TWC BioSearch
Signal Transduction Supplier

PROTEASOMES AND PROTEASES

(SEE APOPTOSIS SECTION FOR CPP32 AND ICE PROTEASE REAGENTS)

PROTEASOME INHIBITORS

PI-102
MG-132
Z-Leu-Leu-Leu-CHO
98%, MW=475.6 [133407-82-6] Storage: -20°C
A potent and selective reversible proteasome inhibitor (Ki= 4 nM). Inhibits NF-kB activation by preventing IkB degradation (IC50=3 mM)1.
5 mg
5 x 5 mg

PI-104
Lactacystin
99%, MW=376.4 [133343-34-7] Storage: -20°C
A potent and selective irreversible proteasome inhibitor2. Inhibits NF-kB activation by inhibiting IkB degradation (IC50=10 mM)3. Induces neurite outgrowth in Neuro 2A mouse neuroblastoma cells4.
200 µg
5 x 200 µg

CALPAIN

CALPAIN INHIBITORS

P-120
Calpain Inhibitor I (ALLN)
N-Acetyl-Leu-Leu-Nle-CHO
>97%, MW=383.5, Storage: -20°C
Cell-permeable, peptide aldehyde inhibitor of calpain and other neutral cysteine proteases. Inhibits cell cycle progression at G1/S and metaphase/anaphase in CHO cells by inhibiting cyclin B degradation5. Also stimulates HMG-CoA synthase transcription by inhibiting degradation of active SREBP-1 (sterol regulatory element-binding protein 1)6. Inhibits proteolytic degradation of IkBa and IkBb in RAW macrophages induced with LPS7.
5 mg
25 mg

PI-100
Calpain Inhibitor II (ALLM)
N-Acetyl-Leu-Leu-Met-CHO
98%, MW=401.6 [136632-32-1] Storage: -20°C
Cell-permeable, peptide aldehyde inhibitor of calpain and other neutral cysteine proteases. Potent inhibitor of cathepsin L (Ki=0.6 nM) and cathepsin B (Ki=100 nM)9.
5 mg
25 mg

PI-101
Calpeptin
Z-Leu-Nle-CHO
(N-Benzyloxycarbonyl-L-leucylnorleucinal)
98%, MW=362.5, Storage: -20°C
Cell-permeable, peptide aldehyde inhibitor of calpain and other neutral cysteine proteases. Inhibits calpain8 and cathepsin L9,10.
10 mg
50 mg

PI-105
E-64
trans-Epoxy succinyl-L-leucylamido-(4-guanidino) butane
98%, MW=357.4 [66701-25-5] Storage: -20°C
Cell-permeable, epoxysuccinyl peptide irreversible inhibitor of calpain and other cysteine proteases11,14. Inhibits a calpain-dependent apoptosis pathway in T cells12 but promotes heat-induced apoptosis in FM3A cells13.
5 mg
25 mg

PI-106
E-64-c
(2S,3S)-trans-Epoxysuccinyl-L-leucylamido-3-methylbutane
98%, MW=314.4 [76684-89-4] Storage: -20°C
Cell-impermeable epoxysuccinyl peptide inhibitor of calpain and other cysteine proteases11. Inhibits calpain and cathepsin B, H and L14.
1 mg
5 mg

PI-107
E-64-d
(2S,3S)-trans-Epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester
98%, MW=342.4 [88321-09-9] Storage: -20°C
Cell-permeable, ethyl ester of E-64-c, above. The ester is hydrolyzed by intracellular esterases to produce E-64-c. Inhibits calpain and cathepsin B, H and L15,16.
1 mg
5 mg

CALPAIN ANTIBODIES

SA-256
Anti-?Calpain (calpain I), domain II
Mouse monoclonal antibody. Clone 2H2A7C2. Immunogen: Purified bovine skeletal muscle ?calpain17. Supplied as ascites IgG1. Epitope is in large subunit, catalytic domain II of human ?calpain (residues 245-265). Recognizes human, bovine and rat 80 kDa subunit of ?calpain. Applications: WB 1/1000, IF 1/25.
100 µl

