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Inhibitor SourceBook™ Second Edition

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Proteases<br />

Calpain <strong>Inhibitor</strong>s, continued<br />

Product Cat. No. Comments Size Price<br />

EST 330005 [E-64d; (2S,3S)-trans-Epoxysuccinyl-L-leucylamido-3-methylbutane Ethyl<br />

Ester; Loxistatin]<br />

A cell-permeable, irreversible inhibitor of cysteine proteases that is<br />

reported to block the action of calpain I. Its action is similar to E-64<br />

(Cat. No. 324890); however, it is devoid of charged groups.<br />

mg $96<br />

PD 45305 513021 A useful negative control for the calpain inhibitors PD 50606<br />

(Cat. No. 5 3022) and PD 5 746 (Cat. No. 5 3024).<br />

mg $99<br />

5 mg $94<br />

PD 50606 513022 [3-(4-Iodophenyl)-2-mercapto-(Z)-2-propenoic Acid]<br />

A cell-permeable, selective non-peptide calpain inhibitor (K i = 2 0 nM<br />

for calpain I and 370 nM for calpain II) directed towards the calcium<br />

binding sites of calpain.<br />

PD 5 746 513024 [3-(5-Fluoro-3-indolyl)-2-mercapto-(Z)-2-propenoic Acid]<br />

A cell-permeable, non-peptidic, and highly selective calpain inhibitor<br />

that displays over 20-fold greater selectivity for calpain I (K = 260 nM)<br />

i<br />

over calpain II (K = 5.33 mM).<br />

i<br />

Calpain <strong>Inhibitor</strong> Set 208733 Provided as a 5 vial set. Each set contains 5 mg ALLN (Cat. No. 2087 9);<br />

25 mg Calpain <strong>Inhibitor</strong> III (Cat. No. 208722); 5 mg of Calpeptin (Cat.<br />

No. 03-34-005 ); mg of EST (Cat. No. 330005); and 5 mg of PD<br />

50606 (Cat. No. 5 3022).<br />

Related Products<br />

Calpain-1 Substrate II, Fluorogenic<br />

An internally quenched peptide substrate that is optimized for calpainamino<br />

acid recognition motifs at the primed as well as the nonprimed<br />

sides.<br />

Cat. No. 208772 1 mg $180<br />

Calpain Substrate III, Fluorogenic<br />

A fluorogenic FRET peptide with a substrate sequence that is optimized<br />

for calpain- and -2 (Cat. Nos. 2087 2, 2087 3, 2087 5, and 2087 8)<br />

based on 06 known cleavage sites. It is cleaved by mammalian<br />

calpains with a much better efficacy (k cat /K mx 0 -2 M - s - ) = 69.8,<br />

38.5, 20.0, 6.8 , 3.58, 0.05, and < 0.05 for calpain-2, trypsin, papain,<br />

calpain-B, calpain-A, chymotrypsin, and cathepsin-B, respectively)<br />

and kinetically superior to other commonly used calpain substrates,<br />

such as LY-AMC (Cat. No. 20873 ) and a-spectrin cleavage site-based<br />

substrate (Cat. No. 208748). Has been used successfully in monitoring<br />

calpain activity in whole Drosophila S2 cells (cellular incorporation<br />

achieved with a lipofection reagent) and in COS-7 cell lysate.<br />

Purity: ≥98% by HPLC.<br />

Cat. No. 208771 1 mg $195<br />

Calpain Activity Assay Kit, Fluorogenic<br />

Assay kit useful for the quantitative determination of calpain- and<br />

calpain-2 activity in human cell lysates, plasma, and serum and for<br />

screening calpain inhibitors. Requires a fluorimeter or microplate<br />

reader capable of measuring fluorescence at wavelengths of<br />

Ex. max: ~360 nm and Em. max: ~460 nm.<br />

Cat. No. QIA120 1 kit $345<br />

Calpain Substrate II, Fluorogenic<br />

Cyclic fluorogenic substrate for the quantitative determination of<br />

calpain - and -2. Also suitable for measuring the peptidase activity of<br />

the 20S proteasome. Typical concentrations range from 0– 00 µM,<br />

depending on assay conditions. Purity: ≥95% by TLC. Ex. max.: ~380 nm,<br />

Em. max.: ~460 nm.<br />

Cat. No. 208731 25 mg $75<br />

Calpain-1 Substrate, Fluorogenic<br />

2 mg $ 69<br />

set $325<br />

An internally quenched fluorogenic substrate peptide derived from the<br />

calpain- cleavage site of a-spectrin. It is not recognized by trypsin<br />

or a-chymotrypsin and serves as a sensitive and specific substrate for<br />

calpain- (K m = 4.6 µM; k cat = s - ). Cleavage occurs between Tyr-Gly<br />

residues and results in enhanced fluorescence. Purity: ≥95% by HPLC.<br />

Ex. max.: ~490 nm, Em. max.: ~518 nm.<br />

Cat. No. 208748 2 mg $163<br />

View more than 20 anti-calpain<br />

antibodies at our updated<br />

Antibody Resource<br />

www.calbiochem.com/<br />

antibodyresource<br />

6 Orders Phone 800 854 34 7<br />

Calbiochem • <strong>Inhibitor</strong> SourceBook<br />

Fax 800 776 0999<br />

Web www.emdbiosciences.com/calbiochem

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