Integrin

信号通路图

研究领域

抑制剂选择性比较

Integrin产品

所有产品(15) Integrin抑制剂(9) Integrin拮抗剂(5) Integrin激动剂(1)

目录号	产品描述	文献引用	实验数据
S7077	Cilengitide trifluoroacetate Cilengitide (EMD 121974, NSC 707544)是一种有效的integrin抑制剂，作用于αvβ3受体和αvβ5受体，无细胞试验中IC50分别为4.1 nM和79 nM，比作用于gpIIbIIIa选择性高10倍左右。Phase 2。	Cell Prolif, 2021, 54(4):e13012 Acta Biochim Biophys Sin (Shanghai), 2021, 53(3):294-303 Exp Brain Res, 2021, 10.1007/s00221-021-06111-x	Cell growth inhibition of non-small cell lung carcinoma (NSCLC) by Cilengitide. Cilengitide is based on the cyclic peptide cyclo(-RGDfV-), which is selective for αv integrins. Interestingly, it acts differently on HTB183 and A549 cell lines. Cilengitide was more efficient on A549, lung adenocarcinoma, while in HTB183 it showed moderate inhibitory activity. This may be due to the mestastatic nature of HTB183 cells which have already lost the cell adhesion properties.
S8008	RGD (Arg-Gly-Asp) Peptides RGD (Arg-Gly-Asp) Peptides是一种细胞粘附序列，可以模仿细胞粘附蛋白并与整合素结合。	Immunity, 2021, S1074-7613(21)00289-2 J Extracell Vesicles, 2021, 10(8):e12091 Nat Commun, 2020, 11(1):282	Observation of actin cytoskeleton and nucleus of MC3T3-E1 cells cultured in the presence of different inhibitors (Control, EDTA, RGD, MAB1998, IgG and Heparin) after 24 hours of incubation.
S2885	A-205804 A-205804是一种强有效和选择性E-selectin和ICAM-1表达抑制剂， IC50分别为20 nM和25 nM。	Cancer Lett, 2018, 438:105-115 Immunol Cell Biol, 2018, 10.1111/imcb.12208 Acta Pharmacol Sin, 2018, 39(8):1326-1337	The effect of rhICAM-1 or inhibitor A-205804 on hepsin or CtsD transfected MCF-7 cells was detected. The level of E-cadherin, claudin-1, N-cadherin, vimentin and Snail1 was analyzed by western blot.
S7540	SB273005 SB273005 是一种有效的integrin抑制剂，对αvβ3 受体和αvβ5受体的K_i分别为1.2 nM 和 0.3 nM。	Nat Methods, 2021, 18(1):84-91 Anal Chim Acta, 2021, 1151:338222 Cell Prolif, 2021, 54(4):e13012	Western blot analysis of levels of p-FAK (Tyr397) and total FAK in SK-N-SH cells treated with SB273005 (3 μM) for 6 h and 24 h. One experiment is shown for each cell line. Control cells (treated with diluent, marked as C, were also included). α-tubulin was used as the reference protein.
S6387^New	Cilengitide Cilengitide (EMD 121974, EMD-12192, EMD-85189, NSC-707544) 是一种有效的、选择性的 integrins α_νβ₃ 和 α_νβ₅ 的抑制剂，对应的IC50值分别为 4 nM和 79 nM。
S4513^New	RGD peptide (GRGDNP) RGD peptide (GRGDNP) 是 integrins 与细胞外基质结合的抑制剂。RGD peptide (GRGDNP) 可能通过直接激活 caspase-3 并诱导凋亡。
S6840	OSU-T315 OSU-T315 (ILK-IN-2)是一种有效的 Integrin-Linked Kinase (ILK) 的抑制剂，其IC50值为0.6 μM。OSU-T315 可诱导自噬和细胞凋亡，这两者都是其抗增殖活性不可或缺的。OSU-T315 具有抗肿瘤活性。
S7834	Cyclo (-RGDfK) Cyclo (-RGDfK)是一种有效的选择性 αvβ3 integrin 抑制剂。	Cell Death Dis, 2020, 14;11(4):230 Elife, 2019, 8 Cell Death Dis, 2019, 10(6):401
S7844	Cyclo(RGDyK) Cyclo(RGDyK)是一种有效的选择性αVβ3 integrin抑制剂，IC50为20 nM。	Immunology, 2020, 20 Nephron, 2019, 10.1159/000499506 Cell, 2018, 175(7):1756-1768	(E, F) Inhibition of integrin pathway by integrin inhibitor Cyclo(RGDyK) (30 µM) eliminated the enhancement of ZC3H14 depletion on integrin pathway in HepG2 (E) and MHCC-97L (F) cells. NS, non-specific reactive band.
S3085	Tirofiban Tirofiban (MK-383)是一种选择性GPIIb/IIIa拮抗剂，可以抑制血小板聚集，IC50为9nM。	Food Funct, 2020, 11(1):139-152
S0314	TR-14035 TR-14035 (SB 683698, MDK-1191) 是一种 alpha4beta (α4β) integrin 双效拮抗剂，对 alpha4beta7 (α4β7) 和 alpha4beta1 (α4β1) 的IC50值分别为7 nM和87 nM。
S8594	Tirofiban Hydrochloride Tirofiban Hydrochloride (MK-383)是tirofiban的盐酸盐形式，tirofiban是一种选择性的platelet GPIIb/IIIa拮抗剂，抑制血小板凝集。它比游离形式的Tirofiban溶解性更好。
S8454	ATN-161 (Ac-PHSCN-NH2) ATN-161 (Ac-PHSCN-NH2)是integrin α5β1的小肽段拮抗剂。它能够结合好几种整合素，包括α5β1和αvβ3，在血管生成和肿瘤进展中发挥作用。	Bioact Mater, 2021, 6(7):2039-2057 Eur Rev Med Pharmacol Sci, 2021, 25(3):1233-1241 Bioact Mater, 2021, 6(7):2039-2057
S3714	Lifitegrast Lifitegrast (SAR1118)是一种新型的integrin拮抗剂，抑制参与DED病理形成中的特定的T细胞介导的炎症途径。	J Biomol Struct Dyn, 2020, 1-14
S8306	Leukadherin-1 Leukadherin-1 (LA1)是一种能增强CD11b/CD18依赖性的细胞与其配体ICAM-1粘着的小分子化合物，是补体受体3（CD11b/CD18）的激动剂。	J Inflamm Res, 2021, 14:1341-1356 bioRxiv, 2020, 10.1101/2020.11.25.398701 Front Immunol, 2019, 10:215

