MS37452 |
Catalog No.GC12630 |
MS37452 es un potente inhibidor de la uniÓn del cromodominio CBX7 a H3K27me3, con una Kd de 27,7 μM. MS37452 puede desreprimir la transcripciÓn del gen objetivo p16/CDKN2A del complejo represivo Polycomb al desplazar la uniÓn de CBX7 al locus INK4A/ARF en células de cÁncer de prÓstata.
Products are for research use only. Not for human use. We do not sell to patients.
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).
Average Rating: 5
(Based on Reviews and 17 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *