pmek

IACS-13909 (BBP-398), a specific and potent allosteric inhibitor of SHP2, that suppresses signaling through the MAPK pathway.

Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5/0.6 nM) and is ATP-competitive. Dabrafenib exhibits antitumor activity for the treatment of B-RafV600E-mutated melanoma.

MSI-1701, an analogue of MSI-1436, enhances (MSI-1436) activity by increasing (pMEK) and (pERK) phosphorylation, thus promoting (PI3K/AKT) pathway signaling and inhibiting apoptosis in neuronal cells, which may contribute to its neuroprotective effects.

SHOC2–RAS PPI-IN-1 (compound 6) is a non-covalent competitive inhibitor that targets the interaction between SHOC2 and RAS proteins. It exhibits an IC50 of 0.048 μM and a KD of 0.065 μM against NRASQ61R. This compound inhibits SMP phosphatase-complex activity, increasing CRAFS259 phosphorylation levels and thus blocking the MAPK signaling pathway (by reducing pMEK and pERK levels). It induces cell cycle arrest and apoptosis in tumor cells. SHOC2–RAS PPI-IN-1 is used in targeting studies for malignancies, such as NRASQ61R-mutant melanoma and colorectal cancer.

MEK-IN-5, a potent MEK inhibitor and nitric oxide (NO) donor, effectively decreases pMEK and pERK levels in a dose-dependent and time-dependent fashion. Additionally, it induces apoptosis in MDA-MB-231 cells.