ras 1/2/3

XRP44X (XRP 44X) is a potent inhibitor of Ras-Net (Elk-3) pathway.

1. Oroxylin A (Baicalein 6-methyl ether) has various anti-tumor effects including apoptosis, cell cycle arrest, drug-resistant reversion. 2. Oroxylin A possesses abilities of inhibiting the ATRA-induced IL-6 production via modulation of LAP LIP CHOP in leukemia cell lines, which could providing a therapeutic strategy for RAS. 3. Oroxylin A inhibits UCP2s triggers the MPTP opening, and promotes the apoptosis in CaCo-2 cells; uncoupling protein 2 plays a key role in mitochondrial apoptotic pathway. 4. Oroxylin A inhibits N1ICD translocating to the nucleus and binding to epithelial-mesenchymal transition-related transcription factor Snail, thus suppressing the invasion and migration of MCF-7 cells. 5. Oroxylin A improves the sensitivity of K562 ADM cells by increasing apoptosis in leukemic cells and decreasing the expression of CXCR4 and PI3K Akt NF-κB pathway, and probably served as a most promising agent for CML treatment.

K-Ras-IN-1, a K-Ras inhibitor, is characterized by its chemical formula C20H19ClN4O2S and is also known as N-[(1S)-3-cyclopropyl-1-[(6-fluoro-1H-benzimidazol-2-yl)sulfanyl]-2-oxo-1-(phenylmethyl)propyl]-4-fluorobenzenesulfonamide (compound [18, dashboard 819041] in brackets).

1. 3-Dehydrotrametenolic acid can be a potential anticancer agent against H-ras transformed tumor. 2. Dehydrotrametenolic acid is a promising candidate for a new type of insulin-sensitizing drug.

MBQ-167 is a dual inhibitor of Rac Cdc42 (IC50s: 103 nM for Rac 1 2 3 and 78 nM for Cdc42 in MDA-MB-231 cells, respectively).

YD-3 is a PAR4 antagonist that significantly inhibits thrombin-induced platelet aggregation in rabbits (IC(50)=28.3 microM). In addition, YD-3 suppresses thrombin-induced proliferation of vascular smooth muscle cells (VSMCs) and reduces neointimal thickening after balloon injury. Through Ras- and ERK1 2-mediated signaling pathways, YD-3 impedes thrombin-driven VSMC proliferation. When analyzed with Western blot, YD-3 primarily inhibits thrombin-induced expression of vascular endothelial growth factor receptor 2 (Flk-1) without affecting extracellular signal-regulated kinase 1 2 phosphorylation. YD-3 could potentially have value in elucidating the pathophysiology of thrombin-induced angiogenesis.

CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane agent that demonstrates effectiveness in inhibiting Ras activation and the downstream effector ERK1 2 pathway, thus effectively combating pancreatic tumor formation in mice. Additionally, CMC2.24 exerts potent inhibitory effects on zinc-dependent MMPs, with IC50s ranging from 2.0-69 μM. Furthermore, CMC2.24 aids in alleviating the progression of osteoarthritis by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis through the NF-κB HIF-2α axis[1][2][3].