1072100-81-2
1072100-81-2 structure
- Name: PF-04577806
- Chemical Name: PF-04577806
- CAS Number: 1072100-81-2
- Molecular Formula: C26H37N7O3
- Molecular Weight: 495.62
- Catalog: Signaling Pathways Epigenetics PKC
- Create Date: 2022-01-13 17:42:27
- Modify Date: 2024-01-14 16:46:10
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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 |
|---|---|
| Synonyms |
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]- |
| 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 | |
| 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 |
| 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 |