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重要文件

382113

Sigma-Aldrich

C646

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

同義詞:

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

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About This Item

經驗公式(希爾表示法):
C24H19N3O6
CAS號碼:
分子量::
445.42
MDL號碼:
分類程式碼代碼:
12352200
NACRES:
NA.77

產品名稱

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.

品質等級

化驗

≥99% (sum of isomers, HPLC)

形狀

solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze
protect from light

顏色

brick red

溶解度

DMSO: 50 mg/mL

運輸包裝

ambient

儲存溫度

−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 密鑰

HEKJYZZSCQBJGB-UNOMPAQXSA-N

一般說明

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。

包裝

用惰性气体包装

警告

毒性:标准处理(A)

重構

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。

其他說明

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

法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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