BIX-01294

Research use only, not for human use.

A specific small molecule G9a histone methyltransferase inhibitor with IC50 of 1.7 uM.

A specific small molecule G9a histone methyltransferase inhibitor with IC50 of 1.7 uM; weakly inhibits the closely related GLP enzyme (IC50=38 uM), no inhibition of the other HMTases (>45 uM); reduces H3K9me2 of bulk histones in several cell lines, enables reprogramming of Oct4/Klf4-transduced mouse embryonic fibroblasts combined with BayK8644; also can reactivate expression of HIV-1 from latently infected cells.

Cell Viability Assay Cell Line:Primary or recurrent tumor cells Concentration:2 μM Incubation Time:48 hours Result:Selectively inhibited recurrent tumor cell growth.

Animal Model:Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells Dosage:10 mg/kg Administration:IP; three times a week for 2 weeks Result:Significantly reduced tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth was not inhibited. Slowed the growth of orthotopic recurrent tumors in athymic nude recipients.

BIX 01294 | BIX01294

Chromatin/Epigenetic

HMTase

HMTase

Cancer

——

935693-62-2

490.6403

C28H38N6O2

>98% (HPLC)

10 mM in DMSO

CN1CCCN(CC1)C2=NC3=CC(=C(C=C3C(=N2)NC4CCN(CC4)CC5=CC=CC=C5)OC)OC

4-Quinazolinamine, 2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-6,7-dimethoxy-N-[1-(phenylmethyl)-4-piperidinyl]-

(-20℃)

With Ice Pack

≥ 2 years