PF-04577806
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.
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- No. CAS: 1072100-81-2
- Fòrmula: C26H37N7O3
- Peso molecular:495.62
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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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) |
PF-04577806 (0.001-10 μM; 10 min) inhibits PKC activity in diabetic rat retinal lysates, with IC50 of 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 IC50 of 0.28 μM[1].
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[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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat T cells
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Concentration:0, 0.12, 0.37, 1.11, 3.33, 10.0 μM
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Incubation Time:Pretreated for 1 hours
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Result:Showed a dose-dependent decrease in phospho-ERK1/2 but not total ERK1/2.
Chemical Information
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No. CAS 1072100-81-2
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Peso molecular 495.62
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Fòrmula C26H37N7O3
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SMILES
O=C(C1=CC=CC=N1)NC2=NNC3=C2CN(C(N4[C@H](CN([C@@H](C4)C)CC5CCOCC5)C)=O)C3(C)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PF-04577806 Related Classifications
HY-139467 Related Classifications
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