product name K02288
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 and ALK6, showing weaker inhibition on other ALKs (3, 4, 5) and ActRIIA. K02288 has in vitro activity against ALK2 at low nanomolar concentrations similar to the current lead compound LDN-193189. K02288 specifically inhibited the BMP-induced Smad pathway without affecting TGF-β signaling and induced dorsalization of zebrafish embryos.
References: PLoS One. 2013 Apr 30;8(4):e62721.
352.38
Formula
C20H20N2O4
CAS No.
1431985-92-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 70 mg/mL (198.6 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: K02288 dose-dependently inhibits BMP4- and BMP6- induced Smad1/5/8 phosphorylation in C2C12 cells without affecting TGF-β-BMP signaling. Kinase Assay: In a panel of 200 human kinases, it shows more than 50% inhibition against only ABL and ARG at 0.1μM and only a further 6 kinases at 1μM. Cell Assay: In C2C12 cells, it reduces the phosphorylation of Smad dose-dependently when using BMP4 or BMP6 as ligands. Furthermore, K02288 induces a dorsalized phenotype in Tg(BRE:mRFP) transgenic zebrafish embryos. |
|---|---|
| In Vivo | In Zebrafish Embryos, K02288 induces a dorsalized phenotype in a dose dependent manner without effect om intersomitic vessel (ISV) formation. |
| Animal model | |
| Formulation & Dosage | |
| References | PLoS One. 2013 Apr 30;8(4):e62721. |
