An inhibitor of CBX7 chromodomain binding to H3K27me3
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MS37452

Item No. 17533

Technical Information
Formal Name
1-[4-(2,3-dimethoxybenzoyl)-1-piperazinyl]-2-(3-methylphenoxy)-ethanone
CAS Number
423748-02-1
Molecular Formula
C22H26N2O5
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlEthanol:PBS(pH 7.2) (1:1): 0.5 mg/ml
SMILES
COC1=CC=CC(C(N2CCN(C(COC3=CC(C)=CC=C3)=O)CC2)=O)=C1OC
InChi Code
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
InChi Key
LUMCNRKHZRYQOV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Chromobox homolog 7 (CBX7) functions through its N-terminal chromodomain, which recognizes histone 3 trimethyl lysine 27 (H3K27me3), to repress gene transcription. It plays a key role in gene transcription in cellular processes related to stem cell self-renewal and differentiation, as well as tumor progression.1 MS37452 is a competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 µM).1 At 250 µM, it has been shown to derepress transcription of the polycomb repressive complex target gene p16/CDKN2A in prostate cancer cells.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ren, C., Morohashi, K., Plotnikov, A.N., et alSmall-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chem. Biol. 22, 161-168 (2015).