BI-7273

SKU: orb1225831

Description

A potent, selective and cell-permeable BRD9 bromodomain inhibitor with IC50 of 19 nM in Alpha assay; displays >5-fold selectiveity over BRD7, and >5,000-fold over BRD4-BD1, BRD4-BD2, and BRD2-BD1; blocks EOL-1 cell proliferation with EC50 of 1.4 uM, and displays antitumor activity in an AML xenograft model.

Key Properties

• CAS Number: 1883429-21-7
• MW: 353.4149
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₃N₃O₃
• SMILES: O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C(OC)=C2)C3=CC=NC=C13
• Target: Bromodomain
• Solubility: DMSO: 10 mg/mL

Bioactivity

• In Vitro:
  BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM. BI-7273 also has slight activity against a panel of kinases such as CECR2, BRPF1, BRD1, CREBBP, EP300, FALZ, TAF1(2) and TAF1 L(2), with Kds of 8.8 nM, 210 nM, 2600 nM, 8600 nM, 10000 nM, 850 nM, 1000 nM, and 1200 nM, respectively. BI-7273 (1 μM) is active in U2OS cell lines. BI-7273 blocks EOL-1 cell proliferation with EC50 of 1400 nM.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BI7273 | BI 7273

Quick Database Links

Gene Symbol

Bromodomain