peptide-competitive

A-366 是一种高选择性的肽竞争性组蛋白甲基转移酶 G9a 抑制剂，对 G9a 和 GLP 的 IC50分别为 3.3 和 38 nM。它比其他 21 种甲基转移酶具有 1000 倍以上的选择性。它是 Spindlin1-H3K4me3相互作用的抑制剂，IC50为182.6 nM。它对人 H3R 表现出很高的亲和力，Ki 值为 17 nM，在组胺能和多巴胺能受体家族的亚群间表现出亚型选择性。

Avexitide (Exendin-3 (9-39) amide) 是一种特异竞争性的glucagon-like peptide-1 (GLP-1)受体拮抗剂。

Aptiganel (CNS-1102) 是一种非竞争性 NMDA 拮抗剂，是一种多肽，可用于研究急性缺血性卒中。

N-Acetylglycine 是一种食物中的少量成分，无基因毒性和急性毒性，能够用于模拟肽的生物研究。N-Acetylglycine 可充当一种多肽的 N 端的阻断剂。

[D-p-Cl-Phe6,Leu17]-VIP acetate 是一种竞争性和选择性的血管活性肠肽 (VIP) 受体拮抗剂 (IC50 = 125.8 nM)。

MLCK inhibitor peptide 18 acetate(224579-74-2 free base) 是肌球蛋白轻链激酶的选择性竞争性抑制剂 (IC50 = 50 nM)。显示出比 CaM 激酶 II 高 4000 倍的选择性，并且不抑制 PKA。细胞可渗透。

Peptide T acetate(106362-32-7 free base) 是一种来自 HIV-1 gp120 V2 区域的八肽。它是一种合成八肽，其可能的作用机制是 gp120 对 CD4 受体的竞争性抑制以及与血管肠肽受体的结合和抑制细胞因子作用。

Gosogliptin（戈格列汀）是一种有效的口服活性、高度选择性和竞争性的DPP-4（二肽基肽酶4）抑制剂，提高肠促胰岛素肽(GLP-1)和葡萄糖依赖性促胰岛素多肽（GIP）的水平，从而增强胰岛素分泌并降低血糖水平。在动物实验中，Gosogliptin能够快速可逆地抑制血浆DPP-4活性。

GLP-1R Antagonist 1 (compound 5d) 是口服有效的、能透过中枢神经系统的，胰高血糖素样肽 1 受体 (GLP-1R) 的非竞争性抑制，其 IC50 值为 650 nM。

GR 159897 is a competitive, brain-penetrated non-peptide NK2 receptor antagonist with anti-tumor effects. GR 159897 inhibits binding of [3H]GR100679 to human NK2-CHO cells and rat colon membranes (pKis: 9.51 and 10, respectively). It can antagonize bronch

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

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. It effectively inhibits the binding between HOX proteins and the transcription factor PBX, specifically in paralogue groups 1 to 8. HXR9 selectively impairs cell proliferation and induces apoptosis in cells with a high expression of the HOXA PBX3 genes, for instance, MLL-rearranged leukemic cells.

AZ8838 是一种有效的、竞争性的、变构的、口服活性的 PAR2非肽小分子拮抗剂，其对 hPAR2 的 pKi 值为 6.4。

L-365260 hemihydrate 是选择性的、具有口服活性的非肽胃泌素和脑胆囊收缩素受体 (CCK-B) 拮抗剂，Kis 值分别为 1.9 nM 和 2.0 nM。L-365260 hemihydrate 以竞争性方式与豚鼠胃泌素和脑 CCK 受体相互作用。

ERAP2-IN-1 (compound 61) 是一种 ERAP2 的非竞争性抑制剂。ERAP2-IN-1 特异性抑制 ERAP2 肽水解活性，抑制 Arg-AMC 水解作用 (IC50: 27 μM) 和模型肽的水解活性 (IC50: 44 μM)。

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.)

BIIE-0246 is a potent, selective and competitive non-peptide antagonist for the neuropeptide Y Y2 receptor. BIIE-0246 displays > 650-fold selectivity over Y1, Y4 and Y5 receptors.

Rimegepant, also known as BMS-927711 and BHV-3000, is a potent, selective, competitive, and orally active calcitonin gene-related peptide (CGRP) antagonist in clinical trials for treating migraines. Rimegepant has shown in vivo efficacy without vasoconstriction effect. BMS-927711 is superior to placebo at several different doses (75 mg, 150 mg, and 300 mg) and has an excellent tolerability profile.

S 8308 is a weak, but specific and competitive, non-peptide antagonist of AII exerting its inhibitory action at the receptor level.

Nonapeptide-1 (Melanostatine-5) acetate salt，一种多肽类激素，是 MC1R 选择性拮抗剂 (Ki: 40 nM)。 Nonapeptide-1 acetate salt 是一种竞争性的α-MSH 拮抗剂，可有效抑制黑素细胞中 α-MSH 诱导的细胞内 cAMP 和黑素体扩散 (IC50分别为 2.5 nM 和 11 nM)。 Nonapeptide-1 acetate salt 抑制黑色素合成，可用于研究皮肤色素沉着和肾上腺类固醇生成的调节、皮肤癌。

PKI(5-24) TFA 是一种强效、竞争性、合成的PKA(cAMP 依赖性蛋白激酶) 抑制剂，Ki 为 2.3 nM。PKI(5-24) TFA 对应于天然存在的热稳定蛋白激酶抑制剂中的 5-24 残基。