Antibodies
FMK
- 貨號 Cat. No.
- S7064
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
FMK
Catalog No.S7064
FMK is a potent and selective inhibitor of p90 ribosomal protein S6 kinaseRSK2 (wt) with IC50 of 15 nM, >600- and 200-fold selectivity for RSK2 than the C436V and T493M mutants.
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Biological Activity
| Description | FMK is a potent and selective inhibitor of p90 ribosomal protein S6 kinaseRSK2 (wt) with IC50 of 15 nM, >600- and 200-fold selectivity for RSK2 than the C436V and T493M mutants. | |||||
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| Targets | RSK2 | |||||
| IC50 | 15 nM [1] | |||||
| In vitro | FMK inhibits the activity of RSK2 with IC50 of 15 nM. FMK suppresses EGF induced Ser386 phosphorylation of endogenous RSK2 in serum-starved COS-7 cells with EC50 of ~200 nM. [1] Pretreatment of myocytes with FMK before exposure to the α1-adrenoceptor agonist phenylephrine inhibited RSK C-terminal kinase activity and thereby RSK N-terminal kinase activation, without affecting MEK or ERK activation. Pretreatment of myocytes with fmk also inhibited phenylephrine-induced increases in NHE1 phosphorylation and the rate of NHE1-mediated H+ efflux under conditions of intracellular acidosis. [2] | |||||
| In vivo | ||||||
| Features | ||||||
Protocol(Only for Reference)
Kinase Assay: [1]
| RSK2 kinase assay | RSK2 CTDs are expressed inE. coli as His6-tagged proteins and activated by incubation with bacterially expressed His6-ERK2 and ATP. Kinase assay conditions: 30 min inhibitor pretreatment, 1 nM RSK2 CTD, 0.1 mM ATP, 0.1 mM ‘‘CTD-tide’’ substrate. |
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References
Chemical Information
| Molecular Weight (MW) | 342.37 |
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| Formula | C18H19FN4O2 |
| CAS No. | 821794-92-7 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | mg/mL (<1 mM) |
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| Water | mg/mL (<1 mM) | ||
| Ethanol | mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | Ethanone, 1-[4-amino-7-(3-hydroxypropyl)-5-(4-methylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]-2-fluoro- |
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