产品
编 号：F742361
分子式：C26H37N7O3
分子量：495.62
分子式：C26H37N7O3
分子量：495.62
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CAS No: 1072100-81-2
产品详情
生物活性：
PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats.
体外研究：
PF-04577806 (0.001-10 μM; 10 min) inhibits PKC activity in diabetic rat retinal lysates, with IC50 of 0.18 μM.PF-04577806 (0.12-10 μM; pretreated for 60 min) inhibits phorbol myristate acetate-stimulated phosphorylation of ERK1/2 in Jurkat cells, with an IC50 of 0.28 μM.PF-04577806 (0.001-10 μM; pretreated for 1 h) inhibits phosphorylation of SHP2 in HEK293 cells, with an IC50 of 5.8 nM. PF-04577806 concentration-dependently inhibits interleukin 8 release from phorbol myristate acetate-stimulated HEK293 cells, with an IC50 of 0.12 μM.PF-04577806 (1 μM; 48 h) shows low cytotoxicity against human umbilical vein endothelial cells with remaining cell viability at 100.5% viable.
PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats.
体外研究：
PF-04577806 (0.001-10 μM; 10 min) inhibits PKC activity in diabetic rat retinal lysates, with IC50 of 0.18 μM.PF-04577806 (0.12-10 μM; pretreated for 60 min) inhibits phorbol myristate acetate-stimulated phosphorylation of ERK1/2 in Jurkat cells, with an IC50 of 0.28 μM.PF-04577806 (0.001-10 μM; pretreated for 1 h) inhibits phosphorylation of SHP2 in HEK293 cells, with an IC50 of 5.8 nM. PF-04577806 concentration-dependently inhibits interleukin 8 release from phorbol myristate acetate-stimulated HEK293 cells, with an IC50 of 0.12 μM.PF-04577806 (1 μM; 48 h) shows low cytotoxicity against human umbilical vein endothelial cells with remaining cell viability at 100.5% viable.
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