1. Epigenetics
    TGF-beta/Smad
  2. PKC
  3. PF-04577806

PF-04577806 

Cat. No.: HY-139467
Handling Instructions

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.

For research use only. We do not sell to patients.

PF-04577806 Chemical Structure

PF-04577806 Chemical Structure

CAS No. : 1072100-81-2

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Description

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[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)

In Vitro

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

495.62

Formula

C₂₆H₃₇N₇O₃

CAS No.
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PF-04577806
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HY-139467
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