mk 2

MK 212 hydrochloride is a 5-HT2C receptor agonist

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 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.

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.

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.

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

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.

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-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.

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.

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

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)

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

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

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].

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

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