- Cat. No.
- A19041
KRAS G12C inhibitor 13
KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30.
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Ras inhibitors and related small GTPase modulators act on KRAS and on the Rac, Rho and Cdc42 proteins. Small GTPases of the Ras superfamily work as molecular switches. They cycle between an active form bound to guanosine triphosphate (GTP) and an inactive form bound to guanosine diphosphate (GDP). Oncogenic KRAS mutations such as G12C keep the protein in its signaling state. ARS-853 and KRas G12C inhibitor 4 target the mutant cysteine of KRAS G12C, while Kobe2602 interferes with binding of Ras to Raf. Salirasib, a farnesylcysteine mimetic, disrupts the membrane association of Ras. Rho-family tools include NSC 23766 and EHT 1864, which inhibit Rac, and CASIN, which targets Cdc42.
KRAS G12C inhibitor 13 is a KRAS G12C inhibitor extracted from patent WO2018143315A1, compound 30.
EPAC 5376753 is an allosterically inhibitor of Epac which inhibits Epac1 with an IC50 of 4 µM in Swiss 3T3 cells.
K-Ras-IN-1 is a K-Ras inhibitor, by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.(the detailed information refer to the reference).
K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.
K-Ras G12C-IN-2 is an irreversible covalent K-Ras G12C inhibitor.
K-Ras G12C-IN-1 is a novel and irreversible inhibitor of mutant K-ras G12C extracted from patent WO 2014152588 A1.
(R)-CE3F4 is a potent and selective inhibitor of exchange protein directly activated by cAMP isoform 1 (Epac1), with an IC50 of 4.2 μM, with 10-fold selectivity for Epac1 over Epac2 (IC50, 44 μM).
Rhosin is a potent, specific RhoA subfamily Rho GTPases inhibitor, which specifically binds to RhoA to inhibit RhoA-GEF interaction with a Kd of ~ 0.4 uM, and does not interact with Cdc42 or Rac1, nor the GEF, LARG. Rhosin induces cell apoptosis.
Synonyms: ML282
CID-1067700 (ML282) is a pan GTPase inhibitor, and competitively inhibits Ras-related in brain 7 (Rab7) with a Ki of 13 nM.
Y16 is a specific inhibitor of Leukemia-associated Rho guanine nucleotide exchange factor (LARG) with a Kd value of 76 nM.
Rhosin hydrochloride is a potent, specific RhoA subfamily Rho GTPases inhibitor.
(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.
RBC10 is an inhibitor of Ral binding to RALBP1 (the effector).
MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 values ranging from 16 μM to 120 μM.
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression.
Synonyms: 3-Phenanthrenebutyric acid
NSC-92828, also known as 3-Phenanthrenebutyric acid, is a Protein-protein interaction inhibitor (PP inhibitor or PPI).
ARS-1323-Alkyne is a novel KRASG12C occupancy probe.
Synonyms: Paluratide
LUNA18 is an orally bioavailable cyclic peptide that functions as a dual inhibitor of KRAS and ERK signaling pathways. It disrupts the interaction between RAS and guanine nucleotide exchange factors (GEFs), effectively inhibiting RAS activation and downstream signaling. In RAS-mutated cancer cells, LUNA18 reduces cell proliferation while modulating key signaling nodes, including phosphorylation of ERK and AKT. In preclinical studies, LUNA18 demonstrates potent anticancer activity, particularly in xenograft models, by blocking RAS-driven tumor growth. It shows significant cellular efficacy against cancer cell lines harboring KRAS mutations, including colon, gastric, pancreatic, and non-small cell lung cancers, highlighting its therapeutic potential as a targeted agent for RAS-driven malignancies.
Synonyms: RMC-6291
Elironrasib is an orally active, covalent inhibitor specifically targeting the active GTP-bound form of KRAS^G12C (KRAS^G12C(ON)). It uniquely functions by forming a stable tri-complex with KRAS^G12C(ON) and cyclophilin A (CypA) within tumor cells, leading to steric hindrance that blocks the interaction between KRAS and its downstream effectors. This mechanism effectively suppresses RAS-mediated signaling, particularly the ERK pathway. Elironrasib induces apoptosis in KRAS^G12C-mutant H358 non-small cell lung cancer cells and demonstrates potent antiproliferative activity across KRAS^G12C-mutant cell lines, with a median IC₅₀ of 0.11 nM. Its high specificity and novel mechanism make it a promising therapeutic candidate for cancers driven by KRAS^G12C mutations.
RMC-7977 is an orally bioavailable, triple-complex RAS inhibitor that functions by simultaneously binding to cyclophilin A (CypA; K_d = 195 nM) and KRAS^G12V (K_d = 292 μM), facilitating the formation of a stable inhibitory complex. It exhibits broad-spectrum activity against RAS isoforms—including KRAS, NRAS, and HRAS—across both wild-type and mutant variants. RMC-7977 suppresses key oncogenic signaling pathways by inhibiting the phosphorylation of ERK, CRAF, and RSK, while promoting apoptosis through enhanced PARP cleavage. This dual mechanism results in significant tumor regression and reduced acquired resistance in KRAS^G12C-driven cancer models. It also shows favorable tolerability across a range of RAS-mutant tumor models, positioning it as a promising therapeutic candidate for RAS-driven malignancies.
RMC-4998 is an orally active inhibitor that selectively targets the active, GTP-bound state of the KRAS^G12C mutant. It forms a ternary complex with intracellular cyclophilin A (CYPA) and activated KRAS^G12C, exhibiting an IC50 of 28 nM. RMC-4998 suppresses ERK signaling and induces apoptosis in KRAS^G12C-mutant cancer cells, making it a valuable candidate for tumor research.
Synonyms: KRAS G12C inhibitor 19
Olomorasib is a potent and selective inhibitor of KRAS^G12C, demonstrating significant tumor growth inhibition, as reported in patent WO2021118877A1. It is under investigation for targeted therapy in KRAS^G12C-mutant cancers
Synonyms: KRAS G12D inhibitor 18; RMC-9805
Zoldonrasib (RMC-9805) is a potent, orally active inhibitor selectively targeting KRAS^G12D. It induces apoptosis in KRAS^G12D-mutant cancer cells and holds significant potential for the study and treatment of KRAS^G12D-driven malignancies.
Synonyms: JAB-21822
Glecirasib (Compound 1-2; JAB-21822) is a potent and orally active inhibitor of KRAS^G12C. As a member of the Ras protein family—key regulators of intracellular signaling involved in cell growth and development—KRAS^G12C is a critical oncogenic driver. Glecirasib shows strong potential for the study and treatment of KRAS^G12C-mediated cancers.
RGT-018 is a potent, orally active SOS1 inhibitor that exhibits anti-tumor activity by blocking KRAS activation. By disrupting the SOS1–KRAS interaction, RGT-018 effectively inhibits cancer cell proliferation, making it a promising candidate for targeting KRAS-driven malignancies.