PF-04577806 是一种有效、选择性和 ATP 竞争性的PKC抑制剂。PF-04577806 对PKCα，PKCβI，PKCβII，PKCγ和PKCθ显示出有效的抑制活性，IC50值分别为 2.4 nM、8.1 nM、6.9 nM、45.9 nM 和 29.5 nM。PF-04577806 可以逆转糖尿病大鼠的视网膜血管渗漏。
| 生物活性 | PF-04577806 is a potent, selective and ATP competitivePKCinhibitor. PF-04577806 shows potent inhibitory activity towardsPKCα,PKCβI,PKCβII,PKCγ, andPKCθwithIC50s 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[1]. |
| IC50& Target[1] | PKCα 2.4 nM (IC50) | PKCβI 8.1 nM (IC50) | PKCβII 6.9 nM (IC50) | PKCγ 45.9 nM (IC50) | PKCδ 586 nM (IC50) | PKCθ 29.5 nM (IC50) | PKCε 522 nM (IC50) |
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体外研究
(In Vitro) | PF-04577806 (0.001-10 μM; 10 min) inhibits PKC activity in diabetic rat retinal lysates, with IC50of 0.18 μM[1].
PF-04577806 (0.12-10 μM; pretreated for 60 min) inhibits phorbol myristate acetate-stimulated phosphorylation of ERK1/2 in Jurkat cells, with an IC50of 0.28 μM[1].
PF-04577806 (0.001-10 μM; pretreated for 1 h) inhibits phosphorylation of SHP2 in HEK293 cells, with an IC50of 5.8 nM. PF-04577806 concentration-dependently inhibits interleukin 8 release from phorbol myristate acetate-stimulated HEK293 cells, with an IC50of 0.12 μM[1].
PF-04577806 (1 μM; 48 h) shows low cytotoxicity against human umbilical vein endothelial cells with remaining cell viability at 100.5% viable[1].
Western Blot Analysis[1] | Cell Line: | Jurkat T cells | | Concentration: | 0, 0.12, 0.37, 1.11, 3.33, 10.0 μM | | Incubation Time: | Pretreated for 1 hours | | Result: | Showed a dose-dependent decrease in phospho-ERK1/2 but not total ERK1/2. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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