Synonyms: 1-Methyl-4-(9-(3-(pyridin-4-yl)-phenyl)-7-oxa-2-aza-bicyclo[4.3.0]nona-1,3,5,8-tetraen-3-yl)-1H-pyrazole; 5-(1-Methyl-1H-pyrazol-4-yl)-3-(3-(pyridin-4-yl)phenyl)furo[3,2-b]pyridine; VN339
Molecular Formula: C22H16N4O
Molecular Weight: 352.39
Linear Structural Formula: C22H16N4O
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: 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 muM) and 194 other kinases. MU1210 enhances alternative spliced MDM4-S mRNA (10 muM, 24 h) and exhibits antiproliferation activity in MCF7 cultures (IC50 in 72 h = 1.1 muM). 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.