| Description |
Tautomycetin is a potent and specifical PP1 inhibitor with the potential apoptosis-inducing activity. Tautomycetin inhibits purified PP1 and PP2A enzymes with IC50s of 1.6 nM and 62 nM, respectively. Tautomycetin is an antifungal antibiotic and has immunosuppressive effects in vivo. Tautomycetin can be used as a novel powerful tool to elucidate the physiological roles of PP1 in various biological events[1].
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| Related Catalog |
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| In Vitro |
Tautomycetin (100 ng/ml-10 μg/ml; 48 hours) has inhibitory effects on T cell proliferation in the murine mixed lymphocyte reaction (MLR) assays. The level of inhibition of MLR by TMC is 100-fold higher than that by CsA, and the IC50 of TMC is 7.8 nM[1]. Tautomycetin (1 μg/ml) possesses immunosuppressive activity to inhibit the proliferation of T cells by inhibition of IL-2 secretion in human primary T cells[1]. Tautomycetin (1 μg/ml; pretreated for 5 hours) blocks the phosphorylation of tyrosine residues on several specific cellular proteins in a dose- and time-dependent manner in T cells stimulated by immobilized OKT3 mAb[1]. Tautomycetin (1 μg/ml; 5 hours) significantly inhibits the phosphorylation of Akt and BAD in a dose-dependent fashion inn Jurkat TAg cell line[1]. Western Blot Analysis[1] Cell Line: Human primary B cells Concentration: 1 μg/ml Incubation Time: Pretreated for 5 hours, and then stimulated with immobilized OKT3 mAb (10 μg/ml) for 0, 5, 10 miuntes Result: Blocked tyrosine phosphorylation of intracellular signal mediators. Apoptosis Analysis[1] Cell Line: Jurkat T cells Concentration: 1 μg/ml Incubation Time: 5 hour Result: Induces cell apoptosis.
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| In Vivo |
Tautomycetin (intraperitoneal injection; 0.03 mg/kg-5 mg/kg; 30 days) exhibits in vivo immunosuppressive effect in in vivo heart allograft transplantation. And the biochemical analysis of GOP, GTP, glucose, and creatine levels in blood after administration of TMC up to 5 mg/kg in rats for 30 days does not show any significant liver and kidney toxicity in rats[1]. Animal Model: Rat[2] Dosage: 0.03 mg/kg, 0.5 mg/kg, 5 mg/kg; 30 days Administration: Intraperitoneal injection Result: Exhibited immunosuppressive effects in vivo
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| References |
[1]. S Mitsuhashi, et al. Tautomycetin is a novel and specific inhibitor of serine/threonine protein phosphatase type 1, PP1. Biochem Biophys Res Commun. 2001 Sep 21;287(2):328-31. [2]. Jae-Hyuck Shim, et al. Immunosuppressive effects of tautomycetin in vivo and in vitro via T cell-specific apoptosis induction. Proc Natl Acad Sci U S A. 2002 Aug 6;99(16):10617-22.
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