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29

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T2494	Cilengitide 西仑吉肽,EMD 121974	Integrin; Autophagy	Autophagy; Cytoskeletal Signaling
	Cilengitide (EMD 121974) 是一种有效的 αvβ3/5 受体整合素抑制剂，可抑制 ανβ3和 ανβ5与玻连蛋白结合，IC50值分别为 4 和 79 nM。
T21785	AG957	Bcr-Abl	Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors
	Tyrphostin AG957 是一种酪氨酸激酶抑制剂，具有抗BCR/ABL 酪氨酸激酶活性。它能够抑制p210bcr/abl 酶活性 (IC50:2.9 μM)。
T5310	TR-14035 MDK-1191	Integrin	Cytoskeletal Signaling
	TR-14035 (MDK-1191) 是一种具有口服活性的 α4β7/α4β1整合素双重抑制剂，对 α4β7和 α4β1作用的 IC50值分别为 7 和 87 nM，可用于炎症和自体免疫疾病的研究。
T7566L1	GRGDSPK acetate GRGDSPK acetate(111119-28-9 Free base)	Beta Amyloid	Neuroscience
	GRGDSPK acetate 显示出对整合素-纤连蛋白结合的抑制活性，可用于研究整合素在骨形成和吸收中的作用。
TQ0250	CWHM-12	Integrin	Cytoskeletal Signaling
	CWHM-12 是 αV 整合素的有效抑制剂，抑制αvβ8、αvβ3、αvβ6和αvβ1，IC50 为 0.2、0.8、1.5 和 1.8 nM。
T6966	RGD RGD (Arg-Gly-Asp) Peptides,Arg-Gly-Asp,RGD Peptides	Integrin	Cytoskeletal Signaling
	RGD (RGD (Arg-Gly-Asp) Peptides) 是一种细胞粘附基序，可以模拟细胞粘附蛋白并与整合素结合。
T2537	Tirofiban hydrochloride monohydrate Tirofiban Hydrochloride,盐酸替罗非班水合物,MK-383 Hydrochloride,盐酸替罗非班	ATPase; Integrin	Cytoskeletal Signaling; Membrane transporter/Ion channel
	Tirofiban hydrochloride monohydrate (MK-383 Hydrochloride) 是一种非肽类糖蛋白IIb/IIIa 的拮抗剂。
T4613	Arg-Gly-Asp TFA (99896-85-2(free base)) RGD Trifluoroacetate,RGD	Integrin	Cytoskeletal Signaling
	Arg-Gly-Asp TFA (99896-85-2(free base)) (RGD Trifluoroacetate) 是一种三肽，可有效触发细胞粘附、定位某些细胞系并引发特定的细胞反应；与整合素结合。
T39933	Bexotegrast PLN-74809	Integrin	Cytoskeletal Signaling
	Bexotegrast (PLN-74809)是一种具有口服活性和强效性的 αvβ6和αvβ1 整合素抑制剂，具有抗纤维化作用，抑制 αvβ6 和 αvβ1 诱导的 TGF-β 激活，可用于研究特发性肺纤维化（IPF）和非特异性间质性肺炎（NSIP）。
T26887	BOP
	BOP is anantagonist of alpha4beta1/alpha9beta1 integrins. BOP rapidly mobilizes long-term multi-lineage reconstituting hematopoietic stem cells (HSC).
T69517	Bexotegrast HCl
	Bexotegrast, also known as PLN-74809, is a small-molecule, dual selective inhibitor of αVβ1 / αVβ6 for idiopathic pulmonary fibrosis (IPF) and primary sclerosing cholangitis (PSC). These integrins cause upstream activation of TGF-β1 in actively fibrotic tissue. Inhibition of these integrins will block TGF-β1 activation, thereby preventing the growth of fibrotic tissue within the lung and bile ducts.
T16875	SF1126	Others	Others
	SF1126 is a relevant pan and dual first-in-class PI3K/BRD4 inhibitor. SF1126 is an RGDS-conjugated LY294002 prodrug, which is designed to exhibit increased solubility and bind to specific integrins within the tumor compartment.
T38793	THI0019 THI0019
	THI0019 is a highly potent agonist of the integrin α4β1 (VLA-4) receptor, with an EC 50 range of 1-2 μM. It effectively promotes the adhesion of stem/progenitor cells. Furthermore, THI0019 successfully modulates adhesion processes mediated by α4β7, α5β1, and αLβ2 integrins.
T16851	SB-267268	Others	Others
	SB-267268 inhibits human and mouse αvβ3 (IC50s: 0.68 and 0.29 nM, respectively). SB-267268 is a selective and nonpeptidic alpha(v)beta3 and alpha(v)beta5 integrins antagonist (Kis: 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respective
T81283	RGD-targeted Proapoptotic Peptide
	RGD-targeted Proapoptotic Peptide为一肽类化合物，其C端RGD-4C肽段（ACDCRGDCFC）能够特异性地与肿瘤新生血管的整合素结合位点优先结合。
T70083	Cilengitide hydrochloride
