I-BRD9

SKU: orb1225951

Description

The first selective cellular chemical probe for BRD9 with pIC50 of 7.3; displays 700-fold selectivity over the BET family and 200-fold over the highly homologous BRD7; decreases cell proliferation, G1-arrest and apoptosis in rhabdoid tumor cells; shows synergistic inhibitory effects on cell proliferation combined with doxorubicin or carboplatin.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1714146-59-4
• MW: 497.5536
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₂F₃N₃O₃S₂
• SMILES: N=C(C(S1)=CC2=C1C(C3=CC=CC(C(F)(F)F)=C3)=CN(CC)C2=O)NC(CC4)CCS4(=O)=O
• Target: Bromodomain
• Solubility: DMSO: 15.5 mg/mL

Bioactivity

• In Vitro:
  I-BRD9 (10 μM, 6 h) has a regulation role in cancer and immunology pathways. I-BRD9 (10 μM) has high BRD9 affinity and excellent broader bromodomain selectivity. I-BRD9 (10 μM) has affinity for BRD9 (TR-FRET), BRD4 BD1 (TR-FRET) and BRD9 NanoBRET with pIC50 values of 7.3 μM, 5.3 μM and 6.8 μM. I-BRD9 (10 μM) has high aqueous solubility (CLND) with 359 μM. I-BRD9 (10 μM) displays >625 fold selectivity in binding with endogenous BRD9 against BET family member BRD3 in HUT-78 cell lysate. RT-PCR Cell line: Kasumi-1 cells. Concentration: 10 μM. Incubation time: 6 h. Result: Showed 4 genes (CLEC1, 62 DUSP6, 63 FES64 and SAMSN165) that were strongly down-regulated and not by I-BET151.
  Read more...

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

I-BRD9 | I-BRD-9 | I-BRD 9

Quick Database Links

Gene Symbol

Bromodomain