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119757-73-2

119757-73-2 structure
119757-73-2 structure
  • Name: Tautomycetin
  • Chemical Name: Tautomycetin
  • CAS Number: 119757-73-2
  • Molecular Formula: C33H50O10
  • Molecular Weight: 606.74400
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphatase
  • Create Date: 2016-01-02 02:55:21
  • Modify Date: 2024-01-21 19:48:36
  • 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].

Name Tautomycetin
Synonyms Taurohyodesoxycholsaeure
tatsinine perchlorate
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].
Related Catalog
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.
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
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.

Density 1.148g/cm3
Boiling Point 763.7ºC at 760mmHg
Molecular Formula C33H50O10
Molecular Weight 606.74400
Flash Point 233.9ºC
Exact Mass 606.34000
PSA 164.50000
LogP 3.94630
Vapour Pressure 6.37E-27mmHg at 25°C
Index of Refraction 1.518

CHEMICAL IDENTIFICATION

RTECS NUMBER :
WX0900000
CHEMICAL NAME :
Tautomycetin
CAS REGISTRY NUMBER :
119757-73-2
LAST UPDATED :
199406
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C33-H50-O12
MOLECULAR WEIGHT :
638.83

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
35 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JANTAJ Journal of Antibiotics. (Japan Antibiotics Research Assoc., 2-20-8 Kamiosaki, Shinagawa-ku, Tokyo, 141, Japan) V.2-5, 1948-52; V.21- 1968- Volume(issue)/page/year: 42,141,1989
Hazard Codes Xi
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