KH CB19

KH-CB19 is a potent and highly specific inhibitor of the CDC2-like kinase isoforms 1 and 4 (CLK1/CLK4).IC50 value: 20 nM (CLK1) [1]Target: CLK1/4 inhibitorin vitro: KH-CB19 showed potent inhibition of CLK1 with an IC50 of 20 nM, and for the pure isomer KH-CB19, almost 100-fold selectivity against the CLK3 isoform. Pretreatment of cells with KH-CB19 or TG003 led to a reduction of the TNF-α-induced increase in phosphorylation of all analyzed SR proteins compared with TNF-α-stimulated controls.Treatment of resting cells with 10 μM KH-CB19 significantly reduced the basal expression of flTF as well as asHTF [1].

Research Areas >> Cancer

CLK1:19.7 nM (IC50)

CLK3:530 nM (IC50)

DYRK1A:55.2 nM (IC50)

[1]. Fedorov O, et al. Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol. 2011 Jan 28;18(1):67-76.

[2]. Grant SK, et al. Kinase inhibition that hinges on halogen bonds. Chem Biol. 2011 Jan 28;18(1):3-4.

Abemaciclib(LY2835219) | Ribociclib (LEE011) | Dinaciclib (SCH727965) | THZ1 2HCl | Roscovitine (CYC202) | THZ531 | RO-3306 | Flavopiridol | NVP 2 | BAY-1143572 Racemate | CYC-065 | AZD5438 | BIO | Kenpaullone | SNS-032 (BMS-387032)