peptide-competitive

A-366 is a highly selective peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP, respectively.It is more than 1,000-fold selective for G9a and GLP over the other 21 methyltransferases. It is an inhibitor of the Spindlin1-H3K4me3 interaction with an IC50 of 182.6 nM.It exhibits high affinity for human H3R with a Ki value of 17 nM, and shows subtype selectivity between subgroups of the histaminergic and dopaminergic receptor families.

Semaglutide is a long-acting, selective, competitive GLP-1R agonist and a long-acting analog of human glucagon-like peptide-1, exhibiting potent hypoglycemic, weight-loss, cardioprotective, and neuroprotective effects. Upon activation of the GLP-1R, semaglutide promotes insulin secretion, inhibits gastric emptying and appetite, while also enhancing autophagy and suppressing oxidative stress and apoptosis. Semaglutide also plays a role in regulating mitochondrial function and lipid metabolism. Semaglutide is being investigated for use in type 2 diabetes, obesity, Parkinson’s disease, metabolic and fatty liver diseases (MASLD), and other neurodegenerative and liver diseases, as well as in cancer research.

Semaglutide Acetate is a GLP-1R agonist (EC50=6.2 pM) with long-acting, selective, competitive, and oral efficacy. Semaglutide acetate can be used in the study of type 2 diabetes.

Avexitide (Exendin-3(9-39)amide) is a specific, competitive GLP-1 receptor antagonist (Ki = 0.36 nM). Avexitide binds to the GLP-1 receptor (GLP-1R) with high affinity (Kd = 0.42 nM), blocking the interaction between endogenous GLP-1 and the receptor, thereby counteracting the effects of excessive GLP-1 secretion. Avexitide is being studied for post-bariatric hypoglycemia (PBH) and congenital hyperinsulinism.

Aptiganel (CNS-1102) is a non-competitive NMDA antagonist, a peptide that may be used to study acute ischemic stroke.

N-Acetylglycine is a minor constituent of food that is not genotoxic or acutely toxic and is capable of being used in biological studies of mimetic peptides.N-Acetylglycine acts as a blocker of the N-terminus of a peptide.3-Hydroxyanthranilic acid is a competitive succinate dehydrogenase inhibitor.

[D-p-Cl-Phe6,Leu17]-VIP acetate is a competitive and selective antagonist of vasoactive intestinal peptide (VIP) receptor (IC50 = 125.8 nM).

Peptide T acetate is an octapeptide from the V2 region of HIV-1 gp120. Peptide T is a synthetic octapeptide whose possible mechanism of action is the competitive inhibition of gp120 to the CD4 receptor as well as binding to vasointestinal peptide receptors and inhibiting cytokine action

Degarelix is a peptide and selective GnRH (human gonadotropin-releasing hormone) receptor antagonist that treats prostate cancer by lowering testosterone levels in the body.

Gosogliptin is a potent, orally active, highly selective and competitive inhibitor of DPP-4 (dipeptidyl peptidase 4), increasing the levels of intestinal glucagon peptide (GLP-1) and glucose-dependent proinsulinotropic polypeptide (GIP), thereby enhancing insulin secretion and lowering blood glucose levels. In animal studies, Gosogliptin rapidly, orally and reversibly inhibits plasma DPP-4 activity.

Devazepide is a competitive, selective, orally available non-peptide CCK1 (cholecystokinin 1) receptor antagonist that inhibits bladder cancer cell proliferation and migration while inducing apoptosis and cell cycle arrest.

GLP-1R Antagonist 1 is an orally active, CNS penetrant and non-competitive glucagon-like peptide 1 receptor (GLP-1R) antagonist (IC50: 650 nM).

Z-Ile-Leu-aldehyde is an effective and competitive peptide aldehyde inhibitor of γ-secretase and notch.

KARI 201 hydrochloride is a selective, brain-penetrant, competitive inhibitor of acid sphingomyelinase (ASM) with an IC50 of 338.3 nM. It also acts as an agonist for the growth hormone-releasing peptide receptor (ghrelin receptor). Additionally, KARI 201 hydrochloride can enhance the neuropathological features of Alzheimer's disease.

