K02288

K02288

Catalog Number:
L002370432APE
Mfr. No.:
APE-B2286
Price:
$305
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      • Overview
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          Background

          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].

          [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.

      • Properties
        • Alternative Name
          3-[6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenol
          CAS Number
          1431985-92-0
          Molecular Formula
          C20H20N2O4
          Molecular Weight
          352.38
          Appearance
          A solid
          Purity
          99.91%
          Solubility
          insoluble in H2O; ≥17.6 mg/mL in DMSO; ≥2.5 mg/mL in EtOH with gentle warming and ultrasonic
          Storage
          Store at -20°C

          * For Research Use Only

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