GNE 220 Hydrochloride

目录号: GC34208纯度: >98.00%

GNE220(Hydrochloride)是一种有效的选择性MAP4K4抑制剂，其IC50值为7nM。

Cas No.: 2448286-21-1

规格	价格	库存	数量
5mg	¥5,801.00	现货	1
10mg	¥10,710.00	现货	1
25mg	¥23,205.00	现货	1
10mM (in 1mL DMSO)	¥6,382.00	现货	1

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187(9):2288-2304 (2024)
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183(7):1867-1883 (2020)
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产品描述 Description

GNE 220 (Hydrochloride) is a potent and selective inhibitor of MAP4K4, with an IC50 of 7 nM.

GNE-220 also inhibits a few other kinases with IC50s of 9 nM, 476 nM and 1.1 μM for MINK (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-220 also dose-dependently increased the number of active-INTβ1+ long focal adhesions (FAs)[1].

[1]. Vitorino P, et al. MAP4K4 regulates integrin-FERM binding to control endothelial cell motility. Nature. 2015 Mar 26;519(7544):425-30.

实验参考方法 Experimental Reference Method

Cell experiment:

HUVECs are cultured in complete EGM-2 (CC-3156 and CC-4176). HUVEC are assayed 3 days after siRNA transfection. CHO cells are cultured in DMEM supplemented with 10% FBS, 1 mM Glutamate, and Penicillin/Streptomycin and transfected using Lipofectamine LTX. HUVEC sprouting assays are performed. 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. For immunofluorescence staining, beads are seeded in thin 100 μL fibrin clots. For scratch wound healing assay, HUVEC are transfected 2 days before re-seeding into a glass-bottom 96-wells plate[1].

References:

[1]. Vitorino P, et al. MAP4K4 regulates integrin-FERM binding to control endothelial cell motility. Nature. 2015 Mar 26;519(7544):425-30.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

CAS 号

2448286-21-1

SMILES

CN1N=CC(C2=NC(C)=C(NC3=NC=C(C4=CC=C(N5CCN(C)CC5)C=C4)C=C36)C6=N2)=C1.Cl

分子式

C₂₅H₂₇ClN₈

分子量

474.99 g/mol

溶解性

DMSO : 5.4 mg/mL (11.37 mM)

保存条件

Store at -20°C

General tips

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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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