K02288 - TGF-β Receptor 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEK02288Cat. No.: HY-12278CAS No.: 1431985-92-0分式: CHNO分量: 352.38作靶點(diǎn): TGF- Receptor作通路: TGF-beta/Smad儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 58.6 mg/mL (166.30 mM)* means soluble, but

2、 saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.8378 mL 14.1892 mL 28.3785 mL5 mM 0.5676 mL 2.8378 mL 5.6757 mL10 mM 0.2838 mL 1.4189 mL 2.8378 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備

3、液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.09 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (7.09 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Mole

4、cules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (7.09 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 K02288種有效的形態(tài)發(fā)蛋 (BMP) I型受體抑制劑，抑制ALK1，ALK2，ALK6的 IC50 為1.8，1.1，6.4 nM。對 ALK3 和 ALK6 的抑制稍弱，IC50在5-34 nM之間。IC50 & Target IC50：1.8 nM (ALK1), 1.1 nM (ALK2), 34.4 nM (ALK3), 6.3 nM (ALK6), 302 nM (ALK4), 321 nM

5、(ALK5) 1體外研究 K02288 reduces a robust phosphorylation of Smad1/5/8 induced by BMP4 stimulation, with an apparent IC50of 100 nM. K02288 causes near complete inhibition of Smad2 phosphorylation at 0.5 M 1. K02288 binds toALK1 in an ATP-mimetic fashion with two hydrogen bonds to the kinase hinge. K02288

6、 also inhibits BMP9-ALK1 signalling, and induces a hypersprouting phenotype in HUVECs 2.體內(nèi)研究 K02288 (1 M) induces dysfunctional angiogenesis in a chick embryo CAM model 2.REFERENCES1. 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. 2015Apr;18(2):209-17.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only