A-485 | B2601

A-485 is a potent and selective p300/CREB-binding protein (CBP) HAT domain inhibitor (IC₅₀ values are 2.6 and 9.8 nM for the CBP-bromodomain HAT-C/H3 (BHC) and p300-BHC domains, respectively). A-485 displays > 1000-fold selectivity over closely related HATs. It decreases acetylated histone H3 lysine 27 (H3K27Ac), but not H3K9Ac, levels in PC3 cells in a concentration-dependent manner. A-485 reduces proliferation of non-small cell lung cancer (NSCLC), small cell lung cancer, triple-negative breast cancer, mantel cell lymphoma, multiple myeloma, non-Hodgkin's, and acute myeloid leukemia cell lines.

A-485 is a potent and selective p300/CREB-binding protein (CBP) HAT domain inhibitor (IC₅₀ values are 2.6 and 9.8 nM for the CBP-bromodomain HAT-C/H3 (BHC) and p300-BHC domains, respectively). A-485 displays > 1000-fold selectivity over closely related HATs. It decreases acetylated histone H3 lysine 27 (H3K27Ac), but not H3K9Ac, levels in PC3 cells in a concentration-dependent manner. A-485 reduces proliferation of non-small cell lung cancer (NSCLC), small cell lung cancer, triple-negative breast cancer, mantel cell lymphoma, multiple myeloma, non-Hodgkin's, and acute myeloid leukemia cell lines.

B2601 | A-485 DataSheet

Alternate Name/Synonyms: A485, (1R)-N-[(4-Fluorophenyl)methyl]-2,3-dihydro-5-[[(methylamino)carbonyl]amino]-2',4'-dioxo-N-[(1S)-2,2,2-trifluoro-1-methylethyl]spiro[1H-indene-1,5'-oxazolidine]-3'-acetamide

Appearance: White solid

Formulation:

CAS Number: 1889279-16-6

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₅H₂₄F₄N₄O₅

Molecular Weight: 536.48

Cell-Permeable?: True

Purity: ≥98% by HPLC

Solubilities: >40 mg/ml in DMSO, >40 mg/ml in Ethanol

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A potent HAT inhibitor

MDL Number:

PubChem CID: 118958122

SMILES: O=C(NC)NC1=CC=C2C(CC[C@]23C(N(CC(N(CC4=CC=C(F)C=C4)[C@@H](C)C(F)(F)F)=O)C(O3)=O)=O)=C1

InChi: InChI=1S/C25H24F4N4O5/c1-14(25(27,28)29)32(12-15-3-5-17(26)6-4-15)20(34)13-33-21(35)24(38-23(33)37)10-9-16-11-18(7-8-19(16)24)31-22(36)30-2/h3-8,11,14H,9-10,12-13H2,1-2H3,(H2,30,31,36)/t14?,24-/m1/s1

InChi Key: VRVJKILQRBSEAG-PYFQUHSISA-N