BIX-01294

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Chemical Information

Product name：BIX-01294	Purity：98% min
CAS NO：935693-62-2	Solubility：DMSO : ≥ 110 mg/mL (224.20 mM)
Molecular Formula：C₂₈H₄₃Cl₃N₆O₃	Package：Package according to customer requirements.
Molecular Weight：618.038	Storage：store at 2-8°C

Quality control

Remarks

BIX-01294 is a reversible and highly selective G9a Histone Methyltransferase inhibitor, with an IC50 of 2.7 μM in DELFIA assay. BIX-01294 specifically inhibits G9a (H3K9me2) and GLP enzyme (H3K9me3), with IC50s of 1.7 μM and 38 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.

Properties:

Boiling point: 654.6±65.0 °C(Predicted)

density: 1.195±0.06 g/cm3(Predicted)

pka: 9.34±0.70(Predicted)

form: Off-white solid

References

[1]. 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.

[2]. 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.