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Now Available from Sigma-RBI
Dephostatin (Prod. No. D 8065)
Ethyl-3,4-dephostatin (Prod. No. E 1904)
Methyl-3,4-dephostatin (Prod. No. M 9440)
Protein-tyrosine phosphatases (PTPases) catalyze the reversible phosphorylation of
tyrosine residues. The PTPases comprise two classes, transmembrane receptor PTPases, which contain linked
cytoplasmic catalytic domains, and intracellular PTPases, which include SRC homology 2 (SH2) domains.1,2
Sigma-RBI is pleased to offer dephostatin (Prod. No. D 8065),
a selective inhibitor of CD45 and SHP1-associated PTPases, and its two stable analogs, Ethyl-3,4-dephostatin
(Prod. No. E 1904) and Methyl-3,4-dephostatin
(Prod. No. M 9440).
- Dephostatin inhibits PTPase prepared from a human neoplastic T-cell line with an
IC50 = 7.7 µM.3
- Ethyl-3,4-dephostatin and Methyl-3,4-dephostatin strongly inhibit PTP-1B and SHPTP,
with IC50 values 0.58 and 0.96 µg/ml, respectively.1
- Ethyl-3,4-dephostatin enhances the phosphorylation of other proteins,
such as c-Cbl, phospholipase Cg (PLCg), phosphatidylinositol
3-kinase (PI3K) and insulin receptor 3 substrate (IRS-3).4
- Methyl-3,4-dephostatin inhibits CD45-associated PTPases while Ethyl-3,4-dephostatin
does not exhibit inhibitory activity.
References:
- Watanabe, T., et al., J. Chem. Soc. Chem. Commun., 4, 437-438 (1993).
- Kaplan, R., et al., Proc. Nat. Acad. Sci. USA, 87, 7000-7004 (1990).
- Imoto, M., et al., J. Antibiot. (Tokyo), 46, 1342-1346 (1993).
- Suzuki, T., et al., J. Biol. Chem., 276, 27511-27518 (2001).
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