proTAME – 1 mg

Brand:
Cayman
CAS:
1362911-19-0
Storage:
-20
UN-No:
Non-Hazardous - /

proTAME is a cell-permeable prodrug form of N-4-tosyl-L-arginine methyl ester (TAME; Item No. 17550), an inhibitor of the anaphase-promoting complex/cyclosome (APC/C), that is converted to TAME by intracellular esterases.{28533,36286} proTAME (12 μM) blocks association of APC/C with the activator CDH1 and inhibits degradation of APC/C substrates in HeLa cells.{28533} It induces mitotic arrest in metaphase followed by cell death in synchronized HeLa H2B-GFP cells when used at a concentration of 12 μM. It also increases mitotic duration in asynchronous HeLa H2B-GFP cells at a concentration of 4 μM, an effect that is enhanced by knockdown of the APC/C co-activator CDC20. proTAME decreases the viability of several laboratory and primary patient-derived human multiple myeloma (MM) cell lines (IC50s = 2.8-20.3 μM) and increases apoptosis in RPMI-8226, LP-1, NCI-H929, and U266 MM cells when used at a concentration of 12 μM.{36286}  

 

Available on backorder

SKU: 25835 - 1 mg Category:

Description

A cell-permeable prodrug form of TAME; is converted to TAME by intracellular esterases; blocks association of APC/C with the activator CDH1 and inhibits degradation of APC/C substrates in HeLa cells at 12 μM; induces mitotic arrest in metaphase followed by cell death in synchronized HeLa H2B-GFP cells at 12 μM; increases mitotic duration in asynchronous HeLa H2B-GFP at 4 μM, an effect that is enhanced by knockdown of the APC/C co-activator CDC20; decreases the viability of several laboratory and primary patient-derived human MM cell lines (IC50s = 2.8-20.3 μM); increases apoptosis in RPMI-8226, LP-1, NCI-H929, and U266 MM cells at 12 μM


Formal name: (2S)-2-[[(4-methylphenyl)sulfonyl]amino]-9,13-dioxo-14-phenyl-7-[[[[(2-phenylacetyl)oxy]methoxy]carbonyl]amino]-10,12-dioxa-6,8-diazatetradec-6-enoic acid, methyl ester

Synonyms:  Pro-N-4-tosyl-L-arginine methyl ester

Molecular weight: 726.8

CAS: 1362911-19-0

Purity: ≥90%

Formulation: A solution in DMSO


Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death