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BIX-01294

CAT: 0804-HY-10587-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-10587-01Size:5 mg
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Description
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl) -quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells[1][2][3][4][5].
CAS Number
[935693-62-2]
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Autophagy; Histone Methyltransferase
Type
Reference compound
Related Pathways
Autophagy; Epigenetics
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/BIX-01294.html
Purity
98.44
Solubility
DMSO : ≥ 110 mg/mL|H2O : < 0.1 mg/mL (ultrasonic)
Smiles
COC1=C(OC)C=C(C(NC2CCN(CC3=CC=CC=C3)CC2)=NC(N4CCN(C)CCC4)=N5)C5=C1
Molecular Formula
C28H38N6O2
Molecular Weight
490.64
Precautions
H302, H315, H319, H335
References & Citations
[1]Kubicek S, et al. Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase. Mol Cell. 2007 Feb 9;25 (3) :473-81.|[2]Yang Q, et al. BIX-01294 treatment blocks cell proliferation, migration and contractility in ovine foetal pulmonary arterial smooth muscle cells. Cell Prolif. 2012 Aug;45 (4) :335-44.|[3]Nathaniel W Mabe, et al. G9a Promotes Breast Cancer Recurrence through Repression of a Pro-inflammatory Program. Cell Rep. 2020 Nov 3;33 (5) :108341.|[4]Iwona Anna Ciechomska, et al. BIX01294, an inhibitor of histone methyltransferase, induces autophagy-dependent differentiation of glioma stem-like cells. Sci Rep|[5]Yanqi Chang, et al.Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294. Nat Struct Mol Biol. 2009 Mar;16 (3) :312-7.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EHMT1/GLP/KMT1D; EHMT2/G9a/KMT1C

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