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A-485

A potent HAT inhibitor
Catalog #: B2601
SKU-Size Size Price Qty
B2601-1 1 mg
$75.00
B2601-5 5 mg
$275.00
More Sizes Get Quote

Product Details

Alternate Name 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
Peptide Sequence N/A
Appearance White solid
CAS # 1889279-16-6
Molecular Formula C₂₅H₂₄F₄N₄O₅
Molecular Weight 536.48
Purity ≥98% by HPLC
Solubility >40 mg/ml in DMSO
>40 mg/ml in Ethanol
SMILES O=C(NC)NC1=CC=C2C(CC[[email protected]]23C(N(CC(N(CC4=CC=C(F)C=C4)[[email protected]@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
PubChem CID 118958122
Handling Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.
Storage Conditions -20ºC
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

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.


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