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Products
Pharmacology
Type
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- Technical support
- Resources
KRpep-2d
Cat. No. GT-010
Structure:
Ac-Arg-Arg-Arg-Arg-Cys*-Pro-Leu-Tyr-Ile-Ser-Tyr-Asp-Pro-Val-Cys*-Arg-Arg-Arg-Arg-NH2; disulfide bridge between cysteines 5 and 15
Other Names:
K-Ras(G12D)-targeting peptide
Activity:
K-Ras inhibitor
KRpep-2d is a potent K-Ras inhibitor, discovered after optimization of an initial hit obtained by phage display technology. KRpep-2d inhibits the enzyme activity of K-Ras(G12D) with an IC50 of 1.6 nM, and with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant in both cell-free enzyme and cell based assays. Mutated Ras proteins play important roles in cell differentiation, proliferation, and survival of various cancers, and K-Ras(G12D) is considered a very important target as K-Ras mutations underlie 86% of Ras-linked cancers, with 83% of K-Ras mutations being at the G12 residue. KRpep-2d can suppress ERK phosphorylation downstream of K-Ras(G12D) and reduce proliferation in A427 cancer cells.
Niida et al (2017) Investigation of the structural requirements of K-Ras(G12D) selective inhibitory peptide KRpep-2d using alanine scans and cysteine bridging. Bioorg Med Chem Lett. 27(12) 2757 PMID: 28457754
Sakamoto et al (2017) K-Ras(G12D)-selective inhibitory peptides generated by random peptide T7 phage display technology. Biochem Biophys Res Commun. 484(3) 605 PMID: 28153726
Lim et al (2021) Discovery of cell active macrocyclic peptides with on-target inhibition of KRAS signaling. Chem Sci. 12(48) 15975 PMID: 35024121
Related areas
All peptides >
All GTPase modulators >
All cancer research categories >
Technical Data
| Structure | Ac-Arg-Arg-Arg-Arg-Cys*-Pro-Leu-Tyr-Ile-Ser-Tyr-Asp-Pro-Val-Cys*-Arg-Arg-Arg-Arg-NH2; disulfide bridge between cysteines 5 and 15 |
| CAS Number | 2098181-84-9 |
| Molecular Weight | 2560.02 |
| Formula | C109H183N43O25S2 |
| Sequence | Ac-RRRRC*PLYISYDPVC*RRRR-NH2 |
| Modifications | N terminal is acetylated, C terminal is amidated, disulfide bridge between cysteines 5 and 15 |
Batch Specific Data
| Purity | >95% by hplc |
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Recent citations
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