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Cat. No. Product Name CAS No. Information
PC-62001

MK-0429

227963-15-7

MK-0429 is a potent, selective, orally-active nonpeptide αvβ3 integrin inhibitor with IC50 of 0.08 nM in SPAV3 assay; displays approximately 100-fold selectivity for αvβ3 over αvβ5 (IC50=10 nM), and no significant activity for the fibrinogen receptor αIIBβ3 (IC50>30 uM); shows activity in different animal models of bone turnover and has potentiation for the prevention and treatment of osteoporosis; also reduces melanoma metastasis both in vitro and in vivo.

Prostate Cancer

Phase 1 Discontinued

PC-70068

Cyclo(RGDyK)

250612-42-1

Cyclo(RGDyK) (Cyclic Arg-Gly-Asp-D-Tyr-Lys) is a cyclic derivative of RGD, potent, selective αVβ3 integrin inhibitor with IC50 of 20 nM; a recognition motif used by extracellular matrix proteins (vitronectin, fibrinogen, laminin, and collagen) to bind to a variety of integrins including αvβ3.

PC-60070

GSK-3008348 hydrochloride

1629249-40-6

GSK-3008348 hydrochloride is a novel potent, selective integrin αvβ6 antagonist for the treatment of idiopathic pulmonary fibrosis (IPF).

Cystic Fibrosis

Phase 1 Clinical

PC-60069

GSK-3008348

1629249-33-7

GSK-3008348 is a novel potent, selective integrin αvβ6 antagonist for the treatment of idiopathic pulmonary fibrosis (IPF).

Cystic Fibrosis

Phase 1 Clinical

PC-45519

OSU-T315

1333146-24-9

A novel potent, orally active ILK (integrin-linked kinase) inhibitor with IC50 of 0.6 uM; exhibits high in vitro potency against a panel of prostate and breast cancer cell lines (IC50=1-2.5 uM) with no effect on normal epithelial cells; facilitates the dephosphorylation of Akt at Ser-473 and other ILK targets, including GSK-3β and myosin light chain; suppresses the expression of the transcription/translation factor YB-1 and HER2, EGFR in PC-3 cells, induces autophagy and apoptosis; demonstrates in vivo efficacy in suppressing PC-3 xenograft tumor growth; orally active.

PC-42179

GLPG-0187

1320346-97-1

GLPG-0187 (GLPG0187) is a highly potent, broad spectrum integrin receptor antagonist with IC50 of 1-10 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1; significantly inhibits angiogenesis both in vivo and in vitro, osteoclastogenesis in vitro, and bone loss in vivo; inhibits de novo formation and progression of bone and visceral metastases in prostate cancer and breast cancer mice models.

Solid Tumors

Phase 1 Clinical

PC-35719

Valategrast hydrochloride

828271-96-1 Valategrast hydrochloride is a potent, α4β1 (VLA-4) and α4β7 dual antagonist.

Asthma

Discontinued

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