OICR-9429

SKU: orb1300349

Description

OICR-9429 is a potent small molecule antagonist that disrupts the WDR5 interaction with MLL and histone H3 peptides. It demonstrates anti-leukemic activity by reducing the viability of acute myeloid leukemia cells in vitro, making it a valuable chemical probe for oncology research targeting epigenetic protein-protein interactions.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1801787-56-3
• MW: 555.59
• Purity: 99.74%
• Formula: C₂₉H₃₂F₃N₅O₃
• SMILES: CN1CCN(CC1)c1ccc(cc1NC(=O)c1c[nH]c(=O)cc1C(F)(F)F)-c1cccc(CN2CCOCC2)c1
• Target: Histone Methyltransferase,JAK,Apoptosis
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.6 mM);Ethanol:12 mg/mL (21.6 mM);DMSO:35.71 mg/mL (64.27 mM)

Bioactivity

• Target IC50:
  WDR5:93 nM(Kd)
• In Vitro:
  OICR-9429 binds WDR5 with high affinity (Kd=93±28 nM) and competitively disrupts its interaction with a high-affinity Wdr5-interacting (WIN) peptide of MLL (Kdisp=64±4 nM).
• Cell Research:
  20,000 viable, actively proliferating primary human AML cells per well were seeded in 96-well plates in triplicates and treated with 0.05% DMSO or OICR-9429. Cell viability was measured using the Cell Titer-Glo luminescent cell viability assay on a VICTOR X4 luminometer after 72 h.(Only for Reference)

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

pancreatic, inhibit, MLL, OICR9429, OICR-9429, OICR 9429, Inhibitor, HistoneMethyltransferase, Histone Methyltransferase, leukaemia, H3K4, bladder cancer (BCa), Apoptosis, colon, WDR5, WD repeat domain 5 (WDR5), prostate cance

Compound Identifiers

PubChem CID

91623360