integrins

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。

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)。

Integrinsignaling inhibitor, mP13 是抑制整合素信号传导，阻止内向外和外向内信号传递，涉及纤维蛋白原结合、血小板粘附及凝块收缩的化合物。

Arg-Gly-Asp-Ser (RGDS peptide)是在纤连蛋白、纤维蛋白原α和血管性血友病因子上发现的保守四肽序列，与细胞表面的整合素结合，抑制凝血酶诱导的血小板与纤连蛋白。

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。

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

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.

BOP is anantagonist of alpha4beta1/alpha9beta1 integrins. BOP rapidly mobilizes long-term multi-lineage reconstituting hematopoietic stem cells (HSC).

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 binding of HUTS-21 antibody to Jurkat E6.1 cells in a concentration-dependent manner[1]. [1]. Baiula M, et, al. New β-Lactam Derivatives Modulate Cell Adhesion and Signaling Mediated by RGD-Binding and Leukocyte Integrins. J Med Chem. 2016 Nov 10;59(21):9721-9742.

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]. M Sato, et al. Echistatin is a potent inhibitor of bone resorption in culture. J Cell Biol. 1990 Oct;111(4):1713-23.[3]. C C Kumar, et al. Biochemical characterization of the binding of echistatin to integrin alphavbeta3 receptor. J Pharmacol Exp Ther. 1997 Nov;283(2):843-53.[4]. I Wierzbicka-Patynowski, et al. Structural requirements of echistatin for the recognition of alpha(v)beta(3) and alpha(5)beta(1) integrins. J Biol Chem. 1999 Dec 31;274(53):37809-14.

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 5 through 14) delays paralysis associated with EAE (experimental autoimmune encephalomyelitis)[2].BIO5192 hydrate (1 mg kg, i.v.) shows the terminal half-life is 1.1 hours. BIO5192 hydrate (3, 10, and 30 mg kg; s.c.) shows half-lives of 1.7, 2.7, and 4.7 hours, respectively. The blood plasma curves show that the AUC for the s.c. route of administration increased about 2.5-fold from 5,460 h*ng ml for the 3 mg kg dose to 14,175 h*ng ml for the 30 mg kg[1]. Animal Model: C57BL 6J x 129Sv J F1 mice[1] [1]. Ramirez P, et al. BIO5192, a small molecule inhibitor of VLA-4, mobilizes hematopoietic stem and progenitor cells. Blood. 2009;114(7):1340‐1343. [2]. Leone DR, et al. An assessment of the mechanistic differences between two integrin alpha 4 beta 1 inhibitors, the monoclonal antibody TA-2 and the small molecule BIO5192, in rat experimental autoimmune encephalomyelitis. J Pharmacol Exp Ther. 2003;305(3):1150-1162.

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.

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）。

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.

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.

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。

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。

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.

Arginine-glycine-aspartic acid (RGD) 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。

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.

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。

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。

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）。

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。