GSK-461364

Izina ryimiti:

(R) -5- (6 - ((4-methylpiperazin-1-yl) methyl) -1H-benzo thiophene-2-carboxamide

Kode ya SMILES:

O = C (C1 = C (O [C @@ H] (C2 = CC = CC = C2C (F) (F) F) C) C = C (N3C = NC4 = CC = C (CN5CCN (C) CC5 ) C = C34) S1) N.

InChi Code:

InChI = 1S / C27H28F3N5O2S / c1-17 (19-5-3-4-6-20 (19) 27 (28,29) 30) 37-23-14-24 (38-25 (23) 26 (31) 36) 35-16-32-21 -8-7-18 (13-22 (21) 35) 15-34-11-9-33 (2) 10-12-34 / h3-8,13-14,16-17H, 9-12,15H2 , 1-2H3, (H2,31,36) / t17- / m1 / s1

InChi Urufunguzo:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Ijambo ryibanze:

GSK-461364, GSK461364, GSK 461364, GSK-461364A, GSK 461364A, GSK461364A, 929095-18-1

Gukemura:Gukemura muri DMSO

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

Ibisobanuro:

Polo-isa na kinase (Plks) ni serine / threonine kinase ifite uruhare runini mukigare cyamagare. GSK461364 ninzitizi ikomeye, ihindagurika ya Plk1 (Ki = 2.2 nM). Ntabwo ari byiza kurwanya Plk2 na Plk3 (Kis = 860 na 1.000 nM, kimwe) kandi byibuze inshuro 1.000 zatoranijwe kuri Plk1 hejuru yitsinda rya 48 za kinase. GSK461364 ikoreshwa cyane ihagarika amagare ya selile mumirongo itandukanye ya kanseri ikwirakwira kandi, iyo ikabije, itera apoptose. Bigaragara ko ari byiza kurwanya ibibyimba bidafite p53 kandi birashobora kurenga inzitizi yubwonko bwamaraso. GSK461364 ifite akamaro muri vivo, itera gukura kw'ibibyimba cyangwa gutinda gukura mubyitegererezo bya xenograft mu mbeba.

Intego: Plk1