OF-1 |
| カタログ番号GC17482 |
OF-1 は強力な汎 BRPF ブロモドメイン (BRD) 阻害剤であり、IC50 値は TRIM24 と BRPF1B でそれぞれ 270 nM、1.2 μM です。
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Cas No.: 919973-83-4
Sample solution is provided at 25 µL, 10mM.
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OF-1 is a selective BRPF1B and BRPF2 bromodomain inhibitor (Kd value = 100nM and 500 nM, respectively; >100-fold selectivity over majority of other bromodomains).
BRPF (BRomodomain and PHD Finger containing) protein family are scaffolding proteins that assembles MYST histone acetyltransferase complexes. MYST complexes play important role in DNA repair, recombination, replication and transcription activation.
In cellular thermal shift assay (CETSA) of full length BRPF1B, OF-1 enhanced thermal stability at 1 µM. In BRPF2 FRAP assay, OF-1 showed accelerated FRAP recovery at 5µM. OF-1 exhibited modest general cytotoxicity.
References:
[1]. OF-1 - A chemical probe for BRPF bromodomains. (2010, October 13). SGC. Retrieved from http://www.thesgc.org/chemical-probes/OF-1
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