Antibodies
K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA.
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| Description | K02288 is a potent, and selective type I BMP receptor inhibitor with IC50 of 1.1, 1.8, 6.4 nM for ALK2, ALK1 andALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA. | |||||
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| Targets | ALK1 | ALK2 | ALK3 | ALK4 | ALK5 | ALK6 |
| IC50 | 1.8 nM | 1.1 nM | 34.4 nM | 302 nM | 321 nM | 6.4 nM [1] |
| In vitro | K02288 dose-dependently inhibits BMP4- and BMP6- induced Smad1/5/8 phosphorylation in C2C12 cells without affecting TGF-β-BMP signaling. [1] | |||||
| In vivo | In Zebrafish Embryos, K02288 induces a dorsalized phenotype in a dose dependent manner without effect om intersomitic vessel (ISV) formation. [1] | |||||
| Features | ||||||
| In vitro Kinase Assay for ALK1-6 | Kinase reactions for ALK1-6 are performed at room temperature for 45 minutes in 96-well plates mixing 2.5 nM kinase, 0.5 mg/mL dephosphorylated casein, 6 µM ATP, 0.05 µCi/µL [γ-32P]ATP, 10 mM MnCl2 and 0.2% BSA in kinase buffer. Inhibitors are added at concentrations between 0 and 10 µM in kinase reaction buffer and tested in triplicate. Reactions are quenched with phosphoric acid, bound to 96-well P81 phosphocellulose filter plates and assayed with Microscint 20 scintillation fluid using a Spectramax L luminometer. Data are normalized to untreated controls at 100% enzyme activity and negative controls subtracted as background. IC50 values are calculated using GraphPad. |
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| Animal Models | Zebrafish Embryos |
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| Dosages | ~10 µM |
| Administration |
| Molecular Weight (MW) | 352.38 |
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| Formula | C20H20N2O4 |
| CAS No. | 1431985-92-0 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 70 mg/mL (198 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 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 | 3-[(6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol |
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