K02288
K02288 is a highly selective inhibitor of ALK2 with IC50 value of 1.1nM [1].
K02288 is a 2-aminopyridine inhibitor of ALK2. It shows high selectivity for the homologous kinases ALK1-6 and ActRIIA. K02288 shows potency against the type I BMP receptors ALK1, ALK2 (IC50s range from 1–2nM), ALK3 and ALK6 (IC50s of 5–34nM), ALK4 (IC50 of 302nM) and ALK5 (IC50 of 321nM). K02288 has a favorable kinome-wide selectivity. 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 [1].
K02288 also affects ALK2 related BMP signaling. 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 [1].
References:
[1] Sanvitale CE, Kerr G, Chaikuad A, Ramel MC, Mohedas AH, Reichert S, Wang Y, Triffitt JT, Cuny GD, Yu PB, Hill CS, Bullock AN. A new class of small molecule inhibitor of BMP signaling. PLoS One. 2013 Apr 30;8(4):e62721.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 352.38 |
| Cas No. | 1431985-92-0 |
| Formula | C20H20N2O4 |
| Solubility | insoluble in H2O; ≥17.6 mg/mL in DMSO; ≥2.5 mg/mL in EtOH with gentle warming and ultrasonic |
| Chemical Name | 3-[6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenol |
| SDF | Download SDF |
| Canonical SMILES | COC1=CC(=CC(=C1OC)OC)C2=C(N=CC(=C2)C3=CC(=CC=C3)O)N |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | K02288 is a potent, and selective inhibitor of type I BMP receptor with IC50 values of 1.1, 1.8, 6.4 nM for ALK2, ALK1 and ALK6,respectively. | |||||
| Targets | ALK2 | ALK1 | ALK6 | ALK3 | ALK4 | ALK5 |
| IC50 | 1.1 nM | 1.8 nM | 6.4 nM | 34.4 nM | 302 nM | 321 nM |
Quality Control & MSDS
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Chemical structure
