GNE-220-Hydrochloride - MAP4K 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGNE 220 HydrochlorideCat. No.: HY-U00428A分式: CHClN分量: 474.99作靶点: MAP4K作通路: MAPK/ERK Pathway储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 5.4 mg/mL (11.37 mM; Need ultrasonic)Mass Solvent1

2、 mg 5 mg 10 mg Concentration制备储备液1 mM 2.1053 mL 10.5265 mL 21.0531 mL5 mM 0.4211 mL 2.1053 mL 4.2106 mL10 mM 0.2105 mL 1.0527 mL 2.1053 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶

3、液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.54 mg/mL (1.14 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.54 mg/mL (1.14 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 0.54 mg/mL (1.14 mM); Clear solution1/2 Mast

4、er of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 GNE 220 (Hydrochloride)种有效的选择性 MAP4K4 抑制剂，其 IC50 值为 7 nM。IC50 & Target MAP4K4 MAP4K5 MAP4K6 DMPK7 nM (IC50) 9 nM (IC50) 1.1 M (IC50) 476 nM (IC50)体外研究 GNE-220 also inhibits a few other kinases with IC50s of 9 nM, 476 nM and 1.1 M for MI

5、NK (MAP4K6),DMPK and KHS1 (MAP4K5), respectively. GNE-220 alters human umbilical vein endothelial cells (HUVEC)sprout morphology. GNE-220 also reduces pERM+ retraction fibres in a dose-dependent manner. GNE-220also dose-dependently increased the number of active-INT1+ long focal adhesions (FAs) 1.PR

6、OTOCOLCell Assay 1 HUVECs are cultured in complete EGM-2 (CC-3156 and CC-4176). HUVEC are assayed 3 days after siRNAtransfection. CHO cells are cultured in DMEM supplemented with 10% FBS, 1 mM Glutamate, andPenicillin/Streptomycin and transfected using Lipofectamine LTX. HUVEC sprouting assays are p

7、erformed.For siRNA treatment, HUVECs are transfected 1 day before coating to beads. For chemical inhibitor (e.g.,GNE-220, 0.1, 1, 10, 100, 1000 and 10000 nM) treatment, is added to media after fibrin is clotted. Forimmunofluorescence staining, beads are seeded in thin 100 L fibrin clots. For scratch

8、 wound healing assay,HUVEC are transfected 2 days before re-seeding into a glass-bottom 96-wells plate 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Vitorino P, et al. MAP4K4 regulates integrin-FERM binding to control endothelial cell motility. Nature. 2015 Mar 26;519(7544):425-30.McePdfHeightCaution: Product has not been fully validated for medical applicatio