kras g12d

KRAS G12D inhibitor 7, is a highly potent inhibitor specifically targeting KRAS G12D.

KRAS G12D Inhibitor 17 (example 8), a quinazoline-linked (4R)-4-hydroxy-L-prolinamide compound, acts as a proteolysis targeting chimera (PROTAC) [1], specifically inducing degradation of the G12D-mutation KRAS protein.

KRAS G12D mutation regulator 4 can be used in studies about Ras.

KRAS G12D inhibitor 5 is a KRAS G12D inhibitor for the potential treatment of pancreatic cancer.

KRAS G12D inhibitor 6 is an efficacious compound that effectively inhibits KRAS G12D.

KRAS G12D modulator-1 (compound 6), a potent modulator of KRAS G12D, exhibits IC50 values ranging from 1-10 μM against NEA-G12D, PPI-G12D, and p ERK-AGS, and is utilized in cancer research [1].

KRAS G12D Inhibitor 10 is a potent agent targeting the KRAS G12D mutation, a variant in the Ras protein family crucial for cellular growth and development. This compound shows promise for investigating cancers mediated by KRAS G12D.

KRAS G12D inhibitor 9 is a potent inhibitor of KRAS G12D. Among them, the RAS protein family is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 9 shows research potential for KRAS G12D-mediated cancer.

KRAS G12D Inhibitor 3 TFA, exhibiting an inhibitory concentration (IC50) of less than 500 nM, is effective as an antitumor agent.

KRAS G12D inhibitor 11 is a potent inhibitor of KRAS G12D. The Ras family of proteins are important intracellular signaling molecules that play an important role in growth and development, and KRAS G12D inhibitor 11 has shown potential for the investigation of KRAS G12D-mediated cancers.

KRAS G12D Inhibitor 3, a compound targeting the KRAS G12D mutation, demonstrates potent antitumor efficacy with an inhibitory concentration (IC50) of less than 500 nM.

KRAS G12D Inhibitor 16 is a potent compound targeting the KRAS G12D and its mutation, exhibiting inhibitory activity with IC50 values of 0.7 nM and 0.35 μM, respectively. It is utilized in researching various malignant tumors including pancreatic ductal adenocarcinomas (PDAC), colon and rectal carcinomas (CRC), and non-small cell lung carcinomas (NSCLC).

KRAS G12D inhibitor 1 (example 243) is an inhibitor of KRAS G12D with an IC 50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation [1].

KRAS G12D inhibitor 15 is a potent inhibitor specifically targeting the KRAS G12D mutation. It holds potential for research into numerous diseases or disorders, including cancer and its metastases[1].

KRAS G12D inhibitor 12 is an effective inhibitor of KRAS G12D. The Ras protein family is an important intracellular signaling molecule, which plays an important role in growth and development. KRAS G12D inhibitor 12 has the potential to perform KRAS G12D-mediated cancer studies.

KRAS G12D inhibitor 13 is a potent inhibitor of KRAS G12D. KRAS G12D inhibitor 13 has shown potential for the investigation of KRAS G12D-mediated cancers.

KRAS G12D inhibitor 14 is a potent inhibitor of KRAS G12D that binds KRAS G12D protein (Kd: 33 nM). KRAS G12D inhibitor 14 inhibits the active form of KRAS G12D (KRAS G12D-GTP), but not KRAS G13D.

Kras4B G12D-IN-1 is an anticancer agent that functions as an inhibitor of the Kras4B G12D protein. It effectively reduces the expression of Kras protein in mouse embryonic fibroblasts (MEFs) harboring the Kras4B G12D mutation[1].

G-{d-Arg}-GDSPASSK is a polypeptide that inhibits cell adhesion, facilitates wound healing, and promotes tissue repair [1].

G-{d-Arg}-GDSP, an RGD peptide analogue, binds to the adhesion receptor of integrins, inhibiting cellular attachment to fibronectin and osteoclast resorption [1].

12-Hydroxyganoderic acid D is a natural product

'(12β)-20-(β-D-Glucopyranosyloxy)-12-hydroxydammar-24-en-3-one is a naturally occurring compound isolated from Cladosporium microorganisms [1].'

12-O-Methylinophyllum D is a natural product for research related to life sciences. The catalog number is TN5897 and the CAS number is 40883-10-1.

Kras binder 12 can be used in studies about Ras.

RMC-9805 is a potent KRAS G12D inhibitor with potential anti-tumor and inhibitory activity against tumor cell proliferation for the study of pancreatic cancer.

Z-L(D-Val)G-CHN2, an isoform of Z-LVG-CHN2, serves as a cell-permeable and irreversible inhibitor of cysteine proteinase. This tripeptide derivative emulates a segment of the human cysteine proteinase-binding center and demonstrates selective antiviral activity, inhibiting herpes simplex virus (HSV) yet exhibiting negligible impact on poliovirus replication. Notably, Z-LVG-CHN2 effectively impedes SARS-CoV-2 replication with an EC50 value of 190 nM by targeting the SARS-CoV-2 3CL protease [3].

KRAS inhibitor-12 (compound 6-1) is a potent inhibitor of KRAS G12C (IC50: 0.537 μM). KRAS inhibitor-12 exhibits p-ERK inhibition in MIA PaCA-2, A549 cells with IC50 values of 1.3, 3.7 μM respectively. KRAS inhibitor-12 has potential to be studied in pancreatic, colorectal and lung cancers.

