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| Product Name: | KT5720 | | Synonyms: | (9R,10S,12S)-2,3,9,10,11,12-HEXAHYDRO-10-HYDROXY-9-METHYL-1-OXO-9,12-EPOXY-1H-DIINDOLO[1,2,3-FG:3',2',1'-KL]PYRROLO[3,4-I][1,6]BENZODIAZOCINE-10-CARBOXYLIC ACID, HEXYL ESTER;KT5720;PROTEIN KINASE INHIBITOR KT 5720;9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, hexyl ester, (9R,10S,12S)-;(9s,10s,12r)-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1h-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid hexyl ester;9,12-Epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-I][1,6]benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, hexyl ester, (9R,10R,12S)-rel-;Aids004395;Aids-004395 | | CAS: | 108068-98-0 | | MF: | C32H31N3O5 | | MW: | 537.61 | | EINECS: | 810-587-2 | | Product Categories: | antibiotic;Cyclic Nucleotide related | | Mol File: | 108068-98-0.mol |  |
| | KT5720 Chemical Properties |
| Boiling point | 715.0±60.0 °C(Predicted) | | density | 1.49±0.1 g/cm3(Predicted) | | storage temp. | −20°C | | solubility | methanol: 5 mg/mL | | form | powder | | pka | 11.96±0.40(Predicted) | | color | white | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months. |
| Hazard Codes | Xi | | Risk Statements | 36/38 | | Safety Statements | 26-36 | | WGK Germany | - | | F | 10 | | HS Code | 29419090 |
| | KT5720 Usage And Synthesis |
| Description | Protein kinase A (PKA) regulates multiple signal transduction events via protein phosphorylation and is integral to all cellular responses involving the cyclic AMP second messenger system. KT 5720 is one of a family of compounds synthesized by the fungus Nocardiopsis sp. It blocks PKA signaling through competitive inhibition of ATP with a Ki value of 60 nM. Reported IC50 values vary widely depending upon ATP concentration tested and can range from 56 nM (low ATP) to 3 μM (physiologic ATP). Non-specific effects of KT 5720 include inhibition of phosphorylase kinase, PDK1, MEK, MSK1, PKBα, and GSK3β at concentrations as effective as or more potent than that for inhibition of PKA. | | Chemical Properties | White solid | | Uses | KT 5720 is a potent, specific and cell-permeable inhibitor of PKA. | | Definition | ChEBI: An organic heterooctacyclic compound that is 1H,1'H-2,2'-biindole in which the nitrogens have undergone formal oxidative coupling to positions 2 and 5 of hexyl (3S)-3-hydroxy-2-methyltetrahydrofuran-3-
arboxylate (the 2R,3S,5S product), and in which the 3 and 3' positions of the biindole moiety have also undergone formal oxidative coupling to positions 3 and 4 of 1,5-dihydro-2H-pyrrol-
-one. | | Biological Activity | Potent, selective inhibitor of protein kinase A (K i = 60 nM). Has no effect on PKG or PKC (K i > 2 μ M). Reversibly arrests human skin fibroblasts in the G 1 phase. Also available as part of the Mixed Kinase Inhibitor Tocriset™ and PKA Tocriset™ . | | Biochem/physiol Actions | Cell permeable: yes | | storage | -20°C (desiccate) | | References | 1) Kase et al. (1987), K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases; Biochem. Biophys. Res. Commun., 142 436
2) Cabell et al. (1993), Effects of selective inhibition of protein kinase C, cyclic AMP-dependent protein kinase, and Ca(2+)-calmodulin-dependent protein kinase on neurite development in cultured rat hippocampal neurons; Int. J. Dev. Neurosci., 11 357 |
| | KT5720 Preparation Products And Raw materials |
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