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    TAME
    TAME

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1321
    CAS #: 901-47-3Purity ≥98%

    Description: TAME (Tosyl-L-Arginine Methyl Ester) is a potent small molecule inhibitor of APC (anaphase-promoting complex/cyclosome), which is an ubiquitin ligase with multiple subunits and can target proteins for degradation, leading to the separation of chromatids.

    References: Cancer Cell. 2010 Oct 19;18(4):382-95; Nat Rev Mol Cell Biol. 2006 Sep;7(9):644-56. 

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    Molecular Weight (MW)342.41
    FormulaC14H22N4O4S 
    CAS No.901-47-3
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 69 mg/mL (201.5 mM)
    Water: 69 mg/mL (201.5 mM)
    Ethanol: 3 mg/mL (8.76 mM) 
    SMILESCC1=CC=C(C=C1)S(N[[email protected]](C(OC)=O)CCCNC(N)=N)(=O)=O
    SynonymsTosyl-L-Arginine Methyl Ester


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    In Vitro

    In vitro activity: TAME inhibits cyclin proteolysis in mitotic Xenopus egg extract with IC50 of 12 µM. TAME at concentration of 1-200 μM arrests interphase extract treated with recombinant cyclin B1/Cdc2 complex in mitosis, with stable cyclin B1 and phosphorylated Cdc27. TAME at concentration of 200 μM dramaticly inhibits the ubiquitin ligase activity of the Anaphase-Promoting Complex (APC), accompanied by reduced binding of Cdh1 to APC. TAME addition to interphase extract reduces Cdc20 association with the APC in a dose-dependent manner partly by binding directly to APC, and the contribution motif is the C-terminal isoleucine-arginine (IR) tail on APC. TAME is hydrolysed by trypsin with Km of 0.328 mM. TAME accelerates the ATP hydrolysis process about 12-fold. TAME interacts with β and γ phosphate and the adenine ring of ATP by the guanidinium group and the aromatic ring. TAME at concentration of 50 mM inhibits nutrient-induced germination and pressure-induced germination at 600 MPa in Bacillus subtilis. TAME induces a concentration dependent contractile response on ileal strips with EC50 of 4.3 x 103 M.


    Kinase Assay: TAME at concentration of 1-200 μM arrests interphase extract treated with recombinant cyclin B1/Cdc2 complex in mitosis, with stable cyclin B1 and phosphorylated Cdc27. TAME at concentration of 200 μM dramaticly inhibits the ubiquitin ligase activity of the Anaphase-Promoting Complex (APC), accompanied by reduced binding of Cdh1 to APC. TAME addition to interphase extract reduces Cdc20 association with the APC in a dose-dependent manner partly by binding directly to APC, and the contribution motif is the C-terminal isoleucine-arginine (IR) tail on APC. TAME is hydrolysed by trypsin with Km of 0.328 mM. TAME accelerates the ATP hydrolysis process about 12-fold. TAME interacts with β and γ phosphate and the adenine ring of ATP by the guanidinium group and the aromatic ring. TAME at concentration of 50 mM inhibits nutrient-induced germination and pressure-induced germination at 600 MPa in Bacillus subtilis. TAME induces a concentration dependent contractile response on ileal strips with EC50 of 4.3 x 103 M.


    Cell Assay: In mitotic Xenopus oocytes, TAME competes with the Cdc20 C-terminal IR-tail for APC binding to inhibit APC-dependent proteolysis. [3] TAME also stabilizes cyclin B1via terminating ubiquitination prenaturally. It slows the unmodified cyclin B1 initial ubiquitination. In the presence of TAME, ubiquitinated cyclin B1 is not able to promote Cdc20 binding to the APC.

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    References

     Cancer Cell. 2010 Oct 19;18(4):382-95; Nat Rev Mol Cell Biol. 2006 Sep;7(9):644-56; Cell. 2004 Jul 9;118(1):99-110


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    TAME

    TAME inhibits APC activation by perturbing binding of Cdc20 or Cdh1. Cancer Cell. 2010 Oct 19;18(4):382-95.
     
     

    TAME

    TAME binds to the APC and inhibits binding of the IR tail of activator proteins. Cancer Cell. 2010 Oct 19;18(4):382-95.
     

    TAME

    TAME inhibits binding of wild type Cdc20 to the APC, but not binding of a ΔIR mutant. Cancer Cell. 2010 Oct 19;18(4):


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