K02288 1431985-92-0

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Molecular Weight:

352.38 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.

Biological Activity

K02288 dose-dependently inhibits BMP4- and BMP6- induced Smad1/5/8
phosphorylation in C2C12 cells without affecting TGF-β-BMP signaling.


In Zebrafish Embryos, K02288 induces a dorsalized phenotype in a dose
dependent manner without effect om intersomitic vessel (ISV) formation.






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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Product Categories : TGF-beta/Smad