A CAAX peptidomimetic that selectively inhibits geranylgeranyltransferase I; arrests human tumor cells (IC50 = 10 µM for A549 cells) in G0/G1 and induces apoptosis by inhibiting proteasome activity and up-regulating the expression of the cyclin-dependent kinase inhibitor p21

GGTI 298 (trifluoroacetate salt) – 1 mg

Brand:
Cayman
CAS:
1217457-86-7
Storage:
-20
UN-No:
Non-Hazardous - /

Post-translational protein prenylation, a process catalyzed by three different enzymes, occurs at the C-terminal of a number of proteins involved in cell growth control and oncogenesis. One of these enzymes, geranylgeranyltransferase I (GGTase I) modifies cysteines of proteins with CAAX terminal sequences, preferring either leucine or isoleucine in the X-position. The Rho family of proteins are typically geranylgeranylated by GGTase I.{26347} GGTI 298 is a CAAX peptidomimetic that selectively inhibits GGTase I with little effect on other prenylation enzymes such as farnesyltransferase.{17870} It has been shown to arrest human tumor cells (IC50 = 10 µM for A549 cells) in G0/G1 and induce apoptosis by inhibiting proteasome activity and up-regulating the expression of the cyclin-dependent kinase inhibitor p21.{17870,17872,26346}  

 

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Description

A CAAX peptidomimetic that selectively inhibits geranylgeranyltransferase I; arrests human tumor cells (IC50 = 10 µM for A549 cells) in G0/G1 and induces apoptosis by inhibiting proteasome activity and up-regulating the expression of the cyclin-dependent kinase inhibitor p21

Formal name: N-[4-[[(2R)-2-amino-3-mercaptopropyl]amino]-2-(1-naphthalenyl)benzoyl]-L-leucine, methyl ester, 2,2,2-trifluoroacetate

Synonyms: 

Molecular weight: 593.7

CAS: 1217457-86-7

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cell Biology|Proteolysis|Ubiquitin/Proteasome System

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