THZ531

Magaca Kiimikada:

(R,E)-N-(4-(3-(5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidine-1-carbonyl) phenyl)-4- (dimethylamino) laakiin -2-enamide

Koodhka dhoola cadeynta:

"O=C(NC1=CC=C(N2C[C@H](NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)CCCC2=O)C= C1)/C=C/CN(C)C"

Koodhka InChi:

InChi=1S/C30H32ClN7O2/c1-37(2)15-6-10-27(39)34-21-13-11-20(12-14-21)29(40)38-16-5-7- 22 (19-38) 35-30-33-18-25 (31)28 (36-30)24-17-32-26-9-4-3-8-23 (24)26/h3-4, 6,8-14,17-18,22,32H,5,7,15-16,19H2,1-2H3,(H,34,39)(H,33,35,36)/b10-6+/ t22-/m1/s1

Furaha InChi:

RUBYHLPRZRMTJO-MOVYNIQHSA-N

Ereyga muhiimka ah:

THZ-531, THZ 531, THZ531, 1702809-17-3

Xalka:Ku milmay DMSO

Kaydinta:0 - 4°C muddo gaaban (maalmo ilaa toddobaadyo), ama -20°C muddo dheer (bilo).

Sharaxaad:

THZ531 waa isku-darka CDK12 iyo CDK13 covalent inhibitor. Kinases-ku-tiirsanaanta cyclin 12 iyo 13 (CDK12 iyo CDK13) ayaa door muhiim ah ka ciyaara habaynta qoraalka hiddo-wadaha. THZ531 waxay si aan leexleexad lahayn u beegsanaysaa cysteine-ka oo ku yaalla meel ka baxsan domain-ka kinase. THZ531 waxay sababtaa luminta muujinta hidda-wadaha iyadoo ay weheliso luminta dhererka iyo hyperphosphorylated RNA polymerase II. THZ531 waxay si weyn u yaraynaysaa muujinta hiddo-wadaha jawaab-celinta DNA-da iyo hiddo-wadaha muhiimka ah ee kor-u-qaadka la xidhiidha. THZ531 ayaa si aad ah u keentay dhimashada unugyada apoptotic. Unugyada yaryar ee awood u leh inay si gaar ah u beegsadaan CDK12 iyo CDK13 ayaa laga yaabaa inay sidaas darteed caawiyaan aqoonsiga noocyada hoose ee kansarka kuwaas oo si gaar ah ugu tiirsan hawlahooda kinase.

Ujeedka: CDK