MS436

SKU: orb1226371

Description

MS436 is a diazobenzene-based small-molecule inhibitor for the BRD4 bromodomains with a Ki value of 30-50 nM.

Key Properties

• CAS Number: 1395084-25-9
• MW: 383.42
• Purity: >98% (HPLC)
• Formula: C₁₈H₁₇N₅O₃S
• SMILES: O=S(C1=CC=C(/N=N/C2=CC(C)=C(O)C=C2N)C=C1)(NC3=NC=CC=C3)=O
• Target: Epigenetic Reader Domain
• Solubility: Ethanol: 1 mg/mL warmed (2.6 mM); DMSO: 55 mg/mL (143.44 mM)

Bioactivity

• In Vitro:
  MS436, through a set of water-mediated interactions, exhibits low nanomolar affinity (estimated Ki of 30-50 nM) with preference for the first bromodomain over the second. MS436 effectively inhibits BRD4 activity in NF-κB-directed production of NO and pro-inflammatory 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. MS436 exhibits potent affinity of an estimated Ki=30-50 nM for the BRD4 BrD1 and a 10-fold selectivity over the BrD2, which is achieved through a unique set of water-mediated intermolecular interactions.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MS436 | MS-436 | MS 436

Quick Database Links

Gene Symbol

Epigenetic Reader Domain