mc4

MC4 is a first-in-class inhibitor of ribosomal RNA synthesis with antimicrobial activity against Staphylococcus aureus.

DLIN-MC4-DMA is a lipid membrane and is a potential nucleic acid carrier.

MC4355 is a dual inhibitor of EZH2 and histone deacetylase (HDAC).

MC4343, a potent dual inhibitor targeting both EZH2 and histone deacetylase, presents promising potential for cancer research applications.

MC4033 is a selective lysine acetyltransferase 8 (KAT8) inhibitor (IC50: 12.1 μM) with anticancer effects, induces apoptosis, and can be used for the study of non-small cell lung cancer.

MC4171 is a selective KAT8 inhibitor with antiproliferative activity and can be used to study cancer.

mC46 (C46) peptide is a membrane-associated fusion peptide inhibitor that effectively impedes the replication and entry of HIV-1. Additionally, mC46 peptide can inhibit CCR5-tropic, CXCR4-tropic, and dual-tropic HIVs, as well as SIV and SHIV.

Ritlecitinib, also known as PF-06651600, is a potent and selective JAK3 inhibitor. PF-06651600 is a potent and low clearance compound with demonstrated in vivo efficacy. The favorable efficacy and safety profile of this JAK3-specific inhibitor PF-06651600 led to its evaluation in several human clinical studies. JAK3 was among the first of the JAKs targeted for therapeutic intervention due to the strong validation provided by human SCID patients displaying JAK3 deficiencies.

PF-07258669 is a selective melanocortin 4 receptor (MC4) antagonist used in the study of cachexia and loss of appetite.

[D-Trp8]-γ-MSH acetate(321351-81-9 free base) is a selective melanocortin 3 (MC3) receptor agonist (IC50 values are 6.7, 340 and 600 nM for human MC3, MC5 and MC4 receptors respectively) and displays anti-inflammatory efficacy.

HS 014 acetate is a potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central

melanocortin MC4 receptor antagonist

MCL0129, a selective and non-peptidergic melanocortin 4 (MC4) receptor antagonist, is a potential treatment for cachexia.

PF-446687 is a highly selective MC4 receptor (MC4R) agonist.

PG-931 TFA, a potent and selective agonist of the melanocortin 4 (MC4) receptor (IC50=0.58 nM) compared to the hMC3R (IC50=55 nM) and hMC5R (IC50=2.4 nM), is an analog of SHU 9119. This compound has demonstrated efficacy in reversing hemorrhagic shock and preventing multiple organ damage in vivo [2].

JKC363 TFA is a selective melanocortin MC4 receptor antagonist that exhibits a 90-fold higher affinity for the MC4 receptor (IC50=0.5 nM) compared to the MC3 receptor (44.9 nM). This compound effectively inhibits the α-MSH-induced stimulation of TRH release. It also demonstrates an anti-hyperalgesic effect [1] [2].

γ1-MSH TFA, a melanocortin MC3 receptor agonist, demonstrates a binding affinity (K i) of 34 nM for the rat MC3 receptor. Notably, it exhibits approximately 40-fold greater selectivity for the MC3 receptor compared to the MC4 receptor, with a K i of 1318 nM for MC4 [1].

HS024, a selective MC4 receptor antagonist, exhibits affinity with Ki values of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1 receptors, respectively. This compound has been shown to increase food intake [1].

HS014 TFA, a potent and selective antagonist of the melanocortin-4 (MC4) receptor, exhibits K i values of 3.16, 108, 54.4, and 694 nM for the human MC4, MC1, MC3, and MC5 receptors, respectively. It effectively increases food intake in free-feeding rats [1] [2].

Fmoc-Aeg(N3)-OH is a click chemistry reagent characterized by its azide group that participates in copper-catalyzed azide-alkyne cycloaddition reactions (CuAAc) with molecules containing alkyne groups. This building block, which also reacts in strain-promoted alkyne-azide cycloaddition (SPAAC) with DBCO or BCN group-containing molecules, facilitates the alteration of cytotoxicity through the creation of peptidomimetics such as Cilengitide, Piscidin 1, and MC3, MC4, MC5 receptor agonists. Its incorporation in molecules can lead to conformational restraint in peptidic structures due to amidic nitrogen alkylation, which results in structures such as N-methylated peptides, allows backbone derivatization, and enables the design of macrocycles through intramolecular cross-linking or stabilization of the main chain by intramolecular cyclization. Fmoc-Aeg(N3)-OH is a potential cornerstone for the construction of custom peptide nucleic acids (PNAs) and peptide synthesis.

β-Melanocyte Stimulating Hormone (MSH), human (Synonyms: Beta-MSH (1-22) (human)) β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

beta-MSH, human is an endogenous peptide hormone and neurotransmitter produced by pro-opiomelanocortin (POMC), and is also an agonist of MC4-R (melanocortin 4 receptor).

Beta-MSH (1-22) (human) acetate (Beta-MSH (1-22) (human) acetate (17908-57-5 Free base)) , is an endogenous melanocortin-4 receptor (MC4-R) agonist.

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist (IC50 values are 11.63, 1115, and >10,000 nM at MC4, MC3, and MC1 receptors, respectively). It significantly reverses stress-induced anorexia without affecting food intake in free-feeding rats and exhibits anxiolytic-like activity in vivo.