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[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 Weight600.02
Molecular FormulaC28H38N6O2.3HCl
SMILESCOC1=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

1 mg5 mg10 mg
1 mM1.6666 mL8.3331 mL16.6661 mL
5 mM0.3333 mL1.6666 mL3.3332 mL
10 mM0.1667 mL0.8333 mL1.6666 mL
50 mM0.0333 mL0.1667 mL0.3333 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.


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