BIX-01294

SKU: orb1299583

Description

BIX-01294 is a cell-permeable, potent, and selective inhibitor of the histone methyltransferase G9a (IC50 = 1.9 µM). It is widely used in epigenetic research to probe the role of histone H3 lysine 9 methylation in gene silencing, cellular differentiation, and has demonstrated utility in both in vitro and in vivo experimental models.

Research Area

Epigenetics & Chromatin, Neuroscience, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 935693-62-2
• MW: 600.0
• Purity: >98%
• Formula: C₂₈H₃₈N₆O₂ • 3HCl
• SMILES: N(C=1C2=C(N=C(N1)N3CCN(C)CCC3)C=C(OC)C(OC)=C2)C4CCN(CC5=CC=CC=C5)CC4
• Target: Protein methyltransferase
• Solubility: Soluble in DMSO (up to 50 mg/ml), or in Water (up to 50 mg/ml).

Bioactivity

• Target IC50:
  G9a:1.9 μM
• In Vitro:
  BIX-01294 induced caspase-dependent apoptosis in human bladder cancer cells. BIX-01294 stimulates endoplasmic reticulum stress (ER stress) and up-regulated expression of PMAIP1 through DDIT3 up-regulation. Furthermore, down-regulation of the deubiquitinase USP9X by BIX-01294 results in downstream reduction of MCL1 expression, leading to apoptosis eventually.
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• Cell Research:
  On the first day, cells were seeded in 96 well plates. Twenty-four hours later, BIX-01294 was added at the indicated concentrations in each well. After treatment by BIX-01294 for another 24 h, we used 10% TCA to immobilize the cells and then evaluated the living cell numbers using the sulforhodamine B assay as previously described
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Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PRMT1, recurrent, p21, SUV39H1(H320R), inhibit, Inhibitor, MLKL, p53, Histone Methyltransferase, HistoneMethyltransferase, Gadd45a, G9a, H3K9me2, H3K9me3, Cdkn1a, Autophagy, BIX 01294, BIX01294, BIX-01294

Compound Identifiers

PubChem CID

25150857