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产品名称
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.
质量水平
方案
>95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
white
溶解性
DMSO: 50 mg/mL
运输
ambient
储存温度
−20°C
一般描述
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）
重悬
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。
其他说明
Knuckley, B., et al. 2010.Biochemistry23, 4852.
Li, P., et al. 2010.Oncogene21, 3153.
Luo, Y., et al. 2006.Biochemistry39, 11727.
Li, P., et al. 2010.Oncogene21, 3153.
Luo, Y., et al. 2006.Biochemistry39, 11727.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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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