	Cilengitide hydrochloride sis the salt form of Cilengitide, a cyclic Arg-Gly-Asp peptide with potential antineoplastic activity. Cilengitide binds to and inhibits the activities of the alpha(v)beta(3) and alpha(v)beta(5) integrins, thereby inhibiting endothelial cell-cell interactions, endothelial cell-matrix interactions, and angiogenesis.
T80214	cRGDfK-thioacetyl ester	Integrin	Cytoskeletal Signaling
	cRGDfK-thioacetyl ester 为具选择性亲和力于整合素（integrins）之生物活性多肽。可应用于修饰NIR荧光探针，实现癌症靶向成像。
TP1555	Fibronectin Active Fragment Control
	Fibronectin is a high-molecular weight (~440kDa) extracellular matrix glycoprotein that binds to membrane-spanning receptor proteins called integrins.In addition to integrins, fibronectin also binds extracellular matrix components such as collagen, fibrin
T82359	G-{d-Arg}-GDSP
	G-{d-Arg}-GDSP为RGD多肽类似物，具有与整合素粘附受体结合的能力，能够抑制细胞对纤维连接蛋白的附着及破骨细胞的重吸收。
T41153	BOP-JF646 BOP-JF646
	BOP-JF646 is a fluorescent dual α9β1/α4β1 integrin inhibitor. Comprises BOP conjugated to Janelia Fluor®646. Fluorogenic: fluoresces only once bound to integrins, enabling hassle-free no-wash experiments. Bright and photostable, enabling live cell tracking of integrin receptors over long time-course experiments. Excitation maximum = 655 nm; emission maximum = 672 nm.
T79792	αvβ1 integrin-IN-2	Integrin	Cytoskeletal Signaling
	αvβ1integrin-IN-2（compound 32）作为整合素ανβ1与α5β1的抑制剂，展现出高效性，其IC50值分别为0.9 nM和33 nM。此外，该化合物对其他整合素亦有抑制作用，其IC50分别为380 nM（ανβ3）、280 nM（ανβ5）、230 nM（ανβ6）、87 nM（ανβ8）。
T41149	BOP-JF549 BOP-JF549
	BOP-JF549 is a fluorescent dual α9β1/α4β1 integrin inhibitor. Comprises BOP conjugated to Janelia Fluor® 549. Fluorogenic: fluoresces only once bound to integrins, enabling hassle-free no-wash experiments. Bright and photostable, enabling live cell tracking of integrin receptors over long time-course experiments. Excitation maximum = 549 nm; emission maximum = 571 nm.
T77154	Etrolizumab
	Etrolizumab (rhuMAb Beta7) 是一种肠道选择性抗-β7整合素单克隆抗体。Etrolizuma b 是针对α4β7和 αEβ7 整合素的 β7 亚基的特异性靶向活性分子。Etrolizumab 可用于炎症性肠病 (IBD) 的研究。
T76255	Certepetide
	Certepetide (CEND-1)，即双功能环肽（a.k.a. iRGD），是一种具有穿透肿瘤功能的多肽。通过与α-V整联蛋白（alphav-integrins）的RGD motif相互作用，以及激活神经纤毛蛋白1（NRP-1），Certepetide能够将实体瘤微环境转化成临时的活性分子通道，从而在肿瘤中累积。该化合物在胰腺癌和其他实体瘤的研究中具有应用潜力。
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。
TP1343	RGD Trifluoroacetate
	RGD Trifluoroacetate is a tripeptide that effectively triggers cell adhesion, addresses certain cell lines and elicits specific cell responses; RGD Trifluoroacetate binds to integrins.RGD Trifluoroacetate is the most effective and most often employed pept
T36296	BIO5192 hydrate
	BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels[1][2]. The combination of BIO5192 hydrate (1 mg/kg; i.v.) and Plerixafor (5 mg/kg; s.c.) exert an additive effect on progenitor mobilization[1].BIO5192 hydrate (30 mg/kg; s.c; bid; during days...
T82379	FN-A208 fusion peptide
	FN-A208 是源自鼠层粘连蛋白 a1 的 A208 与纤连蛋白 (GRGDS) 活性位点和甘氨酸间隔区融合形成的生物活性肽。该肽能形成淀粉样原纤维，并有助于促进肌动蛋白应力纤维的形成，进而介导成纤维细胞附着，显示出其在组织再生和工程生物粘合剂方面的应用潜力。FN-A208 与 IKVAV 受体和整合素发生相互作用，而在 EDTA 存在下，其活性则会被破坏。
T36291	Integrin modulator 1
	Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM[1]. Integrin modulator 1 (2-10 μg/mL; 30 min) significantly increases Jurkat E6.1 cell adhesion[1].Integrin modulator 1 (1-100 nM; 1 h) strongly and significantly increases ERK1/2 phosphorylation in Jurkat E6.1 cells[1].Integrin modulator 1 (1 nM-10 μM; 30 min) significantly increases the...

