PF-04577806

Modify Date: 2024-01-14 16:46:10

PF-04577806 structure	Common Name	PF-04577806
	CAS Number	1072100-81-2	Molecular Weight	495.62
	Density	1.2±0.1 g/cm3	Boiling Point	613.4±55.0 °C at 760 mmHg
	Molecular Formula	C₂₆H₃₇N₇O₃	Melting Point	N/A
	MSDS	N/A	Flash Point	324.8±31.5 °C

Use of 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[1].

Name	PF-04577806
Synonym	More Synonyms

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].
Related Catalog	Signaling Pathways >> Epigenetics >> PKC Research Areas >> Metabolic Disease Signaling Pathways >> TGF-beta/Smad >> PKC
Target	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]. 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.
References	[1]. Grant S, et, al. Discovery of a novel class of targeted kinase inhibitors that blocks protein kinase C signaling and ameliorates retinal vascular leakage in a diabetic rat model. Eur J Pharmacol. 2010 Feb 10;627(1-3):16-25.

Density	1.2±0.1 g/cm3
Boiling Point	613.4±55.0 °C at 760 mmHg
Molecular Formula	C₂₆H₃₇N₇O₃
Molecular Weight	495.62
Flash Point	324.8±31.5 °C
Exact Mass	495.295776
LogP	2.02
Vapour Pressure	0.0±1.8 mmHg at 25°C
Index of Refraction	1.602

N-(5-{[(2S,5R)-2,5-Dimethyl-4-(tetrahydro-2H-pyran-4-ylmethyl)-1-piperazinyl]carbonyl}-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl)-2-pyridinecarboxamide

PF-04577806

2-Pyridinecarboxamide, N-[5-[[(2S,5R)-2,5-dimethyl-4-[(tetrahydro-2H-pyran-4-yl)methyl]-1-piperazinyl]carbonyl]-1,4,5,6-tetrahydro-6,6-dimethylpyrrolo[3,4-c]pyrazol-3-yl]-

DC Chemicals Limited
China
Product Name: PF-04577806
Price: ￥Inquiry/1g
Purity: 98.9%
Stocking Period: 1 Day
Contact: Tony Cao

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