TAME hydrochloride

SKU: orb1225913

Description

TAME is a small molecule anaphase-promoting complex/cyclosome (APC/C) inhibitor that binds to the APC preferentially suppresses APC/C(Cdc20) rather than APC/C(Cdh1); inhibits cyclin proteolysis in mitotic Xenopus egg extract with IC50 of 12 uM; promotes Cdc20 autoubiquitination, blocks cyclin degradation in interphase extract.

Key Properties

• CAS Number: 1784-03-8
• MW: 378.87
• Purity: >98% (HPLC)
• Formula: C₁₄H₂₂N₄O₄S.HCl
• SMILES: N=C(N)NCCC[C@@H](C(OC)=O)NS(=O)(C1=CC=C(C)C=C1)=O.[H]Cl
• Target: E3 Ubiquitin Ligase
• Solubility: DMSO: 37.9 mg/mL (100 mM) （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vitro:
  The absence of APC substrates, TAME hydrochloride ejects Cdc20 from the APC by promoting Cdc20 auto-ubiquitination in its N-terminal region. Cyclin B1 antagonizes TAME hydrochloride's effect by promoting binding of free Cdc20 to the APC and suppressing Cdc20 auto-ubiquitination. TAME hydrochloride stabilizes cyclin B1 in Xenopus extract by two mechanisms. First, it reduces the kcat of the APCCdc20/cyclin B1 complex without affecting the Km, slowing the initial ubiquitination of unmodified cyclin B1. Second, as cyclin B1 becomes ubiquitinated, it loses its ability to promote Cdc20 binding to the APC in the presence of TAME hydrochloride. As a result, cyclin B1 ubiquitination terminates before reaching the threshold necessary for proteolysis.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tosyl-L-arginine methyl ester hydrochloride

Quick Database Links

Gene Symbol

E3 Ubiquitin Ligase