KRpep-2d

Catalog No.S8499 Batch:S849902

Technical Data

Formula	C₁₀₈H₁₈₂N₄₄O₂₅S₂
Molecular Weight	2561.01	CAS No.	2098181-84-9
Solubility (25°C)*	In vitro


* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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

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].

Protocol (from reference)

Cell Assay:^{^[2]}	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.

Cell Assay:^{^[2]}

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.

References

Selleck's KRpep-2d has been cited by 2 publications

Overexpressed integrin alpha 2 inhibits the activation of the transforming growth factor β pathway in pancreatic cancer via the TFCP2-SMAD2 axis [ J Exp Clin Cancer Res, 2022, 41(1):73]	PubMed: 35193647
A PDX model combined with CD-DST assay to evaluate the antitumor properties of KRpep-2d and oxaliplatin in KRAS (G12D) mutant colorectal cancer [ Heliyon, 2022, 8(12):e12518]	PubMed: 36590511

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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