Ras

INCB159020 is an orally active inhibitor of KRAS G12D, exhibiting a KRAS G12D SPR value of 2.2 nM. It demonstrates anti-tumor activity.

XMU-MP-9, a bifunctional compound, targets the C2 domain of Nedd4-1 and the allosteric site of K-Ras. It enhances the interaction and induces conformational changes within the Nedd4-1/K-Ras complex. Furthermore, XMU-MP-9 facilitates the ubiquitination and degradation of various K-Ras mutants and inhibits the proliferation of cells with these mutants. This compound is useful in cancer research.

AH001 is an orally active compound that binds to a concealed pocket near GDP within RhoA, exhibiting a binding affinity of 73.16 nM. By interacting with GDP, AH001 stabilizes the interaction between RhoA and its endogenous inhibitor, RhoGDIα. This compound reduces nuclear translocation of downstream MRTFA and downregulates fibrosis/hypertrophy-related proteins. AH001 alleviates myocardial remodeling in various heart failure animal models and 3D cardiac tissue models. Its cardioprotective effects are mediated through the RhoA-RhoGDIα axis, effectively inhibiting downstream RhoA activation signals.

SOS2 ligand 1 (compound 2) is a selective ligand for son of sevenless 2 (SOS2), exhibiting a KD value of 4.6 µM.

pan-KRAS-IN-17 (Example 34) is an inhibitor that targets multiple forms of the KRAS protein.

BMS-214662 is a selective farnesyl transferase inhibitor with anti-tumor activity, used in research on pancreatic cancer, head and neck cancer, and lung cancer.

KRas G12C inhibitor 2 is a compound that inhibits KRas G12C.