mk-1

MK-1-907 is a potential bioactive agent. No further details yet.

MK-1064 (Urokinase inhibitor 1) is a selective orexin 2 receptor antagonist (2-SORA).

Pembrolizumab (MK-3475) is a humanized monoclonal antibody inhibiting the PD-1 receptor and the first in the class of agents called the HER2 dimerization inhibitors that impairs the ability of HER2 to bind to other members of the HER family.

Fosaprepitant dimeglumine (MK-0517) is the dimeglumine salt form of fosaprepitant, a water-soluble, N-phosphorylated prodrug of aprepitant with antiemetic activity. Upon intravenous administration and rapid conversion to aprepitant, this agent selectively binds to human substance P neurokinin 1 (NK1) receptors in the central nervous system (CNS), inhibiting receptor binding of endogenous substance P and preventing substance P-induced emesis.

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.

Ivermectin (MK-933) is an activator of glutamate-gated chloride channels (GluCls) with antiparasitic activity.

MK-8033 hydrochloride is an effective and orally active dual inhibitor of ATP competitive c-Met/Ron, with 1 nM for c-Met and 7nM for Ron IC50. MK-8033 hydrochloride has a high affinity for activated kinase conformation, and is suitable for the study of breast cancer, bladder cancer, and non-small cell lung cancer (NSCLC).

Vorapaxar (MK-5348) (SCH 530348) is an effective and orally active thrombin receptor (PAR-1) antagonist (Ki: 8.1 nM).

Omarigliptin is a potent and selective oral dipeptidyl peptidase 4 (DPP4) inhibitor with IC50 value of 1.6 nM. [3]

Doravirine (MK-1439) is a non-nucleoside reverse transcriptase inhibitor used for the treatment of HIV AIDS.

SCH900776 (MK-8776) is an agent targeting cell cycle checkpoint kinase 1 (Chk1) with potential radiosensitization and chemosensitization activities.

MK-886 (L 663536) is an inhibitor of leukotriene biosynthesis, acting by inhibiting the 5-lipoxygenase-activating protein (FLAP), and serves as a moderately potent PPARα antagonist.

MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1 2 3 (IC50: 1.0 1.0 14 nM).

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-4101, an effective inhibitor of the Hedgehog pathway, has anti-tumor activity through the induction of extensive apoptosis and inhibition of proliferation in tumor cells.

Islatravir (MK-8591) is an effective anti-HIV-1 agent. It acts as a nucleoside reverse transcriptase inhibitor (EC50s: 0.068 nM, 3.1 nM, and 0.15 nM for HIV-1 (WT), HIV-1 (M184V), HIV-1 (MDR), respectively).

MK-9470 is a selective, high-affinity reverse agonist and is also a fluorine 18 labeled positron emission tomography (PET) radiotracer [(18) F]. The MK-9470 has been used to image cannabinoid receptor type 1 in healthy and ill human brains.

MK-8245 trifluoroacetate is a phenoxy piperidine isoxazole derivative functioning as a potent, liver-targeting stearoyl-CoA desaturase (SCD) inhibitor, demonstrating significant anti-diabetic and anti-dyslipidemic effects. It showcases high specificity and efficacy against SCD1 across various species, with IC50 values of 1 nM for human SCD1 and 3 nM for both rat and mouse SCD1. MK-8245's mechanism includes a tetrazole acetic acid moiety that facilitates liver-targeting through OATPs recognition. Its inhibition potency in rat hepatocyte assays (IC50 of 68 nM) surpasses that in HepG2 cell assays devoid of active OATPs (IC50 of ~1 μM), highlighting its liver specificity. Moreover, MK-8245 exhibits over 100,000-fold selectivity against Δ-5 and Δ-6 desaturases in comparative assays. In vivo studies reveal MK-8245's preferential liver distribution in mice, rats, dogs, and rhesus monkeys, underscoring its potential for minimizing adverse effects in non-target tissues. Additionally, its administration in eDIO mice before glucose challenges significantly improves glucose clearance, indicating its therapeutic promise in diabetes management.

MK-0916 is a 11β-hydroxysteroid dehydrogenase type 1 inhibitor indicated for the treatment of type 2 diabetes and metabolic syndrome as well as obesity-related diseases.

MK-8457 is a dual inhibitor of SYK and ZAP70, valuable for rheumatoid arthritis research [1].

MK-1468, a highly selective and brain-penetrant LRRK2 inhibitor, exhibits an IC50 of 0.8 nM and is utilized in the study of Parkinson's disease [1].

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-5204, an orally active β-1,3-glucan synthesis inhibitor, impedes the synthesis of β-1,3-glucan [1].