化合物

Cat.No: T2494

Synonym: 西仑吉肽,EMD 121974

Target: Integrin, Autophagy

Cat.No: T21785

Target: Bcr-Abl

Cat.No: T5310

Synonym: MDK-1191

Target: Integrin

GRGDSPK acetate

Cat.No: T7566L1

Synonym: GRGDSPK acetate(111119-28-9 Free base)

Target: Beta Amyloid

Cat.No: TQ0250

Target: Integrin

Cat.No: T6966

Synonym: RGD (Arg-Gly-Asp) Peptides,Arg-Gly-Asp,RGD Peptides

Target: Integrin

Tirofiban hydrochloride monohydrate

Cat.No: T2537

Synonym: Tirofiban Hydrochloride,盐酸替罗非班水合物,MK-383 Hydrochloride,盐酸替罗非班

Target: ATPase, Integrin

Arg-Gly-Asp TFA (99896-85-2(free base))

Cat.No: T4613

Synonym: RGD Trifluoroacetate,RGD

Target: Integrin

Cat.No: T39933

Synonym: PLN-74809

Target: Integrin

Cat.No: T26887

Bexotegrast HCl

Cat.No: T69517

Cat.No: T16875

Target: Others

Cat.No: T38793

Synonym: THI0019

Cat.No: T16851

Target: Others

RGD-targeted Proapoptotic Peptide

Cat.No: T81283

Cilengitide hydrochloride

Cat.No: T70083

cRGDfK-thioacetyl ester

Cat.No: T80214

Target: Integrin

Fibronectin Active Fragment Control

Cat.No: TP1555

Cat.No: T82359

Cat.No: T41153

Synonym: BOP-JF646

αvβ1 integrin-IN-2

Cat.No: T79792

Target: Integrin

Cat.No: T41149

Synonym: BOP-JF549

Cat.No: T77154

Cat.No: T76255

Cat.No: T75765

RGD Trifluoroacetate

Cat.No: TP1343

BIO5192 hydrate

Cat.No: T36296

FN-A208 fusion peptide

Cat.No: T82379

Integrin modulator 1

Cat.No: T36291

Cat. No.	Product Name	Target	Signaling Pathways
T36295	Echistatin TFA
	Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1[1][2][3][4]. [1]. J Musial, et al. Inhibition of platelet adhesion to surfaces of extracorporeal circuits by disintegrins. RGD-containing peptides from viper venoms. Circulation. 1990 Jul;82(1):261-73.[2]. ...

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Cat.No: T36295

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