目录号	产品描述	文献引用	实验数据
S7077	Cilengitide trifluoroacetate Cilengitide (EMD 121974, NSC 707544)是一种有效的integrin抑制剂，作用于αvβ3受体和αvβ5受体，无细胞试验中IC50分别为4.1 nM和79 nM，比作用于gpIIbIIIa选择性高10倍左右。Phase 2。	Cell Prolif,2021, 54(4):e13012 Acta Biochim Biophys Sin (Shanghai),2021, 53(3):294-303 Exp Brain Res,2021, 10.1007/s00221-021-06111-x	Cell growth inhibition of non-small cell lung carcinoma (NSCLC) by Cilengitide. Cilengitide is based on the cyclic peptide cyclo(-RGDfV-), which is selective for αv integrins. Interestingly, it acts differently on HTB183 and A549 cell lines. Cilengitide was more efficient on A549, lung adenocarcinoma, while in HTB183 it showed moderate inhibitory activity. This may be due to the mestastatic nature of HTB183 cells which have already lost the cell adhesion properties.
S8008	RGD (Arg-Gly-Asp) Peptides RGD (Arg-Gly-Asp) Peptides是一种细胞粘附序列，可以模仿细胞粘附蛋白并与整合素结合。	Immunity,2021, S1074-7613(21)00289-2 J Extracell Vesicles,2021, 10(8):e12091 Nat Commun,2020, 11(1):282	Observation of actin cytoskeleton and nucleus of MC3T3-E1 cells cultured in the presence of different inhibitors (Control, EDTA, RGD, MAB1998, IgG and Heparin) after 24 hours of incubation.
S2885	A-205804 A-205804是一种强有效和选择性E-selectin和ICAM-1表达抑制剂， IC50分别为20 nM和25 nM。	Cancer Lett,2018, 438:105-115 Immunol Cell Biol,2018, 10.1111/imcb.12208 Acta Pharmacol Sin,2018, 39(8):1326-1337	The effect of rhICAM-1 or inhibitor A-205804 on hepsin or CtsD transfected MCF-7 cells was detected. The level of E-cadherin, claudin-1, N-cadherin, vimentin and Snail1 was analyzed by western blot.
S7540	SB273005 SB273005 是一种有效的integrin抑制剂，对αvβ3 受体和αvβ5受体的K_i分别为1.2 nM 和 0.3 nM。	Nat Methods,2021, 18(1):84-91 Anal Chim Acta,2021, 1151:338222 Cell Prolif,2021, 54(4):e13012	Western blot analysis of levels of p-FAK (Tyr397) and total FAK in SK-N-SH cells treated with SB273005 (3 μM) for 6 h and 24 h. One experiment is shown for each cell line. Control cells (treated with diluent, marked as C, were also included). α-tubulin was used as the reference protein.
S6387^New	Cilengitide Cilengitide (EMD 121974, EMD-12192, EMD-85189, NSC-707544) 是一种有效的、选择性的 integrins α_νβ₃ 和 α_νβ₅ 的抑制剂，对应的IC50值分别为 4 nM和 79 nM。
S4513^New	RGD peptide (GRGDNP) RGD peptide (GRGDNP) 是 integrins 与细胞外基质结合的抑制剂。RGD peptide (GRGDNP) 可能通过直接激活 caspase-3 并诱导凋亡。
S6840	OSU-T315 OSU-T315 (ILK-IN-2)是一种有效的 Integrin-Linked Kinase (ILK) 的抑制剂，其IC50值为0.6 μM。OSU-T315 可诱导自噬和细胞凋亡，这两者都是其抗增殖活性不可或缺的。OSU-T315 具有抗肿瘤活性。
S7834	Cyclo (-RGDfK) Cyclo (-RGDfK)是一种有效的选择性 αvβ3 integrin 抑制剂。	Cell Death Dis,2020, 14;11(4):230 Elife,2019, 8 Cell Death Dis,2019, 10(6):401
S7844	Cyclo(RGDyK) Cyclo(RGDyK)是一种有效的选择性αVβ3 integrin抑制剂，IC50为20 nM。	Immunology,2020, 20 Nephron,2019, 10.1159/000499506 Cell,2018, 175(7):1756-1768	(E, F) Inhibition of integrin pathway by integrin inhibitor Cyclo(RGDyK) (30 µM) eliminated the enhancement of ZC3H14 depletion on integrin pathway in HepG2 (E) and MHCC-97L (F) cells. NS, non-specific reactive band.

