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BIX-01294

Chemical Structure : BIX-01294

CAS No.: 935693-62-2

BIX-01294 (BIX 01294, BIX01294)

Catalog No.: PC-42673Not For Human Use, Lab Use Only.

BIX-01294 is a specific small molecule G9a histone methyltransferase inhibitor with IC50 of 1.7 uM.

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Biological Activity

BIX-01294 is a specific small molecule G9a histone methyltransferase inhibitor with IC50 of 1.7 uM.
BIX-01294 weakly inhibits the closely related GLP enzyme (IC50=38 uM), no inhibition of the other HMTases (>45 uM).
BIX-01294 reduces H3K9me2 of bulk histones in several cell lines, enables reprogramming of Oct4/Klf4-transduced mouse embryonic fibroblasts combined with BayK8644.
BIX-01294 also can reactivate expression of HIV-1 from latently infected cells.

Physicochemical Properties

M.Wt 490.6403
Formula C28H38N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Kubicek S, et al. Mol Cell. 2007 Feb 9;25(3):473-81.

2. Shi Y, et al. Cell Stem Cell. 2008 Nov 6;3(5):568-74.

3. Chang Y, et al. Nat Struct Mol Biol. 2009 Mar;16(3):312-7.

4. Imai K, et al. J Biol Chem. 2010 May 28;285(22):16538-45.

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