NI-57

SKU: orb1296217

Description

NI-57 is a potent small molecule inhibitor targeting the BRPF family of proteins, exhibiting IC50 values of 3.1 nM for BRPF1, 46 nM for BRPF2/BRD1, and 140 nM for BRPF3. This compound is a valuable chemical probe for epigenetic research, enabling the investigation of BRPF function in chromatin regulation and gene expression in both cellular and biochemical assays.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1883548-89-7
• MW: 383.42
• Purity: >99.99% (May vary between batches)
• Formula: C₁₉H₁₇N₃O₄S
• SMILES: COc1cc(ccc1S(=O)(=O)Nc1ccc2n(C)c(=O)c(C)cc2c1)C#N
• Target: Epigenetic Reader Domain
• Solubility: DMSO:80 mg/mL (208.65 mM);10% DMSO+90% Corn Oil:3.3 mg/mL (8.61 mM)

Bioactivity

• Target IC50:
  BRPF2 BRD1:46 nM|BRPF3:140 nM|BRPF1:3.1 nM
• In Vitro:
  NI-57 binds the BRD of BRPF1 with a Kd of 31 nM, BRD1 with a Kd of 110 nM, and BRPF3 with a Kd of 410 nM, whereas binding to BRD9 is weaker (Kd 1000 nM) measured by isothermal titration calorimetry. NI-57 shows less active effect on BRD9 (IC50, 520 nM) and BRD4 (BD1) (IC50, 3700 nM), TRIM24 (IC50, 1600 nM). NI-57 also inhibits BRPF BRDs in the nucleus but shows little effect on the proliferation of many cancer cell lines with GI50s of 10.4 μM (NCI-H1703 cells), 14.7 μM (DMS114), 15.6 μM (HRA-19), and 16.6 μM (RERF-LC-Sq1). Furthermore, Inhibition on BRPF1 of NI-57 (10 μM) reduces the gene expression of CCL-22 by 27.7%.
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Storage & Handling

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

Alternative Names

BRPF1, BRPF2, BRPF3, inhibit, Inhibitor, NI 57, NI57, NI-57, EpigeneticReaderDomain, Epigenetic Reader Domain

Compound Identifiers

PubChem CID

91827373