Integrin-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Integrin.html IntegrinIntegrins, a family of heterodimeric adhesion receptors for diverse extracellular matrices, have consistently been implicated ascrucial drivers of ovarian cancer development and progression. A number of the RGD-based members of the integri

2、n family,including 51, and v3 or v5 integrins, are markedly elevated in aggressive ovarian tumors. These adhesion receptors appearto promote cell adhesion, survival, motility and invasion during ovarian tumor growth or metastatic progression. Importantly, thefunctions of these integrins are strongly

3、 dependent on the activation of focal adhesion kinase (FAK) and its downstream signaling,including the PI3K/Akt- and Ras/MAPK-dependent pathways.Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion. Modulationof these molecules, part

4、icularly v integrin family, has exhibited profound effects on fibrosis in multiple organ and disease state.Based on the several studies, the integrins v3, v5, v6, and v8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)- in pre-clinical models

5、of fibrosis.Each integrin is typically formed by the non-covalent pairing of one subunit, of which, 18 types are known to exist, and one subunit, of which 8 types are known to exist. Together, 24 distinct heterodimers have been identified to date. The v subunit canform heterodimers with the 1, 3, 5,

6、 6 or 8 subunits and 1 can associate with many different subunits from 1 to 11, andv, indicating that not all theoretically possible and subunit pairs form. Interestingly, the activation of TGF- appears to be acommon function of multiple v integrins.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targe

7、ts/Integrin.html Integrin HYPERLINK https:/www.MedChemE/Targets/Integrin.html HYPERLINK https:/www.MedChemE/Targets/Integrin.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Integrin.html HYPERLINK https:/www.MedChemE/Targets/Integrin.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Integr

8、in.html HYPERLINK https:/www.MedChemE/Targets/Integrin.html Antagonists HYPERLINK https:/www.MedChemE/Targets/Integrin.html HYPERLINK https:/www.MedChemE/Targets/Integrin.html & HYPERLINK https:/www.MedChemE/Targets/Integrin.html HYPERLINK https:/www.MedChemE/Targets/Integrin.html Modulators HYPERLI

9、NK https:/www.MedChemE/a-205804.html A-205804 HYPERLINK https:/www.MedChemE/a-205804.html HYPERLINK https:/www.MedChemE/a-286982.html A-286982Cat. No.: HY-100226 Cat. No.: HY-107587A-205804 is an orally bioavailable, potent andselective lead inhibitor of E-selectin andICAM-1 expression, with an IC o

10、f 20 nM and 2550nM for E-selectin and ICAM-1, respectively.A-205804 can be used in the research of chronicinflammatory diseases.A-286982 is a potent and allostericLFA-1/ICAM-1 interaction inhibitor with IC s of5044 nM and 35 nM in an LFA-1/ICAM-1 binding andLFA-1-mediated cellular adhesion assay,res

11、pectively.Purity: 98.12%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mgPurity: 99.69%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/alicaforsen.html Alicaforsen(ISIS-2302) Cat. No.: HY-145728 HYPERLINK https:/www.MedChemE/Arg-

12、Gly-Asp-Ser.html Arg-Gly-Asp-Ser(RGDS peptide; Fibronectin tetrapeptide) Cat. No.: HY-12290Alicaforsen is a 20-base antisenseoligonucleotide inhibiting ICAM-1 production,which is an important adhesion molecule involvedin leukocyte migration and trafficking to the siteof inflammation.Arg-Gly-Asp-Ser

13、is an integrin binding sequencethat inhibits integrin receptor function.Arg-Gly-Asp-Ser directly and specifically bindpro-caspase-8, pro-caspase-9 and pro-caspase-3,while it does not bind pro-caspase-1.Purity: 98%Clinical Data: Phase 3Size: 1 mg, 5 mgPurity: 99.76%Clinical Data: No Development Repor

14、tedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/arg-gly-asp-ser-tfa.html Arg-Gly-Asp-Ser HYPERLINK https:/www.MedChemE/arg-gly-asp-ser-tfa.html HYPERLINK https:/www.MedChemE/arg-gly-asp-ser-tfa.html (TFA)(RGDS peptide (TFA); Fibronectin tetrapeptide (TFA) Cat. No.: HY-12290A

15、HYPERLINK https:/www.MedChemE/atn-161.html ATN-161Cat. No.: HY-13535Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits integrin receptor function.Arg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8, pro-caspase-9 andpro-caspase-3, while it does not bindpro-caspase-1.ATN

16、-161 is a novel integrin 51 antagonist, whichinhibits angiogenesis and growth of livermetastases in a murine model.Purity: 98%Clinical Data:Size: 1 mg, 5 mgPurity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ATN-161-trifluoroacetate-salt.html ATN-161 HYPERLINK https:/www.

