K-Ras G12D inhibitor KS-58 is the first K-Ras(G12D) selective, bicyclic peptide inhibitor with binding Ki of 22 nM;
KS-58 suppressed growth of A427 cells and PANC-1 cells (human pancreas carcinoma, G12D mutant) down to 21.1% and 50.1% at 30 uM.
KS-58 showed significantly weaker cell growth suppression activities against A549 (human lung carcinoma, G12S mutant), H1975 (human lung carcinoma, WT), MIA PaCa-2 (human pancreas carcinoma, G12C mutant), and Capan-1 (human pancreas carcinoma, G12V mutant) cells.
KS-58 reduced the phosphorylation of ERK down to 26.0% and 57.6% at 30 uM, respectively.
Biotin-KS-58 exhibited stronger binding to K-Ras(G12D) than to other Ras proteins; KS-58 enters cells, binds to both forms of intracellular K-Ras(G12D)GDP/GTP, and inhibits K-Ras(G12D)GDP/GTP-effector protein interactions, thus preventing downstream Ras signal pathways, such as ERK, and suppressing cell proliferation.
KS-58 exhibits anti-cancer activity when given as an intravenous injection to mice with subcutaneous or orthotropic PANC-1 cell xenografts.
Cat.No
DC70546
Name
K-Ras G12D inhibitor KS-58
Chemical Properties
CAS
Formula
MW
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
Return Policy
If you are in any way unsatisfied with your purchase, you may return any item(s) within 365 days of its original purchase date.
Please provide your Order Number in the email. We strive to reply to all email inquiries within one business day.
