MAK-683 hyrochloride

SKU: orb1297951

Description

MAK683 hydrochloride is a potent and selective embryonic ectodermal development (EED) inhibitor that disrupts PRC2 complex activity, demonstrating strong anti-proliferative effects in cancer cells. This tool compound is widely used in epigenetic research to investigate PRC2-driven malignancies in both cellular and animal models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 2170606-94-5
• MW: 412.85
• Purity: >99.99% (May vary between batches)
• Formula: C₂₀H₁₈ClFN₆O
• SMILES: FC1=CC=C2C(CCO2)=C1CNC3=NC=C(C(C=CC=N4)=C4C)C5=NN=CN35.Cl
• Target: Histone Methyltransferase
• Solubility: DMSO:10 mg/mL (24.22 mM);10% DMSO+90% Saline:0.46 mg/mL (1.11 mM)

Bioactivity

• Target IC50:
  H3K27me3 (HeLa cells):1.014 nM
• In Vivo:
  METHODS: To detect anti-tumor activity in vivo, WT G401 or p16 knockout cells were washed and resuspended in cold PBS. The tumor cell mixture was then injected subcutaneously into female Balb/c nude mice. When the tumor volume reached about 60-350 mm, The mice were numbered and randomly assigned to the 100 mg/kg MAK683 treatment group, which was administered at 8 a.m. The mouse body weight and tumor volume were measured and recorded every 3 days. RESULTS MAK683 treatment significantly inhibited the proliferation of female mouse G401 WT or p16 KO cells.
• In Vitro:
  METHODS: Human cervical cancer HeLa cells were treated with MAK683 (1.5-370nM) for 72 hours, and H3K27me3 protein expression was observed by Western Blot experiment. RESULTS MAK683 dose-dependently inhibited H3K27me3 protein expression in HeLa, with an IC50 of approximately 1.014nM.

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

EED, EED inhibitor, embryonic ectoderm development, Inhibitor, Histone Methyltransferase, HistoneMethyltransferase, MAK683 Hydrochloride, MAK-683 Hydrochloride, MAK683 hyrochloride, MAK 683, MAK 683 Hydrochloride, MAK 683 hyrochloride, MAK683, MAK-683, inhibit

Compound Identifiers

PubChem CID

138734886