mk-2

MK2-IN-3 hydrate (MK-2 Inhibitor III) is an orally active, selective, and ATP-competitive inhibitor of MAPKAP-K2 (MK-2) (IC50 of 0.85 nM)

MK-8353 (SCH900353) is a potent, selective, and orally available inhibitor of ERK1 2 with IC50 values of 23.0 nM and 8.8 nM, respectively.

Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.

Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent DPP-IV inhibitor with an IC50 of 19 nM in Caco-2 cell extracts.

Rofecoxib (MK 966) binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. Rofecoxib is a synthetic, nonsteroidal derivative of phenyl-furanone with anti-inflammatory, antipyretic and analgesic properties and potential antineoplastic properties. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2.

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.

Emamectin Benzoate (MK-244), by binding gamma-aminobutyric acid (GABA) receptor and glutamate-gated chloride channels disrupting nerve signals within arthropods, acts as a chloride channel activator.

MK-4827 Racemate (Niraparib Racemate) is a selective PARP1 and PARP2 inhibitor with IC50s of 3.8 nM and 2.1 nM, respectively, over 330-fold selectivity for PARP3, V-PARP and Tank1.

MK-0941 free base is an orally active glucokinase activator with potent glucose-lowering activity, making it a potential therapeutic agent for type 2 diabetes.

MK-571 sodium (L-660711 sodium salt) is a selective, orally active antagonist of the CysLT1 receptor. MK-571 sodium is a multidrug resistance protein-2 (ABCC2, Mrp2) inhibitor used to demonstrate the role of Mrp2 in the cellular efflux of drugs, xenobiotics, and their conjugates. MK-571 sodium can inhibit the synthesis of K-4′-O-GlcA (19.7 μM). MK571 dose-dependently inhibits the intracellular biosynthesis of all flavonol sulphates and glucuronides by Caco-2 cells. MK-571 sodium significantly inhibits phase-2 conjugation of kaempferol by cell-free extracts of Caco-2, and production of kaempferol-4′-O-glucuronide was competitively inhibited. In addition to inhibiting MRP2, MK571 is a potent inhibitor of enterocyte phase-2 conjugation.

Navarixin (MK-7123)(SCH527123) is a novel, selective CXC chemokine receptor 2(CXCR2) antagonist that inhibits neutrophil activation and modulates neutrophil trafficking in animal models, characteristics that may be beneficial in the treatment of conditions with unbalanced pulmonary neutrophilia.

Birabresib (MK-8628) is a synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity.

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

MK2-IN-3 (MK2 Inhibitor III) is a potent, cell-permeable inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) and can be used for the treatment of rheumatoid arthritis

MK-3697, an isonicotinamide small molecule, acts as a potent and selective Orexin 2 receptor antagonist (Ki: 0.95 nM).

Mk-0533 is a selective peroxisome proliferator-activated receptor gamma modulator for the treatment of type 2 diabetes mellitus.

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.

Ascr#2 (asc-C6-MK) is a glycoside analogue in Cryptococcus hidradii that promotes dauer formation.Ascr#2 mixtures with ascr#3 at low concentrations act as a male elicitor and can be used to detect population density.Ascr#5 (asc-ωC3) is a highly conserved ascaroside analogue in Cryptococcus hidradii that regulates a variety of responses in Cryptococcus hidradii.

MK 1903 is a potent and selective complete agonist for the hydroxy-carboxylic acid receptor 2 (HCA2). HCA2 is also known as G protein-coupled receptor 109A(GPR109A). MK 1903 reduced Foschlin-induced cAMP production in uniform time-resolved fluorescence (htf) measurements using CHO cells expressing the human receptor (ECso-12.9 nM).

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 Hydrochloride (MK-3207 HCl) is a potent CGRP receptor antagonist with IC50 and Kiof 0.12 nM and 0.022 nM, highly selective versus human AM1, AM2, CTR, and AMY3. Phase 2.

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].

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].

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

Reveromycin A is the major component of a complex of spiroketal antibiotics isolated from Streptomyces sp. It inhibits the mitogenic activity of epidermal growth factor in Balb MK cells (IC50 = 0.7 μg ml), displays antiproliferative activity against human KB and K562 tumor cell lines (IC50s = 1.9 and 1.6 μg ml, respectively), and demonstrates antifungal activity against C. albicans (MIC = 2 μg ml at pH 3). Reveromycin A also has been shown to inhibit bone resorption by inducing apoptosis in osteoclasts with an IC50 value of 0.7 μM.

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.

MK-8133 is an antagonist of orexin-2 selective receptor with favorable development properties.

MK-0941 is an orally active and allosteric glucokinase activator, has potential in the treatment of type 2 diabetes.

MK-8282 is an effective G-Protein-Coupled Receptor 119 agonist for the treatment of Type 2 Diabetes.

MK-0703 is a selective cyclooxygenase-2 inhibitor.

MK 0767 is a dual peroxisome proliferator-activated receptor (PPAR) α/γ agonist that has been investigated as a potential treatment for type 2 diabetes and dyslipidemia.

Fludalanine (MK641), an analogue of D-alanine, irreversiably inactivates racemase and also inhibits synthase. When used in combination with cycloserine, it has been found to be more active against a variety of non-mycobacterium organisms than fludalanine

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].

Reveromycin D is a bacterial metabolite originally isolated from Streptomyces. It inhibits EGF-induced mitogenic activity in Balb MK cells and exhibits pH-dependent antifungal activity against C. albicans [MICs = 2 and >500 μg ml at pH 3 and 7.4, respectively]. Reveromycin D also inhibits the proliferation of KB and K562 cells [IC50s = 1.6 and 1.3 μg ml, respectively].

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.

Agitoxin-2 TFA, a potent inhibitor of K+ channels, exhibits IC50 values of 201 pM and 144 pM for mK V 1.3 and mK V 1.1, respectively [1] [2].

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).