GSK-461364

Lub npe tshuaj:

(R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy) Thiophene-2-carboxamide

SMILES Code:

O=C(C1=C(O[C@@H](C2=CC=CC=C2C(F)(F)F)C)C=C(N3C=NC4=CC=C(CN5CCN(C)5) )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 ib 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 Key:

ZHJGWYRLJUCMRT-QGZVFWFLSA-N

Lo lus tseem ceeb:

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

Solubility:Soluble hauv DMSO

Cia:0 - 4 ° C rau lub sijhawm luv (hnub mus rau lub lis piam), lossis -20 ° C rau lub sijhawm ntev (hli)

Nqe lus piav qhia:

Polo-zoo li kinases (Plks) yog serine / threonine kinases nrog lub luag haujlwm tseem ceeb hauv cell cycling. GSK461364 yog lub zog, thim rov qab inhibitor ntawm Plk1 (Ki = 2.2 nM). Nws tsis tshua muaj txiaj ntsig rau Plk2 thiab Plk3 (Kis = 860 thiab 1,000 nM, feem) thiab tsawg kawg yog 1,000-fold xaiv rau Plk1 hla lub vaj huam sib luag ntawm 48 lwm kinases. GSK461364 koob tshuaj-raws li nres lub xov tooj ntawm tes cycling nyob rau hauv ntau yam proliferating mob qog noj ntshav cell kab thiab, ntawm ntau dua koob tshuaj, ua rau apoptosis. Nws zoo nkaus li muaj txiaj ntsig zoo rau cov qog p53-tsis muaj peev xwm thiab muaj peev xwm hla cov ntshav-hlwb teeb meem. GSK461364 muaj txiaj ntsig zoo hauv vivo, ua rau qog kev loj hlob inhibition lossis kev loj hlob qeeb hauv xenograft qauv hauv nas.

Hom phiaj: Plk1