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A-485

CAS No. : 1889279-16-6

MCE 站：A-485

产品活性：A-485 是 p300/CBP 的强效选择性催化抑制剂，对 p300 和 CBP 组蛋白乙酰转移酶 (HAT) 的 IC₅₀ 值分别为 9.8 nM 和 2.6 nM。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain  |  Histone Acetyltransferase

In Vitro: A three-hour treatment of prostate adenocarcinoma PC-3 cells with A-485 results in a dose-dependent decrease in H3K27Ac, with a half maximal effective concentration (EC₅₀) of 73 nM. Treatment with A-485 does not alter p300 or CBP protein levels.
The broadest sensitivity is observed in haematological tumours, where A-485 exhibits potent activity in most multiple myeloma cell lines, and in a subset of acute myeloid leukaemia lines and non-Hodgkin’s lymphoma lines. A-485 induces a comparable decrease in H3K27Ac in all five prostate cancer cell lines.

In Vivo: After tumours are established in SCID male mice, twice daily intraperitoneal injections of A-485 induce 54% tumour growth inhibition after 21 days of dosing (P<0.005 as compare to vehicle control). In addition, in tumour-bearing animals, dosing with A-485 for seven days induces a decrease in the mRNA levels of MYC and the AR-dependent gene SLC45A3 at three hours post-dosing, and (for MYC) a decrease in the protein level, indicating that A-485 inhibits p300-mediated transcriptional activity in vivo. However, at 16?hours post-dosing on the seventh day, A-485 drug levels in the plasma and tumour are decreased as compare to 3?hours. A-485 induces a moderate 9% body weight loss, and the animals recover rapidly upon completion of the A-485 dosing regimen.

相关产品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  Covalent Screening Library  |  Reprogramming Compound Library  |  Chemical Probe Library  |  Anti-Blood Cancer Compound Library  |  Acetaminophen  |  Curcumin  |  Birabresib  |  C646  |  JQ-1 (carboxylic acid)  |  Anacardic Acid  |  I-BET151  |  SGC-CBP30  |  MG 149  |  KG-501  |  A-366  |  NSC 228155  |  CPI-203  |  Garcinol  |  PFI-1  |  IACS-9571 hydrochloride  |  ACBI1  |  CPTH2  |  GSK2801  |  MI-3  |  (+)-JQ1 PA  |  Histone Acetyltransferase Inhibitor II  |  SGC-iMLLT  |  PF-CBP1 hydrochloride  |  Bromosporine  |  EML 425  |  L002  |  YF-2  |  MS436  |  GSK1379725A

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