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Search Results for " peptide-competitive "

47

抑制剂 & 化合物

1

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Cat. No.	Product Name	Target	Signaling Pathways
T3624	A-366 A 366,A366	Epigenetic Reader Domain; Histone Methyltransferase	Chromatin/Epigenetic
	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。
T26645	Aptiganel CNS 1102,CNS-1102,CNS1102	NMDAR	Neuroscience
	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。
TP2100	Avexitide Exendin-3 (9-39) amide,Exendin (9-39),艾塞那肽	Glucagon Receptor	GPCR/G Protein
	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。
TP1523	PKG inhibitor peptide TFA (82801-73-8 free base) PKG inhibitor peptide TFA	PKA	Tyrosine Kinase/Adaptors
	PKG inhibitor peptide TFA (82801-73-8 free base) 是 ATP 竞争性 cGMP 依赖性蛋白激酶 (PKG) 的抑制剂。
TP2103L	[D-p-Cl-Phe6,Leu17]-VIP acetate	Others	Others
	[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)。
T78223	γ-Glu-Tyr gamma-Glutamyltyrosine,gamma-GLU-TYR
	γ-Glu-Tyr (gamma-Glutamyltyrosine) 是一种对二肽基肽酶-IV (DPP-IV) 具有竞争性抑制作用的 kokumi 肽，可用于研究糖尿病。
T15387	GLP-1R Antagonist 1	Glucagon Receptor	GPCR/G Protein
	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。
TP1887L1	[Ala107]-MBP (104-118) acetate [Ala107]-MBP (104-118) acetate(99026-77-4 free base)	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	[Ala107]-MBP (104-118) acetate ([Ala107]-MBP )(99026-77-4 free base) 是牛髓鞘碱性蛋白 (MBP) 的合成肽类似物。 PKC 的非竞争性抑制剂 (IC50 = 46 - 145 mM)。
TP1785L	Peptide T acetate(106362-32-7 free base)	Others; HIV Protease	Microbiology/Virology; Others; Proteases/Proteasome
	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。
TP1890L1	MLCK inhibitor peptide 18 acetate MLCK inhibitor peptide 18 acetate(224579-74-2 free base)	Serine/threonin kinase	Cell Cycle/Checkpoint; Metabolism
	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。
T8313	HCH6-1	Others	Others
	HCH6-1 是甲酰肽受体 1 的竞争性二肽拮抗剂。它能够抑制 fMLF (FPR1激动剂) 特异性激活的人中性粒细胞的趋化性、超氧阴离子生成和弹性酶释放。动物实验中，它对急性肺损伤具有保护作用，可用于研究 FPR1 参与的炎症性肺部疾病。
T8691	PD 168368 PD168368	Bombesin Receptor	GPCR/G Protein
	PD 168368 是一种新型有效且具有竞争性和选择性的非肽类神经调节蛋白 B 受体 (NMB-R) 拮抗剂，对胃泌素释放肽受体 (GRPR)具有抑制作用。PD 168368 是一种高效的 FPR1/FPR2/FPR3 的混合激动剂。
T71280	S 8308
	S 8308 is a weak, but specific and competitive, non-peptide antagonist of AII exerting its inhibitory action at the receptor level.
T69621	BIIE-0246 HCl
	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.
T17281	Z-Ile-Leu-aldehyde Z-IL-CHO,GSI-XII,γ-Secretase inhibitor XII	Others	Others
	Z-Ile-Leu-aldehyde is an effective and competitive peptide aldehyde inhibitor of γ-secretase and notch.
