mk-2-in-1

MK2-IN-1 is a potent and selecitve MAPKAPK2(MK2) inhibitor(IC50=0.11 uM) with a non-ATP competitive binding mode.

Etoricoxib (MK-663) is a synthetic, nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic, and potential antineoplastic properties. Etoricoxib specifically binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in inhibition of the conversion of arachidonic acid into prostaglandins. Inhibition of COX-2 may induce apoptosis and inhibit tumor cell proliferation and angiogenesis.

MK-3207 is a highly potent and orally bioavailable small molecule antagonist of the calcitonin gene-related peptide (CGRP) receptor, demonstrating an in vitro IC50 of 0.12 nM and a Ki of 0.024 nM for the human receptor with exceptional selectivity over the related human AM1, AM2, CTR, and AMY3 receptors, though it exhibits lower affinity for CGRP receptors from other species such as canine and rodent; in vitro studies confirm its potent antagonism of human and rhesus monkey CGRP receptors (K(i) = 0.024 nM), and in vivo models show it produces a concentration-dependent inhibition of dermal vasodilation, requiring plasma concentrations of 0.8 nM and 7 nM to block 50% and 90% of the blood flow increase, respectively.

MK2-IN-1 hydrochloride (MK 25) is a highly selective, non-ATP competitive inhibitor of p38 mitogen-activated protein kinase-activated protein kinase 2 (MAPKAPK2 or MK2, IC50: 0.11 μM) [1].

MK-8666 Tris is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 Tris has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.

MK-8666 is a partial GPCR (G-protein-coupled receptor) agonist that is coordinated with the action of GPR40. GPR40, also known as free fatty acid (FFA) receptor 1 modulates fatty acid-induced insulin secretion in pancreatic beta cells and in intestinal enteroendocrine cells. Thus, MK-8666 has been investigated for treatment of type 2 diabetes mellitus and has been shown to robustly lower glucose without negative effects.

Ganoderic acid Mk (GA-Mk), a triterpenoid acid derived from Ganoderma lucidum mycelia, exhibits potent anti-proliferative properties and can induce apoptosis in HeLa cells through a mitochondria-mediated pathway, making it significant for cervical cancer research [1] [2].

Dalotuzumab (MK-0646) is a recombinant humanized IgG1 monoclonal antibody that specifically targets the insulin-like growth factor 1 receptor (IGF-1R). its mechanism of action involves the inhibition of IGF-mediated oncogenic signaling, which subsequently induces apoptosis and cell cycle arrest in tumor cells, and it has demonstrated enhanced antitumor efficacy when used in combination with other chemotherapeutic agents.

MK-2206 free base is a potent, selective, and orally administered allosteric Akt inhibitor with IC50 values of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. It demonstrates sensitivity in various breast cancer cell lines, including those with PIK3CA mutations and PTEN loss, indicating its potential for anticancer activities [1] [2].

Favezelimab (MK-4280), a humanized monoclonal antibody directed against LAG-3, inhibits the molecular interaction between LAG-3 and its ligand MHC class II, thereby restoring T-cell function. Favezelimab (MK-4280) has been evaluated as a candidate for colorectal cancer (CRC) research, particularly in studies that investigate synergistic effects in combination with the PD-L1 inhibitor Pembrolizumab (HY-P9902).

Timolol hemimaleate ((S)-L-714,465; MK 950), a β-blocker, is formulated for both systemic and topical use. It is commonly applied topically to decrease intraocular pressure in cases of open-angle glaucoma and ocular hypertension. Additionally, it is utilized in research for the treatment of infantile hemangiomas, hypertension, myocardial infarction, migraine prophylaxis, and atrial fibrillation. Moreover, Timolol has been recognized for its cardioprotective effects [1] [2].

Etoricoxib (Standard) is the standard substance of Etoricoxib, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Etoricoxib (MK-663) is a synthetic, nonsteroidal anti-inflammatory drug (NSAID) with antipyretic, analgesic, and potential antineoplastic properties. Etoricoxib specifically binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in inhibition of the conversion of arachidonic acid into prostaglandins. Inhibition of COX-2 may induce apoptosis and inhibit tumor cell proliferation and angiogenesis.