SA-257
Anti-?Calpain (calpain I), domain III
Mouse monoclonal antibody. Clone 9A4H8D3. Immunogen: Purified bovine skeletal muscle ?calpain17. Supplied as ascites IgG1. Epitope is in large subunit, domain III of human ?calpain (residues 465-520). Recognizes 80 kDa subunit of ?calpain from several mammalian species. Applications: WB 1/2000, IF 1/100.
100 µl

SA-255
Anti-m-Calpain (calpain II)
Mouse monoclonal antibody. Clone 107-82. Immunogen: Purified bovine skeletal muscle m-calpain17. Supplied as ascites IgG1. Epitope is in large subunit, domain III/IV of human calpain (residues 502-699). Recognizes human, procine and rat 80 kDa subunit of m-calpain. Applications: WB 1/500, IF 1/50.
100 µl

SA-283
Anti-Calpastatin, domain II
Mouse monoclonal antibody. Clone 2G11D6. Immunogen: Purified bovine skeletal muscle calpastatin17. Supplied as ascites IgG2a. Epitope is in domain II of human calpastatin (residues 295-501). Recognizes ~77 kDa human, bovine and rat calpastatin. Western blotting shows 150, 125, 90 and 70 kDa protein bands believed to be translation variants of calpastatin. Applications: WB 1/5000, IF 1/1000.
100 µl

SA-284
Anti-Calpastatin, domain IV
Mouse monoclonal antibody. Clone 1F7E3D10. Immunogen: Purified bovine skeletal muscle calpastatin17. Supplied as ascites IgG1. Epitope is in domain IV of human calpastatin (residues 543-673). Recognizes ~77 kDa human, bovine and rat calpastatin. Western blotting shows 150, 125, 90 and 70 kDa protein bands believed to be translation variants of calpastatin. Applications: WB 1/5000, IF 1/200.
100 µl

OTHER PROTEASE INHIBITORS

EI-212
Bestatin (Ubenimex)
99%, MW=308.4 [65391-42-6] Storage: 0°C
Aminopeptidase inhibitor18, Ki=3.5 µM for aminopeptidase-M19. Inhibits LTA4 hydrolase, a dual function protease and epoxide hydrolase, in a rapid, reversible, dose-dependent manner (IC50=4 µM)20. Immunomodulator21.
5 mg
25 mg

EI-213
Captopril
99%, MW=217.3 [62571-86-2] Storage: RT
Reversible and competitive inhibitor of LTA4 hydrolase (IC50=11 µM)22. An orally active inhibitor of angiotensin converting enzyme (ACE)20.
1 g
5 g

REFERENCES

1. J. Adams and R. Stein Ann. Rep. Med. Chem. 1996 31 279

2. G. Fenteany et al. Science 1995 268 726

3. L.R. Dick et al. J. Biol. Chem. 1997 272 182

4. G. Fenteany et al. Proc. Natl. Acad. Sci. USA 1994 91 3358

5. S.W. Sherwood et al. Proc. Natl. Acad. Sci. USA 1993 90 3353

6. X. Wang et al. Cell 1994 77 53

7. S.A. Milligan et al. Arch. Biochem. Biophys. 1996 335 388

8. Y. Banno et al. J. Biol. Chem. 1995 270 4318

9. T. Sasaki et al. J. Enz. Inhib. 1990 3 195

10. Tsujinaka et al. Biochem. Biophys. Res. Commun. 1988 153 1201

11. K.K.W. Wang and P.-W. Yuen TIPS 1994 15 411

12. A. Sarin et al. J. Immunol. 1994 153 862

13. W.G. Zhu et al. Biochem. Biophys. Res. Commun. 1996 225 924

14. A.J. Barrett et al. Biochem. J. 1982 201 189

15. M. Tamai et al. Chem. Pharm. Bull. 1987 35 1098

16. E.B. McGowan et al. Biochem. Biophys. Res. Commun. 1989 158 432

17. J. Cong et al. J. Biol. Chem. 1993 268 25740

18. S. Wilkes and J. Prescott J. Biol. Chem. 1985 260 13154

19. C. Tarnus et al. Bioorg. Med. Chem. 1996 4 1287

20. L. Orning et al. J. Biol. Chem. 1991 266 1375

21. V. St Georgiev Trends Pharmacol. Sci. 1990 11 373

22. L. Orning et al. J. Biol. Chem. 1991 266 16507

TWC Biosearch International Home Page