TP1888	[Ala113]MBP(104-118) [Ala113]-MBP (104-118)
	Synthetic peptide analog of bovine myelin basic protein (MBP). Non-competitive inhibitor of PKC (IC50 = 28 - 62 mM).
T81448	PKG inhibitor peptide TFA
	PKG inhibitor peptide TFA 是 ATP 竞争性抑制剂，具有 86 μM 的Ki值。
TP1887	[Ala107]MBP(104-118) [Ala107]-MBP (104-118)
	Synthetic peptide analog of bovine myelin basic protein (MBP). Non-competitive inhibitor of PKC (IC50 = 46 - 145 mM).
TP1785	Peptide T
	Peptide T 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 in
T38460	SN52
	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.
T60319	AZ8838
	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。
T68192	OK-1035
	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.
T70837	Rimegepant sulfate hydrate
	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.
T81817	Met-Arg-Phe-Ala
	Met-Arg-Phe-Ala为一种肽类化合物，同时作为脑啡肽生成内肽酶（EGE）的有效竞争性抑制剂，应用于神经系统疾病的研究。
TP1903	PKG inhibitor peptide cGMP Dependent Kinase Inhibitor Peptide
	Competitive inhibitor of cGMP-dependent protein kinase (PKG); analog of a substrate peptide corresponding to a phosphorylation site of histone H2B. Competes with synthetic substrates (Ki = 86 mM) but does not inhibit phosphorylation of intact histones by
T15415	GR 159897	Others	Others
	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
T41062	HXR9
	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.
T75878	Catestatin TFA
	Catestatin TFA，一个含有21个氨基酸残基、阳离子性疏水性肽，作为内源性肽，调节心脏功能及血压。它通过烟碱型乙酰胆碱受体(nAChRs)以非竞争性方式抑制儿茶酚胺释放，功能为烟碱类拮抗剂。
T32004	GSK172981 GSK 172981,GSK-172981
	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
T62039	L-365260 hemihydrate
	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。
T78003	[D-p-Cl-Phe6,Leu17]-VIP TFA
	[D-p-Cl-Phe6,Leu17]-VIP TFA，为竞争性及选择性血管活性肠肽(VIP)受体拮抗剂，其IC50为125.8 nM。该化合物针对胰高血糖素、促胰液素和GRF受体均不表现活性。
TP1989	NEP(1-40) Nogo-66 (1-40)
	Peptide fragment corresponding to residues 1 - 40 of Nogo-66, the domain of the myelin protein Nogo that inhibits axonal outgrowth. Acts as a competitive antagonist at the Nogo-66 receptor (NgR); blocks Nogo-66- and CNS myelin-induced inhibition of axonal
T75739	PKI(5-24) TFA
	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。
T75765	GRGDSPK TFA
	GRGDSPK TFA (EMD 56574 TFA) 是一种含有精氨酸-甘氨酸-天冬氨酸 (RGD) 序列的多肽。作为竞争性且可逆的抑制剂，它能够抑制整联蛋白与纤连蛋白的结合，用于探究整联蛋白在骨形成及吸收过程中的功能。
T80516	human GALP (3-32) Galanin-like peptide (3-32)	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	Human GALP (3-32) (Galanin-like peptide (3-32)) 是一种高效的galanin receptor激动剂。在竞争性结合实验中，该化合物对GalR1 (IC50=33 nM) 及GalR2 (IC50=15 nM) 表现出强烈亲和力。此外，human GALP (3-32) 显著增加了转染GalR2 (EC50=360 nM) 的 SH-SY5Y细胞的胞外酸化速率。
