In heterogeneous catalysis, catalysts provide a surface to which reactants bind in a process of adsorption. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction. 33024-60-1, Name is Tetrahydro-2H-pyran-4-amine hydrochloride, molecular formula is C5H12ClNO. In a Article，once mentioned of 33024-60-1, Synthetic Route of 33024-60-1
Aberrant activation of the MAPK pathway drives cell proliferation in multiple cancers. Inhibitors of BRAF and MEK kinases are approved for the treatment of BRAF mutant melanoma, but resistance frequently emerges, often mediated by increased signaling through ERK1/2. Here, we describe the fragment-based generation of ERK1/2 inhibitors that block catalytic phosphorylation of downstream substrates such as RSK but also modulate phosphorylation of ERK1/2 by MEK without directly inhibiting MEK. X-ray crystallographic and biophysical fragment screening followed by structure-guided optimization and growth from the hinge into a pocket proximal to the C-alpha helix afforded highly potent ERK1/2 inhibitors with excellent kinome selectivity. In BRAF mutant cells, the lead compound suppresses pRSK and pERK levels and inhibits proliferation at low nanomolar concentrations. The lead exhibits tumor regression upon oral dosing in BRAF mutant xenograft models, providing a promising basis for further optimization toward clinical pERK1/2 modulating ERK1/2 inhibitors.
If you are interested in 33024-60-1, you can contact me at any time and look forward to more communication.Synthetic Route of 33024-60-1
Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics