218833
Caspase-6 Inhibitor XII, pep419
The Caspase-6 Inhibitor XII, pep419 controls the biological activity of Caspase-6. This small molecule/inhibitor is primarily used for Cancer applications.
别名:
Caspase-6 Inhibitor XII, pep419, Caspase inhibitor, pep419
质量水平
方案
≥95% (HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
water: 100 mg/mL
运输
ambient
储存温度
−20°C
一般描述
An 18-mer synthetic peptide that acts as a selective, non-competitive inhibitor of caspase-6 (IC50 = 8.6 µM). Blocks the activity of processed caspase-6 as evidenced by its reduced ability to process VEID-AMC substrate. Exhibits only a trivial effect on caspase-9 and 7 and does not affect the activities of caspases 1, 2, 3, 4, 5, 8, and 10. Acts as an allosteric peptide ligand that binds outside the active site of the enzyme and impairs its activity. Pep419 is shown to bind as a dimer to an allosteric site of caspase-6 zymogen resulting in its tetramerizaton and stabilization. Its binding site is shown to be distinct from the substrate binding site of the enzyme. Electroporation has been shown to enable the entry of 5-carboxyfluorescein-labeled peptide into SKNAS bone marrow neuroblastoma cells.
包装
Packaged under inert gas
其他说明
Ac-TEKEKGRLHCVEWTILER-NH2
Stanger, K., et al. 2012. Nat. Chem. Bio.8, 655.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Karen Stanger et al.
Nature chemical biology, 8(7), 655-660 (2012-06-12)
The caspases are a family of cytosolic proteases with essential roles in inflammation and apoptosis. Drug discovery efforts have focused on developing molecules directed against the active sites of caspases, but this approach has proved challenging and has not yielded
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