T75895	UFP-101 TFA
	UFP-101 TFA 是一种强效、选择性和竞争性的 NOP 受体拮抗剂，pKi 为 10.24。UFP-101 TFA 对 δ、μ 和 κ 类阿片受体的选择性大于 3000 倍。UFP-101 TFA 具有抗抑郁药样作用。
T80253	S3 Fragment
	S3 Fragment 是具有生物活性的肽，含有 ADF/cofilin 的特异性 N-端磷酸化位点，即 LIM 激酶（LIMK）的靶点。LIMK1 通过在 ADF/cofilin 的丝氨酸 3 位磷酸化来失活该蛋白，是肌动蛋白细胞骨架重要调控因子。该肽段包含 ADF/cofilin 丝氨酸 3 位点，作为 LIMK1 的有效竞争性抑制剂而被广泛研究。
T80175	Conopeptide rho-TIA	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Conopeptide rho-TIA为从掠食性海螺Conus tulipa毒液中提炼的多肽，对人类α1B-Adrenergic Receptor呈现非竞争性抑制作用，同时对α1A-Adrenergic Receptor和α1D-Adrenergic Receptor表现出竞争性抑制。Conopeptide rho-TIA与这些亚型的结合特性可能对开发针对α1-Adrenergic Receptor亚型的选择性新药具有参考价值。
T75810	AKTide-2T TFA
	AKTide-2T TFA 是一个优良的体外AKT 底物，可竞争性抑制组蛋白 H2B 磷酸化，其Ki 值为 12 nM。AKTide-2T TFA 模拟Akt 的磷酸化序列，是一种抑制肽，是 S22 位置中缺失了野生型 AKTide。
T75832	Cyclotraxin B TFA
	Cyclotraxin B TFA 是一种环肽，是一种高效且选择性的 TrkB 抑制剂，且不会改变 BDNF 的结合。Cyclotraxin B TFA 非竞争性地抑制 BDNF 诱导的 TrkB 活性，IC50值为 0.30 nM。Cyclotraxin B TFA 可以穿越血脑屏障，并具有止痛和抗焦虑的行为作用。
T80167	αC-Conotoxin PrXA αC-PrXA
	αC-Conotoxin PrXA为麻痹肽类神经毒素，亦是竞争性nAChR拮抗剂，对α1β1εδ（成人型）和α1β1γδ（胎儿型）nAChR的IC50值分别为1.8 nM和3.0 nM。该化合物通过与α-bungarotoxin竞争nAChR的α/δ及α/γ亚基界面，展现出对神经肌肉型nAChR的高度特异性。
T69383	NBI-42902
	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...
T80166	α-Conotoxin BuIA
	α-Conotoxin BuIA 是一种麻痹性肽类神经毒素，同时也是竞争性nAChR拮抗剂。它对nAChR亚型表现出不同的IC50值：0.258 nM（α6/α3β2）、1.54 nM（α6/α3β4）、5.72 nM（α3β2）。该化合物可用于鉴别包含β2与β4亚单位的nAChR亚型。此外，α-Conotoxin BuIA 对αxβ2nAChR的区分能力按照α6>α3>α2>α4的顺序减弱。
T76213	HXR9 hydrochloride
	HXR9 hydrochloride 是一种针对 HOX/PBX 相互作用的细胞渗透性肽类竞争性拮抗剂。它通过阻碍 HOX 蛋白与 PBX，一个与旁系同源基因组 1 至 8 结合的第二转录因子，之间的相互作用来发挥作用。特别地，HXR9 hydrochloride 能够选择性抑制细胞增殖，并在表达 HOXA/PBX3 基因高水平的细胞中，如 MLL 重排的白血病细胞，促进细胞凋亡。
T75715	Nonapeptide-1 acetate salt
	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。
T78224	Histatin-3
	Histatin-3是一肽类物质，由32个氨基酸残基构成，表现出显著的抗菌活性。作为前蛋白转化酶1(PC1)的底物，Histatin-3在Arg25位点的羧基端被该蛋白酶特异性切割（HRGYR降低SN）。此外，Histatin-3亦作为中等效力的、可逆的以及具竞争性的抑制剂，能够抑制弗林蛋白酶介导的五肽pGlu-Arg-Thr-Lys-Arg-MCA荧光底物的裂解，其抑制常数Ki大约为1.98μM。
T37522	Teneligliptin
	Teneligliptin (MP-513) is a potent chemotype prolylthiazolidine-based DPP-4 inhibitor, which competitively inhibits human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50s of approximately 1 nM. Teneligliptin (MP-513) inhibits all these DPP-4 enzymes in a concentration-dependent manner. The IC50s of Teneligliptin (MP-513) for rhDPP-4, human plasma, and rat plasma are 0.889, 1.75, and 1.35 nM, respectively. A study of enzyme inhibition kinetics is conducted for Teneligliptin (M...

