Ras Inhibitor

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

SOS1-IN-9 is a potent SOS1 inhibitor with an IC₅₀ of 116.5 nM for SOS1-KRAS G12C (WO2022028506A1, compound 302).

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

KRAS G12C-IN-71 (Compound 11) is a covalent G12C KRAS inhibitor with a K_i of 380 nM. KRAS G12C-IN-71 can be used in the research of non-small cell lung cancer.

KRAS G12C-IN-70 is a selective KRAS G12C mutant inhibitor. KRAS G12C-IN-70 blocks KRAS G12C-mediated downstream signaling pathways (e.g., RAF-MEK-ERK) and inhibits tumor cell proliferation. KRAS G12C-IN-70 is promising for research of KRAS G12C mutation-related tumors (such as non-small cell lung cancer, colorectal cancer).

SL43 is an orally active and potent SOS1 inhibitor with a K_d of 0.16 μM. SL43 disrupts SOS1-KRAS interaction, inhibits SOS1-mediated nucleotide exchange on KRAS mutants, and suppresses RAS-MAPK signaling. SL43 exerts antiproliferative activity against KRAS-mutant cancer cells, induces early apoptosis and G1 phase cell cycle arrest, and reduces phosphorylated MEK and ERK levels. SL43 suppresses tumor growth in a colorectal cancer xenograft model.

SS-3091 is a pan-KRas inhibitor active across KRas^G12D, KRas^G12C, KRas^G12V, KRas^G12S mutants, with minimal effects on non-KRas-driven cancer cells. SS-3091 binds to the KRas·ARaf interaction interface, destabilizes the complex, and attenuates KRas activity. SS-3091 suppresses phosphorylation of S6K, Akt, and ERK. SS-3091 reduces proliferation and decreases colony formation of cancer cells bearing KRas^G12 mutations. SS-3091 can be used for the research of KRas-driven cancers.

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.

KRAS inhibitor-17 (compound 3-9) is a potent KRAS G12C inhibitor with an IC₅₀ of 3.37 µM. KRAS inhibitor-17 shows p-ERK inhibition activities with IC₅₀s of 9.25, >33.3 µM in MIA PaCA-2, A549 cells, respectively. KRAS inhibitor-17 has the potential for the research of pancreatic, colorectal, and lung cancers.

KRAS-IN-58 is a KRAS inhibitor with a IC₅₀ of 0.223 μM against KRAS^G12D. KRAS-IN-58 binds to KRAS^G12C and KRAS^G12D proteins, and reduces the levels of phosphorylated Raf1, AKT and ERK in pancreatic cancer cells. KRAS-IN-58 can be used for the research of pancreatic cancer.

RAS GTPase-IN-3 is a RAS GTPase inhibitor that targets multiple KRAS-Q61 mutant variants. RAS GTPase-IN-3 binds to the switch II pocket of GTP-bound KRAS-Q61R, positions its side-chain imidazole group near the GTP γ-phosphate, and accelerates GTP hydrolysis of KRAS-Q61. RAS GTPase-IN-3 inhibits Sos-catalyzed nucleotide exchange on GTP-bound KRAS. RAS GTPase-IN-3 only activates GTP hydrolysis of HRAS-Q61R/Q95H and NRAS-Q61R/L95H mutant proteins. RAS GTPase-IN-3 can be applied in research related to cancers driven by KRAS-Q61 mutations.

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.

Tyrphostin 8 is a tyrosine kinase, with an IC₅₀ of 560 μM for EGFR kinase. Tyrphostin 8 is also a GTPase inhibitor. Tyrphostin 8 can inhibit the protein serine/threonine phosphatase calcineurin (IC₅₀=21 μM).

SOS1-IN-6 (compound 33-P1) is a potent SOS1 inhibitor with IC₅₀s of 14.9 and 73.3 nM for SOS1-G12D and SOS1-G12V, respectively.

KRAS G12D-IN-27 (H12a) is an inhibitor of KRAS G12D. KRAS G12D-IN-27 inhibits ERK phosphorylation, with an IC₅₀ of 112 nM. KRAS G12D-IN-27 can be used in cancer research.

KRAS G12C-IN-78 is a selective SWII-binding KRASG12C dual inhibitor targeting both inactive and active states. KRAS G12C-IN-78 rapidly inhibits ERK1/2 phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits cellular proliferation in KRASG12C mutant cells. KRAS G12C-IN-78 can be used for the research of KRASG12C mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer.

(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.

KRAS G12C inhibitor 45 (compound 78) is a potent KRAS G12C inhibitor.

MG-Lin1 is a Lin28/Lin28A molecular glue degrader with a DC₅₀ of approximately 0.7 μM. It induces Lin28 degradation via the ubiquitin-proteasome pathway by forming a ternary complex, thereby upregulating the levels of let-7 miRNA and reducing the expression of its downstream oncogenic targets KRAS and PDK1, and inhibiting cancer cell migration. MG-Lin1 can be used in studies of ovarian cancer and choriocarcinoma.

KRas G12C inhibitor 2 is a compound that inhibits KRas G12C, extracted from patent US 20180072723 A1.