382113

C646

≥99% (sum of isomers, HPLC), solid, histone acetyltransferase p300 inhibitor, Calbiochem^®

• 別名: Histone Acetyltransferase p300 Inhibitor, C646, 4-(4-{[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene}-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid, p300/CBP Inhibitor IV, Histone Acetyltransferase Inhibitor V, HAT Inhibitor V
• 実験式（ヒル表記法）: C₂₄H₁₉N₃O₆
• CAS番号: 328968-36-1
• 分子量: 445.42
• MDL番号: MFCD01784780
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• product name: Histone Acetyltransferase p300 Inhibitor, C646, Histone Acetyltransferase p300 Inhibitor, C646, CAS 328968-36-1, is a cell-permeable, reversible inhibitor of p300/CBP HAT (Ki = 400 nM). Competes with acetyl-CoA for the p300 Lys-CoA binding pocket.
• 品質水準: 100
• アッセイ: ≥99% (sum of isomers, HPLC)
• 形状: solid
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: brick red
• 溶解性: DMSO: 50 mg/mL
• 輸送温度: ambient
• 保管温度: −20°C
• InChI: 1S/C24H19N3O6/c1-13-10-20(21(27(31)32)11-14(13)2)22-9-8-18(33-22)12-19-15(3)25-26(23(19)28)17-6-4-16(5-7-17)24(29)30/h4-12H,1-3H3,(H,29,30)/b19-12-
• InChI Key: HEKJYZZSCQBJGB-UNOMPAQXSA-N

詳細

詳細

A reversible, cell-permeable pyrazolone p300/CBP HAT inhibitor (K_i = 400 nM), which competes with acetyl-CoA for the p300 Lys-CoA binding pocket. This compound demonstrates 86% inhibition against p300 at 10 nM, but elicits less than 10% inhibition against serotonin N-acetyltransferase, PCAF histone acetyltransferase, GCN5 histone acetyletransferase, Rtt109 histone acetyletransferase, Sas histone acetyl transferase, and MOZ histone acetyltransferase in a chemical screening assay. Treatment of C3H 10T1/2 mouse fibroblasts with 25 µM of compound results in an inhibitory effect against basal and TSA-inducible acetylation of histones H3 and H4. It is also shown to inhibit human cell growth in both melanoma and non-small-cell-lung (NSCL) cancer cell lines at 10 µM with similar or higher potency compared with that of the peptide-based bisubstrate p300/CBP HAT inhibitor Lys-CoA-Tat at 25 µM.

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C. Stock solutions are stable for up to 3 months at -20°C.

その他情報

Bowers, EM., et al. 2010. Chem Biol17, 471.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable