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K02288

Catalog No.
B2286
ALK inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$149.00
In stock
10mg
$135.00
In stock
50mg
$450.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

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].

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt352.38
Cas No.1431985-92-0
FormulaC20H20N2O4
Solubility≥17.6mg/mL in DMSO
Chemical Name3-[6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenol
SDFDownload SDF
Canonical SMILESCOC1=CC(=CC(=C1OC)OC)C2=C(N=CC(=C2)C3=CC(=CC=C3)O)N
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

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

Chemical structure

K02288