BI-9564

SKU: orb1300467

Description

BI-9564 is a potent and cell-permeable small molecule inhibitor that selectively targets the bromodomain of BRD9 with a Kd of 5.9 nM, while exhibiting minimal activity against the BET family (IC50 > 100 µM). This tool compound is widely used in vitro and in vivo to probe BRD9 function in oncology, immunology, and epigenetics research.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1883429-22-8
• MW: 353.41
• Purity: 99.38% (May vary between batches)
• Formula: C₂₀H₂₃N₃O₃
• SMILES: COc1cc(c(OC)cc1CN(C)C)-c1cn(C)c(=O)c2cnccc12
• Target: Epigenetic Reader Domain
• Solubility: DMSO:3.54 mg/mL (10.02 mM)

Bioactivity

• Target IC50:
  BRD9:Kd: 20 nM|BRD7:3.4 μM|BRD7:239 nM (Kd)
• In Vivo:
  In vivo proof-of-concept studies, BI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles. Compared to survival of the control group in a xenograft model of human AML, BI-9564 results in a modest but significant additional survival benefit of 2 days.
• In Vitro:
  EOL-1, human acute myeloid eosinophilic leukemia cell line, was antiproliferative byBI-9564 with EC50 of 800 nM.BRD7 implied as a tumor suppressor and is down-regulated in cancer cells, BI-9564 shows Kd of 73 nM for it, and is >10-fold more selective for BRD9 over the high homologues bromodomain. BI-9564 (<5 μM) shows no activity against 324 kinases, when BI-9564 at 10 μM, an inhibition >40% is observed for only 2 out of 55 GPCRs.
• Cell Research:
  To 750,000 MV-4-11 cells in 250 μl growth medium (in IMDM, 10 % FBS, GlutaMAX, 25 mM HEPES and 0,1% 2-Mercaptoethanol) per well compound is added at the desired concentration from a 10 mM stock solution using the HP D300 Digital Dispenser. After 2 hours of incubation with the compound, cells are collected by centrifugation, washed in ice cold PBS and lysed in 15 μl of cell extraction buffer. After 30 minutes on ice, nucleic acids are disrupted by sonication. cMYC levels are measured using the human c-Myc (Total) ELISA Kit. (Only for Reference)
• Animal Research:
  Female CIEA-NOG mice engrafted intravenously with 1×107 EOL-1 AML cells, which express stably luciferase and GFP, were administered orally on day 5 with BI-9564(10 mL/kg body weight), which is formulated with 0.5% Natrosol.

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

inhibit, Inhibitor, Epigenetic Reader Domain, EpigeneticReaderDomain, BI9564, BI-9564, BI 9564, BRD9

Compound Identifiers

PubChem CID

117072549