(D-Phe12,Nle21,38,α-Me-Leu37)-CRF (12-41) (human, rat) is a corticotropin-releasing factor (CRF) antagonist known to counteract the inhibitory effects of IL-1a on Luteinizing hormone (LH) production [1].

19-O-beta-D-carboxyglucopyranosyl-12-O-beta-D-glucopyranosyl-11,16-dihydroxyabieta-8,11,13-triene is a natural product of Pinus, Pinaceae. The catalog number is TN6493 and the CAS number is 1011714-20-7. 19-O-beta-D-carboxyglucopyranosyl-12-O-beta-D-glucopyranosyl-11,16-dihydroxyabieta-8,11,13-triene can be used as a reference standard.

Compound 40, NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal), a macrocyclic analogue of Ape13, acts as a potent APJ agonist with a Ki of 5.7 nM. It demonstrates favorable Gα12-biased signaling and possesses an enhanced in vivo half-life [1].

Compound 39 (NH2-c[X-R-L-S-X]-K-G-P-(D-1Nal)) is a potent agonist of the APJ receptor, possessing a K i value of 0.6 nM. It is capable of activating Gαi1, with an EC 50 of 0.8 nM, and of recruiting β-arrestin2, with an EC 50 of 31 nM. Furthermore, this compound demonstrates extended effects on cardiac function [1].

'(D-Phe5,Cys6,11,N-Me-D-Trp8)-Somatostatin-14 (5-12) amide (Compound 4) is a somatostatin analogue exhibiting varying affinity for somatostatin receptors, with dissociation constants (Kd) of 0.61 nM for SSTR5, 11.05 nM for SSTR3, 23.5 nM for SSTR2, 1200 nM for SSTR1, and >1000 nM for SSTR4, respectively [1].'

BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cells expressing KRAS G12C, G12D, or G12V mutants. BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants with an average IC50 value of approximately 140 nM.

MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.

KRPEP-2D acetate was identified as a K-Ras(G12D) selective inhibitory peptide against the G12D mutant of K-Ras, which is a key member of the Ras protein family and an attractive cancer therapeutic target.

Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1/2 activating mutations in the MAPK pathway.

MRTX1133 is a highly selective, first-in-class inhibitor of KRAS G12D. MRTX1133 targets the KRAS G12D protein in both active and inactive states. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells[1][2]. MRTX1133 demonstrates dose-dependent inhibition of the KRAS pathway tumor regression in G12D mutant tumor models[2]. [1]. Xiaolun Wang, et al.Kras g12d inhibitors.WO2021041671A1.[2]. KRAS G12D Inhibitor: MRTX1133. [(accessed on 22 April 2021)];2021 Available online.

GAGGVGKSAL, a wild-type KRAS G12D 10mer peptide, serves as an immunogenic neoantigen in cancer immunotherapy research [1].

GADGVGKSA, a mutant KRAS G12D 9mer peptide, serves as an immunogenic neoantigen for cancer immunotherapy research [1].

SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity ( EC 50 =106-175 nM). SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS [1] .

GADGVGKSAL, a mutant KRAS G12D 10mer peptide, serves as an immunogenic neoantigen in cancer immunotherapy research [1].

LUNA18 is an orally active inhibitor targeting KRAS, exhibiting potent activity with an IC50 value of less than 2 nM against the KRAS G12D-SOS mutation. It is utilized in cancer research [1].

Pan-KRAS-IN-2 (compound 6) is a broad-spectrum KRAS inhibitor exhibiting potent activity with IC50 values of ≤10 nM against KRAS wild type and its mutants (G12D, G12C, G12V, G12S, G12A, Q61H), while showing significantly reduced inhibition, with an IC50 ＞10 μM, for the KRAS G13D mutant [1].

GAGGVGKSA, a wild-type KRAS G12D 9mer peptide, serves as an immunogenic neoantigen pivotal for cancer immunotherapy research [1].

TH-Z827 is a mutant-selective inhibitor targeting KRAS(G12D) with an IC50 of 2.4 μM, demonstrating specificity by not binding to KRAS(WT) or KRAS(G12C). Additionally, it disrupts the KRAS(G12D)-CRAF interaction with an IC50 of 42 μM [1].

KRAS inhibitor-3, an efficacious inhibitor of both wild-type (WT) and oncogenic KRAS mutations, exhibits high-affinity binding (K D: 0.28 μM for KRAS WT, 0.63 μM for KRAS G12C, 0.37 μM for KRAS G12D, and 0.74 μM for KRAS Q61H). Additionally, it impedes the interaction between KRAS and Raf, highlighting its potential as a targeted therapeutic agent in KRAS-mutant cancers.

MRTX-EX185 is an effective inhibitor of GDP-loaded KRAS and KRAS (G12D) with an IC50=90 nM for KRAS (G12D). MRTX-EX185 is also capable of binding GDP-loaded HRAS.

TUS-007, a modified CANDDY (Chemical knockdown with Affinity aNd Degradation DYnamics) molecule originally derived from a proteasome inhibitor, scarcely affects proteasome activity. It is a potent, orally active degrader of KRAS G12D/V, effective in cell-free chemical knockdown of KRAS G12D/V. Furthermore, TUS-007 has been shown to suppress tumor growth [1].

TH-Z835 is a mutant-selective KRAS(G12D) inhibitor with an IC50 of 1.6 μM.This compound inhibits mantGMPPNP GPPNP exchange and GPPNP mantGMPPNP exchange.