MK-0736 hydrochloride is a potent and selective 11β-HSD-1 inhibitor.

Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor with an IC50 of 4.2 nM for type II 5α-reductase, demonstrating approximately 100-fold higher affinity for type II than type I. Finasteride acetate can be used for research on benign prostatic hyperplasia (BPH) and androgenic alopecia [1] [2] [3].

Verubecestat tosylate, also known as MK-8931 or SCH 900931, is a potent and selective beta-secretase inhibitor, and BACE1 protein inhibitor or Beta-site APP-cleaving enzyme 1 inhibitor. Verubecestat tosylate is a promising novel therapeutic drug candidate in Alzheimer's disease. Verubecestat tosylate reduced Aβ cerebral spinal fluids (CSF) levels up to 92% and was well tolerated by patients.

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].

Verubecestat (MK-8931) (MK-8931) is an effective and specific β-secretase inhibitor and β-site APP-cleaving enzyme 1 inhibitor or BACE1 protein inhibitor.

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].

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].

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-8033 is a new and selective dual ATP competitive c-Met Ron inhibitor (IC50: 1 nM Wt c-Met).

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

Sulindac (sodium) (MK-231) is an orally active nonsteroidal anti-inflammatory agent. Sulindac (sodium) is used to reduce pain, swelling, and joint stiffness from arthritis. Sulindac is also used for the research of arthritis of the spine, gouty arthritis. Sulindac (sodium), as an immunomodulatory agent, can downregulate PD-L1 through the blockade of NF-κB signaling and modulates the response of pMMR colorectal cancer (CRC) to anti-PD-L1 immunotherapy, inhibits the development and progression of colorectal cancer CRC. Sulindac (sodium) also inhibits TGF-β1- induced epithelial-mesenchymal transition (EMT) and suppresses lung cancer cell migration and invasion via downregulation of SIRT1 [1] [2].

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.

BTL-MK (Compound 19) is an orally active antiallergic agent that inhibits degranulation of mast cells with an IC50 of 6.7 μM by binding to the inhibitory receptor FcγRIIB. BTL-MK improves metabolic stability in human liver microsomes and ameliorates the allergic response in an Ovalbumin-induced food allergy mice model. It exhibits good pharmacokinetic characteristics with metabolic stability [1].

MK-1084, a selective KRAS G12C inhibitor, is currently in a Phase I clinical trial (NCT05067283). It demonstrates anticancer activity and can be utilized alone or in combination with pembrolizumab for cancer research [1].

Grazoprevir (MK-5172) is a nitrogenous macrocyclic compound used as an inhibitor of the hepatitis C virus NS3 4A protease. Grazoprevir is commonly combined with elbasvir for treating chronic HCV genotype 1 or 4 infections in adults.

Ertapenem sodium (MK-826) is a new long-acting 1-β-methyl carbapenem antibiotic with a broad antibacterial spectrum including common aerobic and anaerobic bacteria and organisms with extended-spectrum β-lactamases.

(5Alpha)-23-methyl-4-aza-21-norchol-1-ene-3,20-dione is a bioactive chemical.

Taranabant (MK-0364) is a selective and potent cannabinoid 1 (CB1) receptor inverse agonist used in the study of obesity and nicotine dependence.

iMDK quarterhydrate, a potent PI3K inhibitor, is effective in inhibiting the growth factor MDK (also known as midkine or MK) while demonstrating suppression of non-small cell lung cancer (NSCLC). In combination with a MEK inhibitor, iMDK quarterhydrate demonstrates cooperative inhibition of NSCLC without causing harm to normal cells and mice [1].

MK-8245 is a liver-targeting SCD inhibitor for human SCD1 (IC50: 1 nM) and for rat/mouse SCD1 (IC50: 3 nM), with anti-diabetic and anti-dyslipidemic function.

MK-8527, an HIV inhibitor and nucleoside reverse transcriptase translocation inhibitor (NRTTI), exhibits a similar inhibitory mechanism to ISL [1].

Quavonlimab (MK-1308) is a novel antibody targeting CTLA-4 [1].

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].

Compound 8 (5-HT6R antagonist 1), a 5-HT6R antagonist (K i : 5 nM), not only demonstrates inhibition of platelet aggregation and excellent metabolic stability but also reverses MK-801-induced memory impairments in rats, suggesting its utility in Alzheimer's disease (AD) research [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.

Potent Shaker K+ channel blocker (Ki = 0.64 nM). Also inhibits Kv1.3, Kv1.6 and Kv1.1 K+ channels (Ki values are 4, 37 and 44 pM respectively).