VHL Ligand 38 (Compound 1) is a competitive inhibitor of the E3 ubiquitin ligase VHL, demonstrating IC50 values of 4.1 μM and 7.0 μM in 1% and 10% DMSO solutions, respectively. It features a hydroxyproline residue and an isoxazole acetamide moiety, and effectively inhibits the binding of the fluorescence peptide derived from HIF1α (FAM-DEALA-Hyp-YIPD) to VHL.

Rimegepant (BMS-927711) hemisulfate is a potent, orally active selective competitive antagonist of the calcitonin gene-related peptide (CGRP) receptor, with a Ki of 0.027 nM and an IC50 of 0.14 nM for the hCGRP receptor. Rimegepant hemisulfate is utilized in migraine research.

GSK172981 is a non-peptide tachykinin NK3 receptor antagonist with a high affinity for the recombinant human (PK (I) value 7.7) and native guinea pig (PK (I) value 7.8) tachykinin NK3 receptor. In vitro, the functional evaluation showed that GSK172981 was

SN52 is a powerful, competitive, and cell-permeable inhibitor of NF-κB2. It is a variant of the SN50 peptide. SN52 effectively prevents the nuclear translocation of p52-RelB heterodimers, exhibiting a robust radiosensitization effect on prostate cancer cells. This compound holds significant potential for cancer research purposes.

HXR9 is a cell-permeable peptide that acts as a competitive antagonist of the HOX/PBX interaction, effectively inhibiting the binding between HOX proteins and the transcription factor PBX in paralogue groups 1 to 8. HXR9 selectively impairs cell proliferation and induces apoptosis in cells with high expression of the HOXA/PBX3 genes (e.g., MLL-rearranged leukemic cells).

AZ8838 is an effective, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pK i of 6.4 for hPAR2 [1].

L-365260 hemihydrate is a selective, orally active non-peptide gastrin and brain cholecystokinin receptor (CCK-B) antagonist, demonstrating competitive interaction with guinea pig stomach gastrin and brain CCK receptors and exhibiting inhibition constants (Kis) of 1.9 nM and 2.0 nM, respectively.

OK-1035 is a potent and selective DNA-PK inhibitor. When a synthetic peptide was used as a substrate, OK-1035 caused 50% inhibition of DNA-PK activity at 8 microM. OK-1035 inhibited the phosphorylation by DNA-PK of consensus peptide as well as that of recombinant human wild type-p53. Kinetic studies indicated that OK-1035 inhibited DNA-PK activity in an ATP-competitive manner.

NBI-42902 is a potent inhibitor of peptide radioligand binding to the human GnRH receptor (K(i) = 0.56 nm). Tritiated NBI-42902 binds with high affinity (K(d) = 0.19 nm) to a single class of binding sites and can be displaced by a range of peptide and nonpeptide GnRH receptor ligands. In vitro experiments demonstrate that NBI-42902 is a potent functional, competitive antagonist of GnRH stimulated IP accumulation, Ca(2+) flux, and ERK1/2 activation. It did not stimulate histamine release from rat peritoneal mast cells. Finally, it is effective in lowering serum LH in castrated male macaques after oral administration. Overall, these data provide a benchmark of pharmacological characteristics required for a nonpeptide GnRH antagonist to effectively suppress gonadotropins in humans and suggest that NBI-42902 may have clinical utility as an oral agent for suppression of the hypothalamic-pituitary-gonadal axis. (source: Endocrinology. 2007 Feb;148(2):857-67. Epub 2006 Nov 9.)

Y27632 HCl hydrate is an orally effective, ATP-competitive ROCK1/ROCK2 inhibitor (Ki=220 nM/300 nM) that inhibits caspase-3 and suppresses stem cell apoptosis induced by multiple conditions. It is suitable for studying induced pluripotent stem cell (iPSC) culture.