17、MedChemE/ATN-161-trifluoroacetate-salt.html HYPERLINK https:/www.MedChemE/ATN-161-trifluoroacetate-salt.html trifluoroacetate HYPERLINK https:/www.MedChemE/ATN-161-trifluoroacetate-salt.html HYPERLINK https:/www.MedChemE/ATN-161-trifluoroacetate-salt.html salt HYPERLINK https:/www.MedChemE/ATN-161-t

18、rifluoroacetate-salt.html HYPERLINK https:/www.MedChemE/bexotegrast.html Bexotegrast(ATN-161 TFA salt) Cat. No.: HY-13535ACat. No.: HY-137561ATN-161 trifluoroacetate salt is a novel integrin51 antagonist, which inhibits angiogenesis andgrowth of liver metastases in a murine model.Bexotegrast is a po

19、tent inhibitor of 6integrin. Bexotegrast can be used for researchingfibrosis such as idiopathic pulmonary fibrosis(IPF) and nonspecific interstitial pneumonia(NSIP) (extracted from patent WO2020210404A1,compound 5).Purity: 95.0%Clinical Data: Phase 2Size: 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinica

20、l Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bi-1950.html BI-1950 HYPERLINK https:/www.MedChemE/bi-1950.html HYPERLINK https:/www.MedChemE/bio-1211.html BIO-1211Cat. No.: HY-124040 Cat. No.: HY-14126BI-1950 is a highly potent lymphocyte functionassociated antigen-1 (

21、LFA-1) inhibitor. LFA-1 isan essential component in normal immune systemfunction and a target for drug discovery.BIO-1211 is a highly selective and orally active41 (VLA-4) inhibitor, with IC values of 4 nM50and 2 M for 41 and 47, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1

22、mg, 5 mgPurity: 99.64%Clinical Data: No Development ReportedSize: 1 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/bio5192.html BIO5192 HYPERLINK https:/www.MedChemE/bio5192.html HYPERLINK https:/www.MedChemE/bio5192-hydrate.html BIO5192 HYPERLINK https:/w

23、ww.MedChemE/bio5192-hydrate.html HYPERLINK https:/www.MedChemE/bio5192-hydrate.html hydrateCat. No.: HY-107589 Cat. No.: HY-107589ABIO5192 is a selective and potent integrin 41(VLA-4) inhibitor (K 10 pM). BIO5192dselectively binds to 41 (IC =1.8 nM) over a50range of other integrins.BIO5192 hydrate i

24、s a selective and potent integrin41 (VLA-4) inhibitor (K 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/birt-377.html BIRT HYPERLINK https:/www.MedChemE/birt-377.html HYPERLINK https:/www.MedChemE/

25、birt-377.html 377 HYPERLINK https:/www.MedChemE/birt-377.html HYPERLINK https:/www.MedChemE/bms-587101.html BMS-587101Cat. No.: HY-110117 Cat. No.: HY-120628BIRT 377 is a potent amd orally bioavailableinhibitor of the interaction between intercellularadhesion molecule-1 (ICAM-1) and lymphocytefuncti

26、on-associated antigen-1 (LFA-1), with a Kiof 25.8 nM. BIRT 377 also inhibits the productionof IL-2 in vivo.BMS-587101 is a potent and orally activeantagonist of leukocyte function associatedantigen-1 (LFA-1). BMS-587101 hasanti-inflammatory effects and can be used forrheumatoid arthritis research.Pu

27、rity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.67%Clinical Data: Phase 2Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bms-688521.html BMS-688521 HYPERLINK https:/www.MedChemE/bms-688521.html HYPERLINK https:/www.MedChemE/bop-sodium.html BOP HYPERLIN

28、K https:/www.MedChemE/bop-sodium.html HYPERLINK https:/www.MedChemE/bop-sodium.html sodiumCat. No.: HY-10596 Cat. No.: HY-129453BMS-688521 is a highly potent, orally activeinhibitor of the LFA-1/ICAM interaction, withan IC of 2.5 nM in the adhesion assay and an50IC of 60 nM in the MLR assay. BMS-688

29、521 is50efficacious in a mouse allergic eosinophilic lunginflammation model.BOP sodium is a potent and selective dual91/41 integrin inhibitor with K values indthe picomolar range. BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors.Purity: 98.72%Cl

30、inical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/c_phg-isoD-G-R-_NMe_k_.html c(phg-isoDGR-(NMe)k) HYPERLINK https:/www.MedChemE/c_phg-isoD-G-R-_NMe_k_.html HYPERLINK https:/www.MedChemE/c-

