MS645

Research use only, not for human use.

MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ).

MS645 (MS-645) is a novel, bivalent bromodomain (BRD) inhibitor with Ki of 18.4 nM for tandem BD1-BD2 (BRD4 BD1/BD2 ), shows12- to 28-fold gain in affinity for binding to the tandem BD1-BD2 over the single BD1 or BD2; shows comparable potency to the tandem BD1-BD2 of BRD2 and BRD3 as to that of BRD4; inhibits the transcription of BRD4 target gene IL-6 in MDA-MB-231 cells with 70% inhibition at 20 nM, much higher than 20-30% inhibition by JQ1 and MS417; potently inhibits cell growth of a panel TNBC with IC50 of 4-20 nM, blocks BRD4 binding to transcription enhancer/mediator proteins MED1 and YY1 with potency superior to monovalent BET inhibitors JQ1.

MS-645;MS 645

Chromatin/Epigenetic

Bromodomain

Bromodomain

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938.05

C48H54Cl2N10O2S2

>98% (HPLC)

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(S)-N,N'-(decane-1,10-diyl)bis(2-((6S)-4-(4-chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f] [1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide)

(-20℃)

With Ice Pack

≥ 2 years