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-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].

MK-3207 is a potent and orally bioavailable CGRP receptor antagonist (IC 50 = 0.12 nM; K i = 0.024 nM); highly selective versus human AM1, AM2, CTR, and AMY3. IC50 Value: 0.024 nM (Ki, Human CGRP) [1] As other CGRP receptor antagonists, MK-3207 shows a lower affinity for human CGRP receptors from other species, including canine and rodent. in vitro: MK-3207 is a potent antagonist of the human and rhesus monkey CGRP receptors (K(i) = 0.024 nM). in vivo: MK-3207 produced a concentration-dependent inhibition of dermal vasodilation, with plasma concentrations of 0.8 and 7 nM required to block 50 and 90% of the blood flow increase, respectively. The tritiated analog [3H]MK-3207 was used to study the binding characteristics on the human CGRP receptor. [3H]MK-3207 displayed reversible and saturable binding (K(D) = 0.06 nM), and the off-rate was determined to be 0.012 min(-1), with a t(1 2) value of 59 min [1]. After the first interim analysis, the two lowest MK-3207 doses (2.5, 5 mg) were identified as showing insufficient efficacy. Per the pre-specified adaptive design decision rule, only the 2.5-mg group was discontinued and the five highest doses (5, 10, 20, 50, 100 mg) were continued into the second stage [2]. Clinical trial: MK-3207 for the treatment of acute migraines. Phase 2b

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.

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.

Dalotuzumab (MK-0646) is a humanized recombinant monoclonal antibody (IgG1 type) that targets IGF-1R, inhibiting tumor cell proliferation, IGF-1R autophosphorylation, and Akt phosphorylation mediated by IGF-1 and IGF-2. It induces apoptosis and cell cycle arrest, and its antitumor activity is significantly enhanced when used alongside other anticancer agents like statins, both in vitro and in vivo [1] [2] [3].

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].

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].

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].

Favezelimab (MK-4280) is a humanized anti-LAG-3 monoclonal antibody that inhibits the LAG-3 MHC class II interaction and shows potential for use in colorectal cancer (CRC) research, particularly when combined with the PD-L1 inhibitor pembrolizumab [1][2].