MS37452 - 10mM in DMSO , CAS No.423748-02-1

CAS: 423748-02-1 Cat. No.: M655277 Molecular Weight: 398.45 PubChem CID: 1072048

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3 , with a K d of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell 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 AssayCell 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.

IC50& Target:CBX7

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3 , with a K d of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• Isomeric SMILES: CC1=CC(=CC=C1)OCC(=O)N2CCN(CC2)C(=O)C3=C(C(=CC=C3)OC)OC
• PubChem CID: 1072048
• Molecular Weight: 398.45