Home Cell Cycle Ras inhibitor KRpep-2d For research use only.

KRpep-2d

KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM.

KRpep-2d Chemical Structure

KRpep-2d Chemical Structure

CAS No. 2098181-84-9

Purity & Quality Control

KRpep-2d Related Products

Signaling Pathway

Ras Signaling Pathways

Ras Signaling Pathway

Biological Activity

Description KRpep-2d is a K-Ras(G12D) selective inhibitory cyclic peptide with selectivity against wild-type (WT) K-Ras and the K-Ras(G12C) mutant. The IC50 value is 1.6 nM.
Targets
K-Ras(G12D) [1]
(Cell-free assay)
1.6 nM
In vitro
In vitro KRpep-2d binds to K-Ras（G12D）with a Kd of 8.9 nM and approximately 6-fold selectivity over WT K-Ras, leading to an extended dissociation half-life[1]. KRpep-2d significantly suppresses ERK-phosphorylation, downstream of K-Ras(G12D), along with A427 cancer cell proliferation at 30 μM peptide concentration[2].
Cell Research Cell lines A427 (lung, G12D mutant) and A549 (lung, G12C mutant) cells
Concentrations 0, 0.3, 3, 30 μM
Incubation Time 3 days
Method

For the growth inhibition assay, A427 and A549 cells are seeded at 4000 and 2000 cells/well in 96-well plates, respectively. Cells are treated with the peptides on the following day. For the 3-day treatments, medium containing the peptides is replaced every day. Relative cell numbers are estimated using CellTiter-Glo according to the manufacturer's instructions. Luminescence is measured using an EnVision plate reader. Percent inhibition is calculated based on cell numbers at Day 0 as low control and at Day 3 without peptide as high control.

Chemical Information & Solubility

Molecular Weight 2561.01 Formula

C108H182N44O25S2
CAS No. 2098181-84-9 SDF Download KRpep-2d SDF
Smiles CCC(C)C1NC(=O)C(CC2=CC=C(O)C=C2)NC(=O)C(CC(C)C)NC(=O)C3CCCN3C(=O)C(CSSCC(NC(=O)C(NC(=O)C4CCCN4C(=O)C(CC(O)=O)NC(=O)C(CC5=CC=C(O)C=C5)NC(=O)C(CO)NC1=O)C(C)C)C(=O)NC(CCCNC(N)=N)C(=O)NC(CCCNC(N)=N)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

Water : 100 mg/mL


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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