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K02288
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
K02288图片
CAS NO:1431985-92-0
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
10mg电议
50mg电议

产品介绍
K02288 是一种有效的骨形态发生蛋白 (BMP) I 型受体抑制剂,对 ALK1、ALK2 和 ALK6 的 IC50 分别为 1.8、1.1、6.4 nM。
Cas No.1431985-92-0
化学名3-[6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenol
Canonical SMILESCOC1=CC(=CC(=C1OC)OC)C2=C(N=CC(=C2)C3=CC(=CC=C3)O)N
分子式C20H20N2O4
分子量352.38
溶解度≥ 17.6mg/mL in DMSO
储存条件Store at -20° C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.