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Chemical Structure : MS645
CAS No.: 2250091-96-2
Catalog No.: PC-35423Not For Human Use, Lab Use Only.
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $128 | In stock | |
| 10 mg | $198 | In stock | |
| 25 mg | $328 | In stock | |
| 50 mg | $548 | In stock | |
| 100 mg | Get quote |
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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.
MS645 shows comparable potency to the tandem BD1-BD2 of BRD2 and BRD3 as to that of BRD4.
MS645 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.
MS645 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.
| M.Wt | 938.048 | |
| Formula | C48H54Cl2N10O2S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(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) |
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1. Ren C, et al. Proc Natl Acad Sci U S A. 2018 Jul 16. pii: 201720000.
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