Ras Inhibitor

KRAS G12C inhibitor 31 is a KRAS G12C inhibitor extracted from patent WO2021252339A1, compound 1. KRAS G12C inhibitor 31 can be used for the research of cancer.

Pan-RAS-IN-5 is a macrocyclic pan-RAS inhibitor that targets mutant RAS (including KRAS, NRAS, and HRAS). Pan-RAS-IN-5 inhibits the proliferation of various KRAS-mutant cancer cells. Pan-RAS-IN-5 is applicable to the research of KRAS mutation-related cancers such as pancreatic cancer, nephroblastoma, and colon adenocarcinoma.

ISIS-2503 sodium is a 20-mer antisense oligonucleotide that inhibits Ha-Ras expression

KRAS inhibitor-38 (Example 18) is a KRAS inhibitor that effectively suppresses the activity of KRAS G12C, KRAS G12D, and KRAS G12V in vivo.

BIM-46068 is a potent, selectively human brain Farnesyltransferase (FTase) inhibitor (IC₅₀ = 91.4 nM). BIM-46068 can specifically inhibit Ras processing in MiaPaCa-2 cancer cells. BIM-46068 can be used for the study of pancreatic cancer.

GGDPS-IN-1 (Compound 37) is a geranylgeranyl diphosphate synthase (GGDPS) inhibitor with an IC₅₀ of 49.4 nM. GGDPS-IN-1 disrupts protein geranylgeranylation in myeloma cells.

(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer.

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.

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.

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

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

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).

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.

RAS-IN-5 (Example 2) is a RAS inhibitor. RAS-IN-5 significantly inhibits the interaction between RAF1 and active KRAS mutant protein or HRAS WT protein. RAS-IN-5 significantly inhibits the cell viability of KRAS, NRAS, and EGFR mutant cells. RAS-IN-5 can be used in the research of colorectal cancer, liver cancer, and non-small cell lung cancer.

Avicin G is a sphingomyelinase inhibitor and plasma membrane disruptor. Avicin G inhibits the enzymatic activities of neutral sphingomyelinases (SMPD2/3) and acid sphingomyelinase (SMPD1), elevates intracellular sphingomyelin levels, and alters the distribution of sphingomyelin. Avicin G interferes with the lateral segregation of GTP- and GDP-bound H-Ras, inhibits the signal output of oncogenic K-Ras and H-Ras, reduces the phosphorylation of ERK and Akt, increases lysosomal pH, and inhibits the endocytic recycling of epidermal growth factor receptor. Avicin G can be used in research related to pancreatic ductal adenocarcinoma and non-small cell lung cancer.