31、phg-isod-g-r-nme-k-tfa.html c(phg-isoDGR-(NMe)k) HYPERLINK https:/www.MedChemE/c-phg-isod-g-r-nme-k-tfa.html HYPERLINK https:/www.MedChemE/c-phg-isod-g-r-nme-k-tfa.html TFACat. No.: HY-111413 Cat. No.: HY-111413Ac(phg-isoDGR-(NMe)k) is a selective and potent51-integrin ligand with an IC of 2.9 nM.50

32、c(phg-isoDGR-(NMe)k) TFA is a selective and potent51-integrin ligand with an IC of 2.9 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/Carotegrast.html Carotegrast HYPE

33、RLINK https:/www.MedChemE/Carotegrast.html HYPERLINK https:/www.MedChemE/carotegrast-methyl.html Carotegrast HYPERLINK https:/www.MedChemE/carotegrast-methyl.html HYPERLINK https:/www.MedChemE/carotegrast-methyl.html methylCat. No.: HY-14857(AJM300) Cat. No.: HY-124290Carotegrast is an orally availa

34、ble 4 integrinreceptor inhibitor with anti-inflammatoriesactivities.Carotegrast methyl (AJM300) is an orally activeand selective 4 integrin antagonist. HCA2969, anactive metabolite of Carotegrast methyl, is aspecific and dual 41/47 integrin antagonist.Carotegrast methyl prevents the development ofco

35、litis in mice. .Purity: 98.14%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.72%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Cilengitide.html Cilengitide(EMD 121974) Cat.

36、 No.: HY-16141 HYPERLINK https:/www.MedChemE/Cilengitide_trifluoroacetate.html Cilengitide HYPERLINK https:/www.MedChemE/Cilengitide_trifluoroacetate.html HYPERLINK https:/www.MedChemE/Cilengitide_trifluoroacetate.html TFA(EMD 121974 TFA) Cat. No.: HY-16143Cilengitide (EMD 121974) is a potent and se

37、lectiveinhibitor of the integrins 3 and 5.Cilengitide inhibits binding of isolated 3and to Vitronectin with an IC value of 4 5 50and 79 nM, respectively .Cilengitide is a potent and selective integrininhibitor for and receptor, withv 3 v 5IC values of 4 nM and 79 nM, respectively.50Purity: 99.32%Cli

38、nical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/Cucurbitacin-B.html Cucurbitacin HYPERLINK https:/www.MedChemE/Cucurbitacin-B.html HYPERLINK https:/www.MedChemE/Cucur

39、bitacin-B.html B HYPERLINK https:/www.MedChemE/Cucurbitacin-B.html HYPERLINK https:/www.MedChemE/CWHM-12.html CWHM-12Cat. No.: HY-N0416 Cat. No.: HY-18644Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids; could represscancer cell progression.CWHM-12 is a potent inhibitor

40、of V integrins withIC50s of 0.2, 0.8, 1.5, and 1.8 nM for v8,v3, v6, and v1.Purity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.65%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Cy

41、clo_-RGDfK_.html Cyclo(-RGDfK) HYPERLINK https:/www.MedChemE/Cyclo_-RGDfK_.html HYPERLINK https:/www.MedChemE/cyclo-rgdfk-tfa.html Cyclo(-RGDfK) HYPERLINK https:/www.MedChemE/cyclo-rgdfk-tfa.html HYPERLINK https:/www.MedChemE/cyclo-rgdfk-tfa.html TFACat. No.: HY-P0023 Cat. No.: HY-P0023ACyclo(-RGDfK

42、) is a potent and selective inhibitorof the v3 integrin, with an IC50 of 0.94 nM.Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the v3 integrin on the cellsurface.Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the v3 integrin, with a

43、n IC50 of0.94 nM. Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the v3 integrin on the cellsurface.Purity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.81%Clinical Data: No Development Rep

44、ortedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Cyclo_Arg-Gly-Asp-D-Phe-Val_TFA.html Cyclo(Arg-Gly-Asp-D-Phe-Val) HYPERLINK https:/www.MedChemE/Cyclo_Arg-Gly-Asp-D-Phe-Val_TFA.html HYPERLINK https:/www.MedChemE/Cyclo_Arg-Gly-Asp-D-Phe-Val_TFA.html TFA HYPERLINK https:/www.Med

45、ChemE/Cyclo_Arg-Gly-Asp-D-Phe-Val_TFA.html HYPERLINK https:/www.MedChemE/Cyclo_RADfK_.html Cyclo(RADfK)Cat. No.: HY-P1613A Cat. No.: HY-P0031Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof integrin v3, with antitumor activity.Cyclo(RADfK) is a selective (v)(3) integrinligand that has been exten

