| 名称 | A-485 |
| 描述 | A-485 is a potent and selective catalytic p300/CBP inhibitor with IC50 values of 9.8 nM for p300 and 2.6 nM for CBP. |
| 体外活性 | 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. [1]
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. [2] |
| 体内活性 | 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. [1] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 60 mg/mL (111.84 mM), Sonication is recommended.
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| 关键字 | inhibit | HATs | Inhibitor | Epigenetic Reader Domain | A485 | Histone Acetyltransferase | HAT | A-485 | A 485 |
| 相关产品 | ABBV-744 | CeMMEC1 | 3-methyl-1,2,3,4-tetrahydroquinazolin-2-one | (+)-JQ-1 | J-147 | Anacardic Acid | Acetaminophen | Curcumin | dBET6 | Piflufolastat | Naphthol AS-E | Bisdemethoxycurcumin |
| 相关库 | 细胞重编程化合物库 | 经典已知活性库 | 抑制剂库 | 抗心血管疾病化合物库 | NO PAINS 化合物库 | 干细胞分化化合物库 | PPI抑制剂库 | 已知活性化合物库 | 共价抑制剂库 | 抗高血压化合物库 |
United States
