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3895-92-9COc1ccc2c(c[n+](C)c3c4cc5c(cc4ccc23)OCO5)c1OC.[Cl-]WEEFNMFMNMASJY-UHFFFAOYSA-M3895-92-9DTXSID70893481CHEMBL258893CHEBI:201466化学的特性yellow to orange solid
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説明Chelerythrine is a potent, cell permeable inhibitor of protein kinase C (IC50 = 660 nM) that does not inhibit tyrosine protein kinases, cAMP-dependent protein kinase, or calcium/calmodulin-dependent protein kinase. Chelerythrine also inhibits Bcl-xL function (IC50 = 1.5 μM) by displacing Bax binding, inducing apoptosis in several cancer cell lines. Chelerythrine can also have PKC-independent effects, activate p38 MAP kinase and JUNK signaling pathways, and induce apoptosis in cancer cells both in vitro and in vivo.
使用Chelerythrine Chloride is a cell permeable protein kinase C (PKC) inhibitor.
一般的な説明Naturally occurring alkaloid. Cell-permeable, selective inhibitor of protein kinase C (IC50 = 660 nM). Acts on the catalytic domain irrespective of the attachment of the regulatory domain. Material is a competitive inhibitor with respect to the phosphate acceptor and a non-competitive inhibitor with respect to ATP. Over ten-fold more potent than H-7, HCl (Cat. No. 371955). Inhibits thromboxane formation and phosphoinositide metabolism in platelets. Also induces apoptotic DNA fragmentation and cell death in HL-60 human promyelocytic leukemia cells.
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