MS37452 |
Catalog No.GC12630 |
MS37452는 27.7μM의 Kd로 H3K27me3에 결합하는 CBX7 크로모도메인의 강력한 억제제입니다. MS37452는 전립선암 세포에서 INK4A/ARF 유전자좌에 대한 CBX7 결합을 대체함으로써 폴리콤 억제 복합 표적 유전자 p16/CDKN2A의 전사를 억제할 수 있습니다.
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Cas No.: 423748-02-1
Sample solution is provided at 25 µL, 10mM.
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 [1].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Ren, C. ,Morohashi, K.,Plotnikov, A.N., et al. Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chemistry & Biology 22, 161-168 (2015).
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