K02288
目录号: PL11857 纯度: ≥99%
CAS No. :1431985-92-0
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中文名称
K02288
中文别名
K02288 抑制剂;3-[6-氨基-5-(3,4,5-三甲氧苯基)吡啶-3-基]苯酚
英文名称
K02288
英文别名
K 02288;3-[6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol;K02288​;K-02288;3-[(6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]phenol;3-[6-Amino-5-(3,4,5-trimethoxyphenyl)-3-pyridinyl]-phenol;3-[6-Amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl]phenol;K02288;3-(6-amino-5-(3,4,5-trimethoxyphenyl)pyridin-3-yl)phenol;A3F;SYN5187;AOB4291;HMS3653M16;BDBM102619;K02288a;BCP09946;s7359;K 02288a;FD5034;SB19486;BC600483;AK175599;Y1876;K02288, >98% (HPLC);SW220200-1;A14311;Phenol
Cas No.
1431985-92-0
分子式
C20H20N2O4
分子量
352.38
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
K02288是一种有效的骨形态发生蛋白 (BMP) I 型受体抑制剂,抑制 ALK1,ALK2,ALK6 的 IC50 为1.8,1.1,6.4 nM。对 ALK3 和 ALK6 的抑制稍弱,IC50在 5-34 nM 之间。
生物活性
K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC 50 s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC 50 s of of 5-34 nM.
性状
Solid
IC50 & Target[1][2]
IC50:1.8 nM (ALK1), 1.1 nM (ALK2), 34.4 nM (ALK3), 6.3 nM (ALK6), 302 nM (ALK4), 321 nM (ALK5)
体外研究(In Vitro)
K02288 reduces a robust phosphorylation of Smad1/5/8 induced by BMP4 stimulation, with an apparent IC50 of 100 nM. K02288 causes near complete inhibition of Smad2 phosphorylation at 0.5 μM. K02288 binds to ALK1 in an ATP-mimetic fashion with two hydrogen bonds to the kinase hinge. K02288 also inhibits BMP9-ALK1 signalling, and induces a hypersprouting phenotype in HUVECs. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
K02288 (1 μM) induces dysfunctional angiogenesis in a chick embryo CAM model. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Sanvitale CE, et al. A new class of small molecule inhibitor of BMP signaling. PLoS One. 2013 Apr 30;8(4):e62721.
[2]. Kerr G, et al. A small molecule targeting ALK1 prevents Notch cooperativity and inhibits functional angiogenesis. Angiogenesis. 2015 Apr;18(2):209-17.
溶解度数据
In Vitro: DMSO : ≥ 58.6 mg/mL (166.30 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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