A p300/CBP inhibitor (IC50 = 60 nM); decreases H3K27Ac levels in PC3 cells; reduces proliferation of various tumor cell lines; inhibits expression of PSA and H3K27Ac occupancy at the PSA enhancer in LNCaP-FGC cells; reduces tumor volume in a LuCaP-77 mouse xenograft model of castration-resistant prostate cancer at 100 mg twice per day for 21 days

A-485 – 5 mg

Brand:
Cayman
CAS:
1889279-16-6
Storage:
-20
UN-No:
Non-Hazardous - /

A-485 is an inhibitor of the histone acetyltransferase p300/CBP (IC50 = 60 nM).{40422} 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. It inhibits expression of prostate specific antigen (PSA) and H3K27Ac occupancy at the PSA enhancer without inhibiting androgen receptor occupancy in LNCaP-FGC cells. A-485 reduces tumor volume in a LuCaP-77 mouse xenograft model of castration-resistant prostate cancer when administered at a dose of 100 mg twice per day for 21 days.  

 

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SKU: 24119 - 5 mg Category:

Description

A p300/CBP inhibitor (IC50 = 60 nM); decreases H3K27Ac levels in PC3 cells; reduces proliferation of various tumor cell lines; inhibits expression of PSA and H3K27Ac occupancy at the PSA enhancer in LNCaP-FGC cells; reduces tumor volume in a LuCaP-77 mouse xenograft model of castration-resistant prostate cancer at 100 mg twice per day for 21 days

Formal name: (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

Synonyms: 

Molecular weight: 536.5

CAS: 1889279-16-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Acetyltransferases||Research Area

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