THZ531

Igoa vaila'au:

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

SMILES Code:

"O=C(NC1=CC=C(C(N2C[C@H])(NC3=NC=C(Cl)C(C4=CNC5=C4C=CC=C5)=N3)CCC2)=O)C= C1)/C=C/CN(C)C "

InChi Code:

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

InChi Key:

RUBYHLPRZRMTJO-MOVYNIQHSA-N

upu autu:

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

Solubility:Solu i le DMSO

Teuina:0 - 4°C mo taimi pupuu (aso i vaiaso), poo le -20°C mo taimi uumi (masina).

Fa'amatalaga:

THZ531 o le CDK12 ma le CDK13 covalent inhibitor. Cyclin-faalagolago kinases 12 ma 13 (CDK12 ma CDK13) e taua tele i le faʻatonutonuina o faʻasologa o kenera. O le THZ531 e le mafai ona faʻaaogaina se cysteine ​​o loʻo i fafo atu o le kinase domain. O le THZ531 e mafua ai le leiloa o le fa'aaliga o kenera ma le leiloa fa'atasi o le RNA polymerase II fa'aumi ma le hyperphosphorylated. O le THZ531 e matua fa'aitiitia ai le fa'aaliga o kenera tali fa'aleagaina DNA ma fa'atupu fa'aliliuga e feso'ota'i sili e fa'aleleia atili. O le THZ531 na matua fa'aosoina le oti o le cell apoptotic. O molelaiti laiti e mafai ona fa'atatau tonu i le CDK12 ma le CDK13 e mafai ona fesoasoani e fa'ailoa vaega laiti o le kanesa e fa'alagolago i a latou gaioiga kinase.

Sini: CDK