1594092-37-1 Usage
Uses
AZ191 is a potent and selective DYRK1B inhibitor (1).
Enzyme inhibitor
This potent and selective DYRK inhibitor (FW = 429.53 g/mol), also systematically named N-(2-methoxy-4-(4-methylpiperazin-1-yl)phenyl)-4- (1-methyl-1H-pyrrolo[2,3-c]pyridin-3-yl)pyrimidin-2-amine, selectively targets DYRK1B, a Dual specificity tyrosine-phosphorylation-regulated kinase, with an IC50 value of 17 nM, or about 5x and 110x higher affinity than for DYRK1A and DYRK2. AZ191 is effective both in vitro and in cells. DYRK1B has also been proposed to promote the turnover of Cyclin D1, a key regulator of mammalian G1-S-phase transitions. Cyclin D1 is phosphorylated on Thr-286 by GSK3β (or glycogen synthase kinase 3β), thereby promoting its degradation.
Check Digit Verification of cas no
The CAS Registry Mumber 1594092-37-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,5,9,4,0,9 and 2 respectively; the second part has 2 digits, 3 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 1594092-37:
(9*1)+(8*5)+(7*9)+(6*4)+(5*0)+(4*9)+(3*2)+(2*3)+(1*7)=191
191 % 10 = 1
So 1594092-37-1 is a valid CAS Registry Number.
1594092-37-1Relevant articles and documents
Discovery and optimization of a novel series of dyrk1b kinase inhibitors to explore a MEK resistance hypothesis
Kettle, Jason G.,Ballard, Peter,Bardelle, Catherine,Cockerill, Mark,Colclough, Nicola,Critchlow, Susan E.,Debreczeni, Judit,Fairley, Gary,Fillery, Shaun,Graham, Mark A.,Goodwin, Louise,Guichard, Sylvie,Hudson, Kevin,Ward, Richard A.,Whittaker, David
, p. 2834 - 2844 (2015/04/14)
Potent and selective inhibitors of Dyrk1B kinase were developed to explore the hypothesis, based on siRNA studies, that Dyrk1B may be a resistance mechanism in cells undergoing a stress response.
