MS8511 HCl

SKU: orb1945018

Description

MS8511 HCl is a selective, covalent inhibitor of the histone methyltransferases G9a and GLP, which it inactivates by targeting catalytic cysteines. This tool compound potently diminishes intracellular H3K9me2 levels and demonstrates antiproliferative effects, supporting its use in cancer research for models including brain, breast, and ovarian malignancies.

Research Area

Epigenetics & Chromatin

Key Properties

• MW: 532.12
• Purity: 98.96% (May vary between batches)
• Formula: C₂₈H₄₂ClN₅O₃
• SMILES: O=C(NC1=CC(NC2CCN(C(C)C)CC2)=C3C=C(OC)C(OCCCN4CCCC4)=CC3=N1)C=C.Cl
• Target: Histone Methyltransferase

Bioactivity

• Target IC50:
  G9a:44 nM (Kd)|G9a:100 nM|GLP:140 nM|GLP:46 nM (Kd)
• In Vitro:
  MS8511 HCl (Compound 8), within a range of 0-100 μM over 10 minutes, selectively inhibits G9a and GLP compared to other PKMTs and PRMTs, with IC50 values of 100 nM (G9a) and 140 nM (GLP) .With a duration of 50 minutes, MS8511 HCl exhibits a preference for covalent modification of G9a over GLP, with Kd values of 44 nM (G9a) and 46 nM (GLP) .Over a range of 0-5 μM and durations of 24-72 hours,MS8511 HCl effectively reduces the H3K9me2 mark in MDA-MB-231 and K562 cells . At concentrations ranging from 0.8 to 25 μM over a period of 3 days, MS8511 HCl inhibits the growth of MDA-MB-231 cells .
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Storage & Handling

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

Alternative Names

MS8511 HCl(2866408-21-9 Free base), MS8511HCl(2866408219Freebase), HistoneMethyltransferase, Histone Methyltransferase, G9a/GLP

Compound Identifiers

PubChem CID

171360694