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

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 935693-62-2
• MW: 490.64
• Purity: 99.64% (May vary between batches)
• Formula: C₂₈H₃₈N₆O₂
• SMILES: N(C=1C2=C(N=C(N1)N3CCN(C)CCC3)C=C(OC)C(OC)=C2)C4CCN(CC5=CC=CC=C5)CC4
• Target: Histone Methyltransferase,Autophagy
• Solubility: DMSO:84.17 mg/mL (171.55 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (6.73 mM)

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.
• 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

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• 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