382113
C646
≥99% (sum of isomers, HPLC), solid, histone acetyltransferase p300 inhibitor, Calbiochem®
别名:
组蛋白乙酰转移酶p300抑制剂，C646, 4-(4-{[5-(4,5-二甲基-2-硝基苯基)呋喃-2-基]亚甲基}-3-methyl-5-氧代-4,5-二氢-1H-吡唑-1-氧)苯甲酸，p300/CBP抑制剂IV，组蛋白乙酰转移酶抑制剂V，HAT抑制剂V
Product Name
组蛋白乙酰转移酶p300抑制剂，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.
质量水平
方案
≥99% (sum of isomers, HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
brick red
溶解性
DMSO: 50 mg/mL
运输
ambient
储存温度
−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
相关类别
一般描述
一种可逆、细胞可渗透吡唑啉酮p300/CBP HAT抑制剂（Ki = 400 nM），可与乙酰辅酶A竞争p300 Lys-CoA结合袋。该化合物在10 nM处对p300有86%的抑制作用，但在化学筛选测定中对羟色胺N-乙酰转移酶、PCAF组蛋白乙酰转移酶、GCN5组蛋白乙酰转移酶、Rtt109组蛋白乙酰转移酶、Sas组蛋白乙酰转移酶以及MOZ组蛋白乙酰转移酶的抑制作用均小于10%。使用25µ M化合物处理C3H 10T1/2小鼠成纤维细胞可对组蛋白H3和H4的基础和TSA诱导乙酰化产生抑制效果。研究还表明，与25 µM基于多肽双底物p300/CBP HAT抑制剂Lys-CoA-Tat相比，10µM时可抑制黑色素瘤和非小细胞肺（NSCL）癌细胞系中人类细胞生长，并且具有相似或更高的药效。
包装
用惰性气体包装
制备说明
复溶后，分装并冷冻保存（-20°C。储备液在-20°C条件下可稳定保存3个月。
其他说明
Bowers, EM., et al. 2010.Chem Biol17, 471.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
毒性：标准处理（A）
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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