile of AAP1742 and further suggest cellular inhibition of CDK9 as a possible target for anticancer drugs.

    Topics: Antineoplastic Agents; Apoptosis; Azo Compounds; Cell Line, Tumor; Cyclin-Dependent Kinase 9; Down-Regulation; Enzyme Activation; Humans; Mitochondria; Multiple Myeloma; Myeloid Cell Leukemia Sequence 1 Protein; Phosphorylation; Proto-Oncogene Proteins c-bcl-2; Pyrazoles; RNA Polymerase II; RNA, Messenger; X-Linked Inhibitor of Apoptosis Protein

2014