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Key Documents

208745

Sigma-Aldrich

Calpain Inhibitor VI

The Calpain Inhibitor VI, also referenced under CAS 190274-53-4, controls the biological activity of Calpain. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

동의어(들):

Calpain Inhibitor VI, N-(4-Fluorophenylsulfonyl)-L-valyl-L-leucinal, SJA6017

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About This Item

실험식(Hill 표기법):
C17H25FN2O4S
CAS Number:
Molecular Weight:
372.45
UNSPSC 코드:
12352200
NACRES:
NA.77

Quality Level

분석

≥97% (HPLC)

형태

lyophilized solid

제조업체/상표

Calbiochem®

저장 조건

OK to freeze
protect from light

색상

white

solubility

DMSO: 5 mg/mL

배송 상태

ambient

저장 온도

−20°C

InChI

1S/C17H25FN2O4S/c1-11(2)9-14(10-21)19-17(22)16(12(3)4)20-25(23,24)15-7-5-13(18)6-8-15/h5-8,10-12,14,16,20H,9H2,1-4H3,(H,19,22)

InChI key

WSJWUIDLGZAXID-UHFFFAOYSA-N

일반 설명

A cell-permeable peptide aldehyde that acts as a potent and reversible inhibitor of calpain (IC50 = 7.5 nM for µ-calpain and 78 nM for m-calpain). Also potently inhibits cathepsin B (IC50 = 15 nM) and cathepsin L (IC50 = 1.6 nM). Reduces βFGF-induced angiogenesis in rat cornea and prevents selenite cataract formation in rats. Reduces A23187-induced nuclear opacity and proteolysis of crystallins and α-spectrin in cultured rat lenses.
A potent, cell-permeable, reversible inhibitor of calpain (IC50 = 7.5 nM for µ-calpain and 78 nM for m-calpain). Also potently inhibits cathepsin B (IC50 = 15 nM) and L (IC50 = 1.6 nM). Reduces bFGF-induced angiogenesis in rat cornea and prevents selenite cataract formation. Reduces A23187-induced nuclear opacity and proteolysis of crystallins and α-spectrin in cultured lenses.

생화학적/생리학적 작용

Cell permeable: yes
Primary Target
µ-calpain
Product does not compete with ATP.
Reversible: yes
Target IC50: 7.5 nM for µ-calpain and 78 nM for m-calpain; 15 nM and 1.6 nM against cathepsin B and L, respectively

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

서열

4-Fluorophenylsulfonyl-Val-Leu-CHO

재구성

Following reconstitution, aliquot and freeze at -20°C. Stock solutions are stable for up to 3 months at -20°C.

기타 정보

Inoue, J., et al. 2003. J. Med. Chem.46, 868.
Tamada, Y., et al. 2001. Curr. Eye Res.22, 280.
Mathur, P., et al. 2000. Curr. Eye Res.21, 926.
Nath, R., et al. 2000. Biochem. Biophys. Res. Commun.274, 16.
Tamada, Y., et al. 2000. J. Ocul. Pharmacol. Ther.16, 271.
Fukiage, C., et al. 1998. Curr. Eye Res.17, 623.
Fukiage, C., et al. 1997. Biochim. Biophys. Acta 1361, 304.

법적 정보

Sold under license of U.S. Patent 6,551,999
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Flash Point (°F)

Not applicable

Flash Point (°C)

Not applicable


시험 성적서(COA)

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