Catalog No. Size PriceQuantity
M22465-C Contact for quotation $100Unavailable


Ki = 43 μM MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3. Chromobox homolog 7 (CBX7) functions via its N-terminal chromodomain, which recognizes histone 3 trimethyl lysine 27 (H3K27me3), to repress gene transcription. Chromobox homolog 7 plays a critical role in gene transcription in cellular processes associated with stem cell differentiation and self-renewal, as well as tumor progression. In vitro: In a previous study, the crystal structures revealed the binding modes of MS37452 and its close analogs that competed against H3K27me3 binding via interactions with key residues in the methyl-lysine binding pocket of CBX7ChD. It was further found that MS37452 as the lead compound was able to derepress the transcription of Polycomb repressive complex target gene p16/CDKN2A through displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells. These findings showed that MS37452 and its close analogs had the potential to be developed into high-potency chemical modulators targeting CBX7 functions in gene transcription in various disease pathways . In vivo: Up to now, there is no animal in vivo data reported. Clinical trial: So far, no clinical study has been conducted.

Product information

CAS Number: 423748-02-1

Molecular Weight: 398.45

Formula: C22H26N2O5

Chemical Name: 1-[4-(2,3-dimethoxybenzoyl)piperazin-1-yl]-2-(3-methylphenoxy)ethan-1-one

Smiles: CC1C=C(C=CC=1)OCC(=O)N1CCN(CC1)C(=O)C1C=CC=C(OC)C=1OC


InChi: InChI=1S/C22H26N2O5/c1-16-6-4-7-17(14-16)29-15-20(25)23-10-12-24(13-11-23)22(26)18-8-5-9-19(27-2)21(18)28-3/h4-9,14H,10-13,15H2,1-3H3

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

Products are for research use only. Not for human use.

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