化合物

Cat.No: T3624

Synonym: A 366,A366

Target: Epigenetic Reader Domain, Histone Methyltransferase

Cat.No: T26645

Synonym: CNS 1102,CNS-1102,CNS1102

Target: NMDAR

Cat.No: TP2100

Synonym: Exendin-3 (9-39) amide,Exendin (9-39),艾塞那肽

Target: Glucagon Receptor

PKG inhibitor peptide TFA (82801-73-8 free base)

Cat.No: TP1523

Synonym: PKG inhibitor peptide TFA

Target: PKA

[D-p-Cl-Phe6,Leu17]-VIP acetate

Cat.No: TP2103L

Target: Others

Cat.No: T78223

Synonym: gamma-Glutamyltyrosine,gamma-GLU-TYR

GLP-1R Antagonist 1

Cat.No: T15387

Target: Glucagon Receptor

[Ala107]-MBP (104-118) acetate

Cat.No: TP1887L1

Synonym: [Ala107]-MBP (104-118) acetate(99026-77-4 free base)

Target: PKC

Peptide T acetate(106362-32-7 free base)

Cat.No: TP1785L

Target: Others, HIV Protease

MLCK inhibitor peptide 18 acetate

Cat.No: TP1890L1

Synonym: MLCK inhibitor peptide 18 acetate(224579-74-2 free base)

Target: Serine/threonin kinase

Cat.No: T8313

Target: Others

Cat.No: T8691

Synonym: PD168368

Target: Bombesin Receptor

Cat.No: T71280

Cat.No: T69621

Z-Ile-Leu-aldehyde

Cat.No: T17281

Synonym: Z-IL-CHO,GSI-XII,γ-Secretase inhibitor XII

Target: Others

[Ala113]MBP(104-118)

Cat.No: TP1888

Synonym: [Ala113]-MBP (104-118)

PKG inhibitor peptide TFA

Cat.No: T81448

[Ala107]MBP(104-118)

Cat.No: TP1887

Synonym: [Ala107]-MBP (104-118)

Cat.No: TP1785

Cat.No: T38460

Cat.No: T60319

Cat.No: T68192

Rimegepant sulfate hydrate

Cat.No: T70837

Met-Arg-Phe-Ala

Cat.No: T81817

PKG inhibitor peptide

Cat.No: TP1903

Synonym: cGMP Dependent Kinase Inhibitor Peptide

Cat.No: T15415

Target: Others

Cat.No: T41062

Cat.No: T75878

Cat.No: T32004

Synonym: GSK 172981,GSK-172981

L-365260 hemihydrate

Cat.No: T62039

[D-p-Cl-Phe6,Leu17]-VIP TFA

Cat.No: T78003

Cat.No: TP1989

Synonym: Nogo-66 (1-40)

Cat.No: T75739

Cat.No: T75765

human GALP (3-32)

Cat.No: T80516

Synonym: Galanin-like peptide (3-32)

Target: Neuropeptide Y Receptor

Cat.No: T75895

Cat.No: T80253

Conopeptide rho-TIA

Cat.No: T80175

Target: Adrenergic Receptor

Cat.No: T75810

Cyclotraxin B TFA

Cat.No: T75832

αC-Conotoxin PrXA

Cat.No: T80167

Synonym: αC-PrXA

Cat.No: T69383

α-Conotoxin BuIA

Cat.No: T80166

HXR9 hydrochloride

Cat.No: T76213

Nonapeptide-1 acetate salt

Cat.No: T75715

Cat.No: T78224

Cat.No: T37522

Cat. No.	Product Name	Target	Signaling Pathways
T75890	Conantokin G TFA
	Conantokin G TFA 是一种 17 个氨基酸的肽，是一种有效，选择性和竞争性的 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂。Conantokin G TFA 抑制鼠皮质神经元中NMDA 诱发的电流，IC50为 480 nM，具有神经保护作用。

天然产物

Conantokin G TFA

Cat.No: T75890

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