[CAS NO. 1392399-03-9] BIX 01294

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PRODUCTS SPECIFICATIONS [1392399-03-9]

Catalog

SLK-S8006

Brand

Selleck

CAS

1392399-03-9

DESCRIPTION [1392399-03-9]

Overview

MDL	-
Molecular Weight	600.02
Molecular Formula	C28H38N6O2.3HCl
SMILES	COC1=CC2=NC(N3CCN(C)CCC3)=NC(NC4CCN(CC5=CC=CC=C5)CC4)=C2C=C1OC.[H]Cl.[H]Cl.[H]Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	1.6666 mL	8.3331 mL	16.6661 mL
5 mM	0.3333 mL	1.6666 mL	3.3332 mL
10 mM	0.1667 mL	0.8333 mL	1.6666 mL
50 mM	0.0333 mL	0.1667 mL	0.3333 mL

Description

BIX01294 is an inhibitor of G9a with of 2.7 μM in a cell-free assay, reduces H3K9me2 of bulk histones, also weakly inhibits GLP (primarily H3K9me3), no significant activity observed at other histone methyltransferases. BIX01294 induces . BIX01294 also inhibits H3K36 methylation by oncoproteins , and .

Targets

G9a ^[1]
(Cell-free assay)

2.7 μM

In vitro

BIX01294 is a selective inhibitor of G9a histone methyltransferase and does not affect SUV39H1(H320R) and PRMT1 within the tested concentration range. BIX-01294 specifically inhibited G9a (H3K9me2) and, to a lesser extent, the closely related GLP enzyme (primarily H3K9me3), with an IC50 of 1.7 μM for G9a and 38 μM for GLP. BIX-01294 inhibits G9a in an uncompetitive manner with SAM. BIX-01294 (4.1μM) reduces H3K9me2 Levels in Bulk Histone Preparations from wt ES cells, mouse embryonic fibroblasts and HeLa cells, but not in G9a deficient stem cells. BIX-01294 is a valuable inhibitor for the transient modulation of chromosomal H3K9me2. BIX-01294 Reduces H3K9me2 at Several G9a Target Genes including Bim1 and Serac1. BIX01294 could reactivate expression of HIV-1 from latently infected cells such as ACH-2 and OM10.1.

References

[1] Kubicek S, et al. Mol Cell, 2007, 25(3), 473-481.
[2] Imai K, et al. J Biol Chem, 2010, 285(22), 16538-16545.
[3] Mabe NW, et al. Cell Rep. 2020 Nov 3;33(5):108341.