KRpep-2d

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Description: Potent and selective KRASG12D inhibitor
Purity: ≥95% (HPLC)
Datasheet
Citations
Reviews
Literature (4)
Pathways (1)

Biological Activity for KRpep-2d

KRpep-2d is a potent KRAS inhibitor. Selective for G12D mutant KRAS over wild type KRAS (IC50 = 1.6 nM and 42 nM respectively). Allosterically binds to KRAS to block interaction with substrate, such as GDP. Cell permeable and suitable for use in vitro.

Technical Data for KRpep-2d

M. Wt 2561.03
Formula C108H182N44O25S2
Sequence RRRRCPLYISYDPVCRRRR

(Modifications: Arg-1 = N-terminal Ac, Disulfide bridge: 5-15, Arg-19 = C-terminal amide)

Storage Store at -20°C
Purity ≥95% (HPLC)
CAS Number 2098181-84-9
InChI Key PNSDZPKWIOBSHR-WVEXBLHFSA-N
Smiles O=C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N)=O)=O)=O)=O)=O)NC1=O)C(N2[C@@H](CCC2)C(N[C@@H](CC(C)C)C(N[C@@H](CC3=CC=C(C=C3)O)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CO)C(N[C@@H](CC4=CC=C(C=C4)O)C(N[C@@H](CC(O)=O)C(N5[C@@H](CCC5)C(N[C@H]1C(C)C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCCNC(NC(C)=O)=N)N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for KRpep-2d

Solubility Soluble to 2 mg/ml in water

References for KRpep-2d

References are publications that support the biological activity of the product.

Sakamoto et al (2017) K-Ras(G12D)-selective inhibitory peptides generated by random peptide T7 phage display technology. Biochem.Biophys.Res.Commun. 484 605 PMID: 28153726


If you know of a relevant reference for KRpep-2d, please let us know.

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Keywords: KRpep-2d, KRpep-2d supplier, KRpep2d, KRAS, krasg12d, g12d, inhibitor, inhibitors, inhibits, potent, selective, cell, permeable, in, vitro, Ras, GTPases, 7928, Tocris Bioscience

Citations for KRpep-2d

Citations are publications that use Tocris products.

Currently there are no citations for KRpep-2d. Do you know of a great paper that uses KRpep-2d from Tocris? Please let us know.

Reviews for KRpep-2d

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer Metabolism Research Product Guide

Cancer Metabolism Research Product Guide

This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:

RAS Oncoproteins Scientific Review

RAS Oncoproteins Scientific Review

Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. Compounds available from Tocris are listed.

Cell Cycle & DNA Damage Repair Poster

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Pathways for KRpep-2d

Akt Signaling Pathway

Akt Signaling Pathway

The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.
MAPK Signaling Pathway

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.