46、sively used forresearch, therapy, and diagnosis ofneoangiogenesis.Purity: 99.40%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.03%Clinical Data: No Development ReportedSize: 1 mg HYPERLINK https:/www.MedChemE/cyclo-rgdyk.html Cyclo(RGDyK) HYPERLINK https:/www.MedChemE/cyclo-rgdyk.h

47、tml HYPERLINK https:/www.MedChemE/Cyclo_RGDyK_trifluoroacetate.html Cyclo(RGDyK) HYPERLINK https:/www.MedChemE/Cyclo_RGDyK_trifluoroacetate.html HYPERLINK https:/www.MedChemE/Cyclo_RGDyK_trifluoroacetate.html trifluoroacetateCat. No.: HY-100563A Cat. No.: HY-100563Cyclo(RGDyK) is a potent and select

48、ive V 3integrin inhibitor with an IC of 20 nM.50Cyclo(RGDyK) trifluoroacetate is a potent andselective integrin inhibitor with anV 3 IC50of 20 nM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg,

49、 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/E7820.html E7820(ER68203-00) Cat. No.: HY-14571 HYPERLINK https:/www.MedChemE/echistatin.html EchistatinCat. No.: HY-P1189E7820 (ER68203-00), an orally active aromaticsulfonamide derivative, is a u

50、nique angiogenesisinhibitor suppressing an expression of integrinalpha2 subunit on endothelium. E7820 inhibits rataorta angiogenesis with an IC of 0.11 g/ml.50Echistatin, the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms, is a potent inhibitorof

51、 platelet aggregation. Echistatin is a potentinhibitor of bone resorption in culture.Purity: 99.25%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/echistatin-tfa.html Echistatin H

52、YPERLINK https:/www.MedChemE/echistatin-tfa.html HYPERLINK https:/www.MedChemE/echistatin-tfa.html TFA HYPERLINK https:/www.MedChemE/echistatin-tfa.html HYPERLINK https:/www.MedChemE/emd527040.html EMD527040Cat. No.: HY-P1189A Cat. No.: HY-101473Echistatin TFA, the smallest active RGD proteinbelongi

53、ng to the family of disintegrins that arederived from snake venoms, is a potent inhibitorof platelet aggregation. Echistatin is a potentinhibitor of bone resorption in culture.EMD527040 is a potent and highly selective v6antagonist with antifibrotic activities. EMD527040can be used for carcinoma and

54、 liver fibrosisresearch.Purity: 95.13%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Eptifibatide.html Eptifibatide HYPERLINK https:/www.MedChemE/Eptifibatide.html HYPERLINK https:/www.MedChemE/ept

55、ifibatide-acetate.html Eptifibatide HYPERLINK https:/www.MedChemE/eptifibatide-acetate.html HYPERLINK https:/www.MedChemE/eptifibatide-acetate.html acetateCat. No.: HY-B0686 Cat. No.: HY-B0686AEptifibatide is a cyclic heptapeptide, acts as acompetitive antagonist for the activated plateletglycoprote

56、in IIb/IIIa receptor, with anti-plateletactivity.Eptifibatide acetate is a cyclic heptapeptide,acts as a competitive antagonist for the activatedplatelet glycoprotein IIb/IIIa receptor, withanti-platelet activity.Purity: 99.91%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mgPurity: 98%C

57、linical Data: LaunchedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/fibronectin.html Fibronectin HYPERLINK https:/www.MedChemE/fibronectin.html HYPERLINK https:/www.MedChemE/Firategrast.html FirategrastCat. No.: HY-P3160(SB 683699) Cat. No.: HY-14951Fibronectin, a glycoprotein (500 kDa) present inb

58、lood as well as in cells, is a biomarker oftissue injury. Fibronectin binds tomembrane-spanning receptor proteins calledintegrins.Firategrast (SB 683699) is an orally active andspecific 41/47 integrin antagonist.Firategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) andd

59、ecreases multiple sclerosis (MS) activity.Purity: 97.40%Clinical Data: No Development ReportedSize: 1 mgPurity: 99.88%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Fradafiban.html Fradafiban HYPERLINK https:/www.MedChemE/Fradafiban.html HYPERLINK ht

60、tps:/www.MedChemE/GLPG0187.html GLPG0187(BIBU-52) Cat. No.: HY-101720Cat. No.: HY-100506Fradafiban is a nonpeptide platelet glycoproteinIIb/IIIa antagonist, which binds to the humanplatelet GP IIb/IIIa complex with a K value ofd148 nM.GLPG0187 is a broad spectrum integrin receptorantagonist with ant