目录号	产品描述	文献引用	实验数据
S3085	Tirofiban Tirofiban (MK-383)是一种选择性GPIIb/IIIa拮抗剂，可以抑制血小板聚集，IC50为9nM。	Food Funct, 2020, 11(1):139-152
S0314	TR-14035 TR-14035 (SB 683698, MDK-1191) 是一种 alpha4beta (α4β) integrin 双效拮抗剂，对 alpha4beta7 (α4β7) 和 alpha4beta1 (α4β1) 的IC50值分别为7 nM和87 nM。
S8594	Tirofiban Hydrochloride Tirofiban Hydrochloride (MK-383)是tirofiban的盐酸盐形式，tirofiban是一种选择性的platelet GPIIb/IIIa拮抗剂，抑制血小板凝集。它比游离形式的Tirofiban溶解性更好。
S8454	ATN-161 (Ac-PHSCN-NH2) ATN-161 (Ac-PHSCN-NH2)是integrin α5β1的小肽段拮抗剂。它能够结合好几种整合素，包括α5β1和αvβ3，在血管生成和肿瘤进展中发挥作用。	Bioact Mater, 2021, 6(7):2039-2057 Eur Rev Med Pharmacol Sci, 2021, 25(3):1233-1241 Bioact Mater, 2021, 6(7):2039-2057
S3714	Lifitegrast Lifitegrast (SAR1118)是一种新型的integrin拮抗剂，抑制参与DED病理形成中的特定的T细胞介导的炎症途径。	J Biomol Struct Dyn, 2020, 1-14

目录号

产品描述

文献引用

实验数据

S8306

Leukadherin-1

Leukadherin-1 (LA1)是一种能增强CD11b/CD18依赖性的细胞与其配体ICAM-1粘着的小分子化合物，是补体受体3（CD11b/CD18）的激动剂。

J Inflamm Res, 2021, 14:1341-1356

bioRxiv, 2020, 10.1101/2020.11.25.398701

Front Immunol, 2019, 10:215