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Cat. No. M21627
Tautomycetin Structure


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Biological Activity

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 (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.

Chemical Information
Molecular Weight 606.74
Formula C33H50O10
CAS Number 119757-73-2
Solubility (25°C) DMSO 10 mg/mL
Storage -20°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Zachary R Woydziak, et al. ChemMedChem. Tautomycetin Synthetic Analogues: Selective Inhibitors of Protein Phosphatase I

[2] Danilo Pereira de Sant'Ana, et al. J Org Chem. Synthetic Studies toward the Total Synthesis of Tautomycetin

[3] Si-Sun Choi, et al. J Ind Microbiol Biotechnol. Biosynthesis, regulation, and engineering of a linear polyketide tautomycetin: a novel immunosuppressant in Streptomyces sp. CK4412

[4] Joon-Hee Lee, et al. Mol Cancer Ther. Tautomycetin inhibits growth of colorectal cancer cells through p21cip/WAF1 induction via the extracellular signal-regulated kinase pathway

[5] H Oikawa. Curr Med Chem. Synthesis of specific protein phosphatase inhibitors, tautomycin and tautomycetin toward structure-activity relationship study

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Keywords: Tautomycetin, TMC supplier, Phosphatase, inhibitors, activators

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