BIX-01294 (hydrochloride hydrate)
BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells[1][2].
Product Specifications
CAS Number
1808255-64-2
UNSPSC
12352005
Target
Apoptosis; Autophagy; Histone Methyltransferase
Type
Reference compound
Related Pathways
Apoptosis; Autophagy; Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/bix-01294-hydrochloride-hydrate.html
Solubility
10 mM in DMSO
Smiles
COC1=CC2=C(NC3CCN(CC3)CC4=CC=CC=C4)N=C(N5CCN(CCC5)C)N=C2C=C1OC.Cl.O.Cl.Cl.[x]
Molecular Formula
C28H38N6O2.3ClH.xH2O
References & Citations
[1]Ciechomska IA, et al., BIX01294, an inhibitor of histone methyltransferase, induces autophagy-dependent differentiation of glioma stem-like cells. Sci Rep. 2016 Dec 9;6:38723.|[2]Kubicek S, O'Sullivan RJ, August EM, Hickey ER, Zhang Q, Teodoro ML, Rea S, Mechtler K, Kowalski JA, Homon CA, Kelly TA, Jenuwein T. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25 (3) :473-81.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EHMT1/GLP/KMT1D; EHMT2/G9a/KMT1C
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