MS37452

SKU: orb1940433

Description

MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 μM).

Key Properties

• CAS Number: 423748-02-1
• MW: 398.459
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₆N₂O₅
• SMILES: COc1cccc(C(=O)N2CCN(CC2)C(=O)COc2cccc(C)c2)c1OC
• Target: Parasite|MmpL3
• Solubility: In Vitro: DMSO : 100 mg/mL (250.97 mM)

Bioactivity

• In Vitro:
  MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control. MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus. MS37452 (200 μM; 5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment. MS37452 (200 μM; 5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy. RT-PCR Cell line: PC3 cells. Concentration: 125-500 μM. Incubation time: 12 hours. Result: Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively. Cell Viability Assay Cell line: Glioblastoma multiforme (GBM) U118MG cells. Concentration: PRT4165 40 μM, PTC209 200 nM, DZnep 25 μM, GSK343 400 nM, MS37452 200 μM, Doxorubicin 200 nM, temozolomide 50 μM, SAHA 1 μM. Incubation time: 5 days. Result: Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Parasite|MmpL3