product name MS436
Description: MS436 is a potent and selective BET bromodomain inhibitor with Ki of <0.085 μM and 0.34 μM for BRD4 (1) and BRD4 (2), respectively. MS436 effectively inhibits BRD4 activity in NF-κB-directed production of nitric oxide and proinflammatory cytokine interleukin-6 in murine macrophages. MS436 represents a new class of bromodomain inhibitors and will facilitate further investigation of the biological functions of the two bromodomains of BRD4 in gene expression.
References: J Med Chem. 2013 Nov 27;56(22):9251-64.
383.42
Formula
C18H17N5O3S
CAS No.
1395084-25-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 55 mg/mL (143.4 mM)
Water: <1 mg/mL
Ethanol: 1 mg/mL (2.6 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19419726
| In Vitro |
In vitro activity: As a chemical probe for BRPF bromodomains, OF-1 increases thermal stability in the cellular thermal shift assay of full length BRPF1B at 1 μM and also demonstrates accelerated FRAP recovery at 5 μM in the BRPF2 FRAP assay. In addition, OF-1 shows modest general cytotoxicity. Kinase Assay: Cell Assay: |
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| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | J Med Chem. 2013 Nov 27;56(22):9251-64. |
