A-485

SKU: orb1308704

Description

A-485 is a potent and selective small molecule inhibitor of the p300 and CBP histone acetyltransferases, with IC50 values of 9.8 nM and 2.6 nM, respectively. It has demonstrated antitumor activity in preclinical studies, including models of hematologic cancers and androgen receptor-positive prostate cancer, in both cellular and animal experiments.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1889279-16-6
• MW: 536.48
• Purity: >99.99% (May vary between batches)
• Formula: C₂₅H₂₄F₄N₄O₅
• SMILES: CNC(=O)Nc1ccc2c(CC[C@@]22OC(=O)N(CC(=O)N(Cc3ccc(F)cc3)[C@@H](C)C(F)(F)F)C2=O)c1
• Target: Histone Acetyltransferase,Epigenetic Reader Domain
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.32 mM);DMSO:252.5 mg/mL (470.66 mM)

Bioactivity

• Target IC50:
  p300:9.8 nM|CBP:2.6 nM
• In Vivo:
  METHODS: To assay in vivo anti-tumor activity, A-485 (100 mg/kg) was administered intraperitoneally twice daily for 21 days to SCID mice bearing LuCaP-77 CR xenografts. RESULTS: A-485 induced 54% tumor growth inhibition (TGI) after 21 days of administration.
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• In Vitro:
  METHODS: 124 tumor cells were treated with A-485 for 3-5 days and cell viability was measured by the CellTiter-Glo Luminescent Cell Viability Assay. RESULTS: The broadest sensitivity was observed in hematologic tumors, where A-485 exhibited potent activity in most multiple myeloma (MM) cell lines, acute myeloid leukemia (AML) cell lines, and non-Hodgkin's lymphoma (NHL) cell lines. In contrast, several solid tumor lines, including melanoma, small cell lung cancer (SCLC), and triple-negative breast cancer (TNBC), showed significantly reduced sensitivity to A-485. METHODS: H1650 and H1650-ER cells were treated with A-485 (20 µM) overnight, followed by TRAIL (10-100 ng/mL) overnight, and apoptosis was detected by apoptotic kit. RESULTS: The combination of A-485 and TRAIL significantly increased the total number of apoptotic cells in H1650 and H1650-ER cells compared to TRAIL alone.A-485 enhanced TRAIL-induced apoptosis.
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Storage & Handling

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

Alternative Names

CBP, CBP/p300, A485, A-485, A 485, Inhibitor, histone acetyltransferase, Histone Acetyltransferase, HistoneAcetyltransferase, HAT, HATs, Epigenetic Reader Domain, EpigeneticReaderDomain, inhibit, p300

Compound Identifiers

PubChem CID

118958122