R8-T198wt

Product Name:R8-T198wt

CAS No:2305815-72-7

Purity:95%

Molar Mass:2820.33

Chemical Formula:C111H211N59O26S

Storage:Store at -20 degrees Celsius

Sequence:GGGRRRRRRRRGCKKPGLRRRQT

Target:Pim-1

Application:R8-T198wt is a cell-penetrating peptide designed to target Pim1, a serine/threonine kinase involved in key cellular processes such as proliferation, survival, and apoptosis. The R8 component, which consists of eight arginine residues, facilitates the delivery of the T198wt peptide into cells, where it can interact with Pim1. This system is particularly useful in cancer research, as Pim1 is frequently overexpressed in various cancers and plays a role in tumor development and progression. R8-T198wt enables researchers to study Pim1's function and develop potential therapeutic strategies targeting Pim1 for cancer treatment.

Current Research:

R8-T198wt is a cell-permeable peptide inhibitor derived from the C-terminal region of p27^Kip1, designed to specifically inhibit Pim-1 kinase activity. Pim-1, a serine/threonine kinase, plays a pivotal role in cell cycle progression and survival, often contributing to oncogenesis when dysregulated.
Mechanism of Action
R8-T198wt binds to Pim-1 with a dissociation constant (K_D) of approximately 323 nM, effectively inhibiting its kinase activity. This inhibition prevents the phosphorylation of downstream substrates such as p27^Kip1 and Bad, leading to cell cycle arrest at the G1 phase and induction of apoptosis in cancer cells.
Antitumor Activity
In vitro studies have demonstrated that R8-T198wt induces G1 arrest and apoptosis in DU145 prostate cancer cells. Notably, it enhances the expression levels of HA-p27^Kip1, indicating its role in stabilizing this tumor suppressor protein.
Selectivity
Importantly, R8-T198wt exhibits minimal effects on the growth of normal prostate epithelial RPWE-1 cells at concentrations up to 20 ??M, suggesting a degree of selectivity towards cancer cells overexpressing Pim-1.
Research Applications
R8-T198wt serves as a valuable tool in cancer research, particularly in exploring the role of Pim-1 in tumorigenesis and evaluating the therapeutic potential of Pim-1 inhibition. Its ability to modulate cell cycle dynamics and apoptosis makes it a promising candidate for developing targeted cancer therapies.

Reference:

Morishita, D., Takami, M., Yoshikawa, S., Katayama, R., Sato, S., Kukimoto-Niino, M., ... & Fujita, N. (2011). Cell-permeable carboxyl-terminal p27Kip1 peptide exhibits anti-tumor activity by inhibiting Pim-1 kinase. Journal of Biological Chemistry, 286(4), 2681-2688.