H-7, Dihydrochloride is a cell-permeable, reversible, ATP-competitive Ser/Thr kinase inhibitor. H-7 is a broad spectrum kinase inhibitor that has been shown to inhibit MYLK (MLCK) (Ki=97 µM), cAMP-dependent protein kinase (PKA) (Ki = 3.0 uM), Protein Kinase C (PKC) (Ki = 6.0 uM), and cGMP-dependent protein kinase (cGKI, PKG) (Ki = 5.8 uM). H-7 inhibits cell invasion and metastasis in B16BL6 cancer cells through the PKC/MEK/ERK pathway. This compound is shown to inhibit Topo I and II in murine L929 cells and induce apoptosis through PKC inhibition.
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Soluble in water (20 g/l) at 20° C, 100% ethanol, and DMSO (75 mM).
Store at -20° C
495.3° C at 760 mmHg (Predicted)
cAMP-dependent protein kinase, gamma catalytic subunit: IC50 = 3.5 µM (human); cAMP-dependent protein kinase alpha-catalytic subunit: IC50 = 3.5 µM (human); cAMP-dependent protein kinase beta-1 catalytic subunit: IC50 = 3.5 µM (human); Protein kinase C zeta: IC50 = 6 µM (human); Protein kinase C mu: IC50 = 6 µM (human)
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Arao M; et alArao M; et al. (PubMed ID: 7804449) determined that H-7, Dihydrochloride completely blocked the PTH-induced increase in inorganic phosphate uptake in the at osteosarcoma cell line, UMR-106. -SCBT Publication Review
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