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Merck
CN

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.

Synonym(s):

Caspase-6 Inhibitor XII, pep419, Caspase inhibitor, pep419

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About This Item

Empirical Formula (Hill Notation):
C99H162N30O29S
Molecular Weight:
2268.59
UNSPSC Code:
12352200

Key Documents

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Product Name

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.

assay

≥95% (HPLC)

form

powder

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

water: 100 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

100

Disclaimer

Toxicity: Standard Handling (A)

General description

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.

Other Notes

Ac-TEKEKGRLHCVEWTILER-NH2
Stanger, K., et al. 2012. Nat. Chem. Bio.8, 655.

Packaging

Packaged under inert gas

Legal Information

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

Storage Class

11 - Combustible Solids

wgk

WGK 1

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

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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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