Ras Inhibitor

FTS-MOM (Salirasib methoxymethyl ester), a Salirasib (FTS) (HY-14754) derivative, is a selective Rap1 inhibitor with selectivity over Ras. FTS-MOM inhibits GTP loading of Rap1 in quiescent and activated T cells. FTS-MOM inhibits Rap1-dependent T cell adhesion to ICAM-1.

KRAS-IN-63 is a KRAS^G12 inhibitor with a pIC₅₀ of 8.11. KRAS-IN-63 can be used in lung cancer-related research.

PROTAC SOS1 degrader-3 is a PROTAC degrader targeting SOS1, which induces the targeted degradation of SOS1 via the ubiquitin-proteasome system, with DC₅₀ values ranging from 0.19 μM to 0.75 μM in multiple distinct colorectal cancer cell lines. PROTAC SOS1 degrader-3 inhibits the phosphorylation of AKT and ERK. PROTAC SOS1 degrader-3 induces apoptosis and morphological changes in KRAS-mutant colorectal cancer organoids. PROTAC SOS1 degrader-3 can be applied in studies related to kras-mutant colorectal cancer.

KRAS inhibitor-40 (Compound 41) is a KRAS inhibitor that interferes with the KRAS G12C-BRAF complex. KRAS inhibitor-40 inhibits the ERK phosphorylation of KRAS downstream signaling pathway. KRAS inhibitor-40 can inhibit the proliferation of tumor cells with different KRAS mutation types and has antitumor activity.

KRAS inhibitor-21 (22b) is a KRAS G12C inhibitor with an IC₅₀ value of <0.01 μM. KRAS inhibitor-21 can be used in cancer research.

KRAS inhibitor-34 (compound 27) is a KRAS inhibitor, with IC₅₀ of 6.4 nM. KRAS inhibitor-34 can be used in tumor research.

PAT-IN-2 is a protein acyl transferases (PAT) inhibitor. PAT-IN-2 competitively inhibits Erf2 autopalmitoylation (WO2017011518A1; compound 25).

KRASG12C IN-18 is an orally active covalent KRAS^G12C inhibitor that achieves complete covalent engagement of KRAS^G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS^G12C and resistance-associated variants, including KRAS^G12C/R68S, with low-nanomolar IC₅₀ values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS^G12C-driven solid tumor and KRAS^G12C/R68S xenograft models and can be used for colorectal cancer research.

KRAS G12D inhibitor 22 (compound 6) is a inhibitor of KRAS mutation. KRAS G12D inhibitor 22 has high activity (IC₅₀＜100 nM), good selectivity and low toxicity.KRAS G12D inhibitor 22 can be used in breast cancer research.

Deltaflexin3 is a potent PDE6D inhibitor. Deltaflexin3 reduces the signaling of Ras and selectively decreases the KRAS mutant and PDE6D-dependent cancer cells growth.

KRAS G12C-IN-75 is an orally active, blood-brain barrier penetrant KRAS^G12C inhibitor with an IC₅₀ of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRAS^G12C alkylation in KRAS^G12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer.

RAS-IN-4 (example DA123) is a RAS inhibitor with antitumor activity.

PAT-IN-1 is a protein acyl transferases (PAT) inhibitor. PAT-IN-1 competitively inhibits Erf2 autopalmitoylation (WO2017011518A1; compound 13).

KRAS G12D inhibitor 13 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 13 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 142).

(7R)-Eras-4001 is an orally active KRAS mutant inhibitor with remarkable selectivity for H-RAS and N-RAS. (7R)-Eras-4001 effectively suppresses cancer cell viability by blocking downstream signaling pathways mediated by RAF family proteins, inhibiting the formation of the KRAS^G12D-RAF1 RBD complex and the phosphorylation of ERK1/2. (7R)-Eras-4001 induces tumor growth inhibition and regression in a dose-dependent manner, and also reduces plasma ERK1/2 phosphorylation levels. (7R)-Eras-4001 exerts a synergistic effect with anti-PD-1 Cetuximab (HY-P9905). (7R)-Eras-4001 can be used in research on non-small cell lung cancer, pancreatic cancer, colorectal cancer, and ovarian cancer.

Debecarasib is a KRAS inhibitor. Debecarasib exhibits antitumor activity and can be used in research on KRAS mutation-driven cancers.

PROTAC SOS1 degrader-1 is a degrader of SOS1 PROTAC, with a DC₅₀ of 98.4 nM and a K_d value of 44 nM. PROTAC SOS1 degrader-1 induces the formation of a ternary complex with SOS1 and the VCB E3 ubiquitin ligase complex, thereby promoting the ubiquitination and proteasomal degradation of SOS1. PROTAC SOS1 degrader-1 reduces KRAS-GTP levels, inhibits the phosphorylation of ERK in the RAS-RAF-MEK-ERK pathway, and suppresses the proliferation of cancer cells carrying KRAS mutations. PROTAC SOS1 degrader-1 inhibits tumor growth in mouse xenograft models. PROTAC SOS1 degrader-1 can be used for the research of KRAS-driven cancers.

KRAS G12D inhibitor 9 is a potent inhibitor of KRAS G12D. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. KRAS G12D inhibitor 9 has the potential for the research of KRAS G12D-mediated cancer (extracted from patent WO2021108683A1, compound 20).

BJ-2302 is a Src kinase inhibitor with an IC₅₀ of 3.23 μM, and inhibits cathepsin S (CTSS) activity.BJ-2302 binds to Src, suppresses PI3K/AKT and Ras/Raf/ERK pathways, and reduces CTSS and MMP-9 expression.BJ-2302 inhibits cancer cell invasion, metastasis, proliferation, and tumor growth.BJ-2302 does not induce cytotoxicity in normal breast epithelial cells.BJ-2302 can be used for the research of breast cancer and triple-negative breast cancer.

ZG1077 is a covalent KRAS G12C inhibitor. ZG1077 can be used in the research of non-small cell lung cancer (NSCLC).