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506282

Sigma-Aldrich

Cl-amidine

>95% (HPLC), solid, PAD inhibitor, Calbiochem®

别名:

PAD抑制剂,Cl-amidine, N-α-苯甲酰基-N5-(2-氯-1-亚氨基乙基)-L-鸟酰胺

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About This Item

经验公式(希尔记法):
C16H20ClF3N4O4
分子量:
424.80
分類程式碼代碼:
12352200
NACRES:
NA.77

product name

PAD抑制剂,Cl-amidine, Cl-amidine is a cell-permeable pan PAD inhibitor (IC₅₀ = 0.8, 6.2, and 5.9 µM for PAD1, PAD3, and PAD4, respectively). Inactivates the calcium bound form of PAD4 in an irreversible manner.

品質等級

化驗

>95% (HPLC)

形狀

solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze

顏色

white

溶解度

DMSO: 50 mg/mL

運輸包裝

ambient

儲存溫度

−20°C

一般說明

一种可渗透细胞的化合物,在酶法测定中充当pan PAD抑制剂(PAD1,PAD3和PAD4的IC50分别为0.8µ M,6.2 µM和5.9 µM)。它以不可逆的方式优先灭活PAD4的钙结合形式,并显示与BAEE一起完成了该酶的活性位点残基。在体内,用浓度在25 µM至200 µM之间的Cl-amidine处理的瞬时转染的CV-1细胞中观察到p300GDB-GRIP1相互作用的效率有小幅但显著的降低。此外,该化合物(200 µM)与HDAC抑制剂SAHA(0.4 µM)一起显示出在U2OS细胞中以p53依赖性方式诱导p21,GADD45和PUMA表达并抑制癌细胞生长的累加作用。

警告

毒性:监管审查(Z)

重構

复溶后,等分并冷冻保存(-20°C)。贮备液在-20°C下可稳定保存至多3个月。

其他說明

Knuckley, B., et al. 2010.Biochemistry23, 4852.
Li, P., et al. 2010.Oncogene21, 3153.
Luo, Y., et al. 2006.Biochemistry39, 11727.

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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