142557-61-7
142557-61-7 structure
- Name: A 484954
- Chemical Name: 7-amino-1-cyclopropyl-3-ethyl-2,4-dioxopyrido[2,3-d]pyrimidine-6-carboxamide
- CAS Number: 142557-61-7
- Molecular Formula: C13H15N5O3
- Molecular Weight: 289.29000
- Catalog: Signaling Pathways Neuronal Signaling CaMK
- Create Date: 2017-04-14 12:43:41
- Modify Date: 2025-08-25 08:14:50
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A-484954 is a highly selective eukaryotic elongationfactor-2 (eEF2) inhibitor, with an IC50 of 280 nM.
| Name | 7-amino-1-cyclopropyl-3-ethyl-2,4-dioxopyrido[2,3-d]pyrimidine-6-carboxamide |
|---|---|
| Synonyms |
Kinome_3822
7-AMino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxopyrido[2,3-d]pyriMidine-6-carboxaMide X5939 7-Amino-1-cyclopropyl-3-ethyl-1,2,3,4-tetrahydro-2,4-dioxo-pyrido[2,3-d]pyrimidine-6-carboxamide A 484954 A-484954 |
| Description | A-484954 is a highly selective eukaryotic elongationfactor-2 (eEF2) inhibitor, with an IC50 of 280 nM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 280 nM (eEF2)[1]. |
| In Vitro | A-484954 is a highly selective eEF2K inhibitor with an IC50 value of 280 nM against eEF2K in the enzymatic assay and little activity against a wide panel of serine/threonine and tyrosine kinases. In enzymatic assay, the IC50 value of A-484954 is increased as the concentration of ATP increased but unaffected by increasing concentrations of calmodulin[1]. |
| In Vivo | A484954 causes relaxation in E (+) and E (-) aorta or mesenteric artery precontracted with NA. Pretreatment with L-NAME but not indomethacin or cimetidine partially inhibits the A484954-induced relaxation in mesenteric artery[2]. Long-term A-484954 treatment inhibits MCT-induced increases PA pressure. It is revealed that A-484954 inhibits MCT-induced PA hypertrophy and fibrosis but not impairment of endothelium-dependent and -independent relaxation. Furthermore, A-484954 inhibits MCT-induced NADPH oxidase-1 expression and ROS generation as well as matrix metalloproteinase-2 activation[3]. |
| References |
| Density | 1.522±0.06 g/cm3 (20 ºC 760 Torr) |
|---|---|
| Molecular Formula | C13H15N5O3 |
| Molecular Weight | 289.29000 |
| Exact Mass | 289.11700 |
| PSA | 127.72000 |
| LogP | 0.40840 |
| Appearance | white to beige |
| Storage condition | 2-8°C |
| Water Solubility | DMSO: soluble 3mg/mL, clear (warmed) |
| Symbol |
GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301-H315-H319-H335 |
| Precautionary Statements | P261-P301 + P310-P305 + P351 + P338 |
| Hazard Codes | T |
| Risk Phrases | R25-36/37/38 |
| Safety Phrases | S26-45 |
| RIDADR | UN 2811 6.1 / PGIII |