kras 1

KRas G12C inhibitor 1 is a compound that selectively inhibits the KRas G12C protein.

Pan-KRAS degrader 1 (Compound 1) is a broad-spectrum KRAS degrader, exhibiting an inhibitory constant Ki value of 25 nM against KRASG12V as determined by surface plasmon resonance (SPR). Additionally, this compound demonstrates antitumor activity.

LZTR1-KRAS modulator 1 is a regulator of the KRAS-LZTR1 interaction, enhancing the recruitment of the LZTR1-KRAS complex.

Pan-KRAS Ligand 1 serves as a ligand for the target protein of PROTAC (Ligand for Target Protein for PROTAC). This compound facilitates the synthesis of PROTAC Pan-KRAS Degrader 4.

KRAS mutant protein inhibitor 1 is a KRAS mutant protein inhibitor [for potential treatment in cancer].

KRas G12R Inhibitor 1 (compound 3) is a selective covalent inhibitor targeting the KRas G12R mutation, leveraging the high nucleophilicity of mutant cysteines to bind irreversibly within the K-Ras Switch II region. This compound is utilized in cancer research [1].

KRAS G12C mutant protein inhibitor A-1 can be used in studies about Ras.

PROTAC KRAS G12C degrader-1, a cereblon-based degrader, promotes CRBN KRAS G12C dimerization and facilitates the degradation of GFP-KRAS G12C in reporter cells [1].

KRAS G12D modulator-1 (compound 6), a potent modulator of KRAS G12D, exhibits IC50 values of 1-10 μM against NEA-G12D, PPI-G12D, and p ERK-AGS, and is utilized in cancer research [1].

KRAS degrader-1 (compound 1) is a potent agent that selectively targets KRAS proteins for degradation via the autophagy-lysosomal pathway [1].

SOS1 KRAS-IN-1 (Compound 2) serves as an inhibitor of SOS1 KRAS, with potential application in the study of diseases mediated by SOS1 KRAS [1].

KRAS G12D inhibitor 1 (example 243) is an inhibitor of KRAS G12D, exhibiting an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation [1].

BI-2865 is a non-covalent pan-KRAS inhibitor.BI-2865 binds to KRAS WT, G12C, G12D, G12V, and G13D mutants with KD values of 6.9, 4.5, 32, 26, and 4.3 nM, respectively.BI-2865 showed antiproliferative activity in BaF3 cells expressing KRAS G12C, G12D, or G12V mutants[1] . BI-2865 showed antiproliferative activity on BaF3 cells expressing KRAS G12C, G12D or G12V mutants, with an average IC50 value of approximately 140 nM.[1]

Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1 2 activating mutations in the MAPK pathway.

BI-3406 is an orally active, highly potent and selective between KRAS and Son of Sevenless 1 (SOS1) interaction inhibitor(IC50 : 6 nM),with anticancer activity.

LJI308 is a potent, and pan-RSK (p90 ribosomal S6 kinase) inhibitor with IC50 of 6 nM, 4 nM, and 13 nM for RSK1, RSK2, and RSK3, respectively.

AMG410 is a non-covalent, bimodal GDP (OFF) and GTP (ON)-binding pan-KRAS inhibitor with Kd (GDP) = 1 nM and Kd (GTP) = 22 nM, which enables circulation-independent blockade of KRAS. AMG410 is more than 100-fold selective for KRAS than HRAS and NRAS2, binds on the same variegated pocket as KRAS G12C inhibitors, and has high potency in KRAS G12D, G12V, G12C, G13D and other mutants, IC 50 = 1-4 nM. AMG140 regresses tumors and reduces phosphorylated ERK levels in colorectal, pancreatic and lung models of KRAS mutations.

RMC-6291 is an orally active, covalent inhibitor of KRAS G12C (ON) that forms a tri-complex within tumor cells between KRAS G12C (ON) and cyclophilin A (CypA), thereby preventing KRAS G12C (ON) from signaling via steric blockade of RAS effector binding and eliciting deep and durable suppression of RAS pathway activity in KRAS G12C tumor models [1].

FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.

FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.

K-Ras G12C-IN-1 is a novel, irreversible inhibitor of mutant K-Ras G12C.

KRAS G12C inhibitor 14 is a potent compound with an IC50 of 18 nM [1].

PROTAC K-Ras Degrader-1 is a PROTAC degrader based on the Cereblon E3 ligand, capable of degrading K-Ras.

Leptomycin B (LMB) is a potent inhibitor of the nuclear export of proteins and is a potent antifungal antibiotic blocking the eukaryotic cell cycle. Leptomycin B inactivates CRM1 exportin 1 by covalent modification at a cysteine residue.