g12d

KRAS G12D inhibitor 5 is a potential treatment for pancreatic cancer that targets the KRAS G12D mutation.

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

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

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

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

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].

KRAS G12D inhibitor 1 (example 243) is an inhibitor of KRAS G12D, exhibiting an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation [1].

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.

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

RMC-9805 (Zoldonrasib) is a mutant-selective covalent KRAS G12D inhibitor with oral activity and significant antitumor activity, inducing tumor cell apoptosis in preclinical models of various KRAS-mutant cancers.

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[1] . BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants, with an average IC50 value of approximately 140 nM.[1]

Setidegrasib is a PROTAC-mediated KRAS degrader (DC50: 37 nM). Setidegrasib induces the formation of a ternary complex between KRAS G12D and the VHL E3 ubiquitin ligase, thereby facilitating the ubiquitination and proteasomal degradation of the oncogenic protein. Setidegrasib inhibits the levels of p-ERK, p-AKT, and p-S6 in AsPC-1 cells. Setidegrasib demonstrates antitumor activity in various mouse xenograft models of cancer. Setidegrasib can be used to study solid tumors with KRAS(G12D) mutations.

BC-LI-0186 (4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide) is a potent and selective inhibitor of the interaction of Leucyl-tRNA synthetase (LRS) and Ras-related GTP-binding protein D (RagD) with IC50 of 46.11 nM. BC-LI-0186 competitively binds the RagD interaction site of LRS with Kd of 42.1 nM and has no effect on LRS-vps34, LRS-eprs, RagB-RagD association, mTORC1 complex formation. BC-LI-0186 potently inhibits the activity of tumor-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 can be used for lung cancer-related research.

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.

KRAS G12D inhibitor 25 (Compound 148) acts as an inhibitor for KRAS G12C and HSP90α, displaying IC50 values of <0.1 μM and 0.1-1 μM respectively. Additionally, it suppresses the proliferation of MIA PaCa-2 and NCI-H358 cell lines, with EC50 values of <0.1 μM and 0.1-1 μM correspondingly. This compound also promotes the degradation of ERBB2, exhibiting a DC50 of 0.1-1 μM.

G12D ligand 1 is a ligand for the target protein in PROTAC (Ligand for Target Protein for PROTAC) and is utilized in the synthesis of Setidegrasib.

KRAS G12D inhibitor 26 (Compound 64B) is an inhibitor of KRAS G12D with an IC50 ≤ 100 nM.

KRAS G12D inhibitor 28 (Compound 1) is an inhibitor of KRAS G12D and can be utilized in cancer research.

PROTACKRAS G12D degrader 2 is a peptidomimetic molecule capable of inducing the degradation of SARS-CoV-2 3-chymotrypsin-like protease (3CLPro). Designed as a PROTAC molecule, it combines a dipeptidyl 3CLPro ligand based on GC-376 with a pomalidomide moiety, linked through a piperazine-piperidine linker.

PROTACKRAS G12D degrader 1 is a potent, rapid, and selective degrader of PROTACKRASG12D, with a DC50 of 38.06 nM. It demonstrates significant antitumor efficacy.

KRAS G12D inhibitor 20 (Compound 14) is a selective G12D KRAS inhibitor with antitumor activity.

KRAS G12D inhibitor 22 (compound 6) is a KRAS mutation inhibitor with high antitumor activity (IC50 < 100 nM), excellent selectivity, and low toxicity. It is applicable in breast cancer research.

KRAS G12D inhibitor 23 (compound 46-3) is a potent inhibitor of KRAS G12D, with an IC50 of 0.007 μM. It plays a significant role in cancer research.

(R)-KRAS G12D inhibitor 28 hydrochloride dihydrate is the dihydrate hydrochloride salt form of (R)-KRAS G12D inhibitor 28. KRAS G12D inhibitor 28 (Compound 1) acts as an inhibitor of the KRAS G12D protein and is utilized in cancer research.