KRpep-2d

£95.00 1mg

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.

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SKU: GT-010 Categories: ,

Additional information

Other Names

K-Ras(G12D)-targeting peptide

Three Letter Sequence

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

Molecular Weight

2560.02

Molecular Formula

C109H183N43O25S2

Sequence

Ac-RRRRC*PLYISYDPVC*RRRR-NH2

Purity

>95% by HPLC

Modifications

N terminal is acetylated, C terminal is amidated, disulfide bridge between cysteines 5 and 15

Searchable Words

KRpep-2d, GT-010, GT010, Ac-RRRRC*PLYISYDPVC*RRRR-NH2, 2098181-84-9, K-Ras(G12D)-targeting peptide