THZ531

Izina ryimiti:

(R, E) -N- (4- (3 - (5 (dimethylamino) ariko-2-enamide

Kode ya SMILES:

"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 Urufunguzo:

RUBYHLPRZRMTJO-MOVYNIQHSA-N

Ijambo ryibanze:

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

Gukemura:Gukemura muri DMSO

Ububiko:0 - 4 ° C mugihe gito (iminsi kugeza ibyumweru), cyangwa -20 ° C mugihe kirekire (amezi).

Ibisobanuro:

THZ531 ni covalent CDK12 na CDK13 ya covalent inhibitor. Cyclin-iterwa na kinase 12 na 13 (CDK12 na CDK13) zigira uruhare runini mugutunganya gene. THZ531 yibasiye bidasubirwaho sisitemu iri hanze ya domaine ya kinase. THZ531 itera gutakaza imvugo ya gene hamwe no gutakaza icyarimwe kuramba hamwe na hyperphosifora RNA polymerase II. THZ531 igabanya cyane imvugo ya ADN yangiza ibyangiritse hamwe ningenzi byingenzi byiyongera-bifitanye isano na transcription. THZ531 yateje urupfu apoptotic selile. Molekile ntoya ishoboye kwibasira CDK12 na CDK13 irashobora rero gufasha kumenya ubwoko bwa kanseri buterwa cyane nibikorwa bya kinase.

Intego: CDK