ATP site-targeting, potent and selective inhibitor against cdc-like kinase (cdc2-like kinase) CLK1, CLK2, CLK4, and homeodomain-interacting protein kinase 2 (HIPK2), but not CLK3.
MU1210 is a potent and selective inhibitor against cdc-like kinase (cdc2-like kinase) CLK1, CLK2, CLK4 (CLK1/2/4 IC50 = 8/20/12 nM; CLK1/2/4 Ki = 84/91/23 nM by NanoBRET) and HIPK2 (IC50 = 29 nM) with good selectivity over HIPK1/3 (IC50 = 187/159 nM), DYRK1a/1b/2 (IC50 = 213/956/1309 nM), CLK3 (IC50 >3 μM) and 194 other kinases. MU1210 enhances alternative spliced MDM4-S mRNA (10 μM, 24 h) and exhibits antiproliferation activity in MCF7 cultures (IC50 in 72 h = 1.1 μM). Unlike most ATP site-targeting kinase inhibitors, X-ray crystallography shows that MU1210 is anchored to the back pocket instead of the hinge region of CLK1. MU140 serves as a negative control.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Choose from one of the most recent versions:
Certificates of Analysis (COA)
Lot/Batch Number
It looks like we've run into a problem, but you can still download Certificates of Analysis from our Documents section.
Angewandte Chemie (International ed. in English), 58(4), 1062-1066 (2018-12-21)
Reported is the identification of the furo[3,2-b]pyridine core as a novel scaffold for potent and highly selective inhibitors of cdc-like kinases (CLKs) and efficient modulators of the Hedgehog signaling pathway. Initially, a diverse target compound set was prepared by synthetic
Questions
Reviews
★★★★★ No rating value
Active Filters
Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.
