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经验公式(希尔记法):
C20H31N5O10
化学文摘社编号:
分子量:
501.49
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
color
white
solubility
water: 1 mg/mL, DMSO: 5 mg/mL
InChI key
XZGUQURUQBIHMG-XUXIUFHCSA-N
SMILES string
N([C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C=O)C(=O)[C@@H](NC(=O)[C@@H](NC(=O)C)CC(=O)O)CC(=O)N
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
shipped in
ambient
storage temp.
−20°C
Quality Level
General description
A tetrapeptidyl aldehyde that acts as a potent, reversible and active site binding inhibitor of caspases-3 and -7 (IC50 = 3.2 nM and 22.6 nM, respectively) and displays ~100-fold greater selectivity over caspases-8 and -9 (IC50 = 577.6 nM and 364.7 nM, respectively). Offers protection against Camptothecin (Cat. No. 208925), and anti-Fas-mediated apoptosis in Jurkat T cells.
Note: aldehyde-based inhibitors are less cell-permeable than FMK-based inhibitors, so higher concentrations may be required for cell-based inhibition studies (e.g. 100 µM).
Note: aldehyde-based inhibitors are less cell-permeable than FMK-based inhibitors, so higher concentrations may be required for cell-based inhibition studies (e.g. 100 µM).
Biochem/physiol Actions
Cell permeable: no
Primary Target
caspase-3, caspase-7
caspase-3, caspase-7
Product does not compete with ATP.
Reversible: yes
Target IC50: 3.2 nM and 22.6 nM, against caspases-3 and -7, respectively
Packaging
Packaged under inert gas
Analysis Note
Single main spot with additional trace spot by TLC
Other Notes
Ac-Asp-Asn-Leu-Asp-CHO
Yoshimori, A., et al. 2004. BMC Pharmacol.4, 7.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Kamila Říhová et al.
Journal of proteome research, 23(8), 2999-3011 (2024-03-19)
Caspase-9 is traditionally considered the initiator caspase of the intrinsic apoptotic pathway. In the past decade, however, other functions beyond initiation/execution of cell death have been described including cell type-dependent regulation of proliferation, differentiation/maturation, mitochondrial, and endosomal/lysosomal homeostasis. As previous
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