Ras Inhibitor

ARN25062 (compound 27) is a CDC42/RHOJ inhibitor with antitumor activity. ARN25062 is a novel trisubstituted pyrimidine derivative.

R-IMPP hydrochloride (PF-00932239 hydrochloride) is a PCSK9 translation inhibitor and a selective 80S ribosome binder. R-IMPP hydrochloride inhibits the KRAS/MEK/ERK signaling cascade. R-IMPP hydrochloride reduces LPS-induced nuclear translocation of NFkB P65. R-IMPP hydrochloride increases LDL-R levels in cells, promotes LDL-C uptake, and does not alter the secretion of transferrin or albumin. R-IMPP hydrochloride inhibits the growth of colorectal cancer (CRC) cells, organoids and xenografts carrying APC/KRAS mutations, as well as the number and burden of spontaneous mouse tumors. R-IMPP hydrochloride can be used in research related to colorectal cancer with APC/KRAS mutations, hepatic ischemia-reperfusion injury and hypercholesterolemia.

CID-1067700 (Standard) is the analytical standard of CID-1067700 (HY-13452). This product is intended for research and analytical applications. CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a K_i of 13 nM.

Perillyl alcohol (Standard) is the analytical standard of Perillyl alcohol (HY-N7000). Perillyl alcohol is an orally active monoterpene. Perillyl alcohol exhibits multiple activities such as analgesic, anti-inflammatory, anti-tumor, anti-angiogenic, and anti-nociceptive effects. Perillyl alcohol can induce apoptosis and cell cycle arrest in tumor cells.

Aspartyl-alanyl-diketopiperazine (DA-DKP) (Standard) is the analytical standard of Aspartyl-alanyl-diketopiperazine (HY-107091). This product is intended for research and analytical applications. Aspartyl-alanyl-diketopiperazine is an immunomodulatory molecule and anti-inflammatory agent. Aspartyl-alanyl-diketopiperazine increases the level of active Rap1 in activated human T lymphocytes and reduces the phosphorylation levels of Ras, ATF-2, c-jun, MEK1, MEKK1, ERK1, JNK1,2,3, p38MAPK and MEF-2. Aspartyl-alanyl-diketopiperazine inhibits the production of pro-inflammatory cytokines, including the levels of IFN-γ and TNF-α. Aspartyl-alanyl-diketopiperazine can be used in studies of inflammatory immune responses.

Antifungal agent 140 (compound 5p) is a potent antifungal agent with broad-spectrum antifungal activity. Antifungal agent 140 exerts a dual mechanism by targeting the Ras/cAMP/PKA pathway to inhibit hyphal formation and the ergosterol biosynthesis pathway. Antifungal agent 140 enhances survival, reduces fungal load in the kidneys, and strengthens host immune responses in a murine model of systemic candidiasis. Antifungal agent 140 can be used for research of resistant fungal infections.

FTI-277 TFA is a farnesyltransferase (FTase) inhibitor. FTI-277 TFA inhibits Ras farnesylation, blocks the phosphorylation of downstream ERK1/2 and mTOR, and reduces membrane-bound active N-ras protein. FTI-277 TFA activates caspase 3, upregulates Bim expression, induces cell apoptosis, suppresses regulatory T cell expansion, enhances macrophage phagocytosis, and improves bacterial clearance. FTI-277 TFA activates the PI3K/Akt signaling pathway, inhibits osteoblast differentiation, and reduces the proliferation ability of neuroblastoma cells. FTI-277 TFA can be used in research related to head and neck squamous cell carcinoma, neuroblastoma, sepsis, and vascular calcification.

Pan-RAS-IN-1 (Standard) is the analytical standard of Pan-RAS-IN-1 (HY-101295). This product is intended for research and analytical applications. Pan-RAS-IN-1 is a pan-Ras inhibitor that disrupts the interaction of Ras proteins and their effectors.

Deltarasin is an inhibitor of KRAS-PDEδ interaction with K_d of 38 nM for binding to purified PDEδ. Deltarasin can be used in the study of cancer.

MRTX1133 (Standard) is the analytical standard of MRTX1133 (HY-134813). This product is intended for research and analytical applications. MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated K_D against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations.

Ketoconazole carbonyl-¹³C (Ketoconazol-¹³C) is ¹³C labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.

CFL-137 is a potent KRasG12C inhibitor. CFL-137 shows an antiproliferative effect. CFL-137 shows anticancer activity. CFL-137 has the potential for the research of lung cancer.

1A-116 (Standard) is the analytical standard of 1A-116 (HY-104064). This product is intended for research and analytical applications. 1A-116, a potent Rac1 inhibitor, is specific for W56 residues, can prevent EGF-induced Rac1 activation and block Rac1-P-Rex1 interaction. 1A-116 can induce apoptosis and inhibit cell proliferation, migration and cycle progression in a concentration-dependent manner. 1A-116 also demonstrates a high antimetastatic activity in vivo.

Adagrasib (Standard) is the analytical standard of Adagrasib (HY-130149). This product is intended for research and analytical applications. Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.

ZINC69391 (Standard) is the analytical standard of ZINC69391 (HY-102078). This product is intended for research and analytical applications. ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects.