GNE 220 Hydrochloride
目录号 : GC34208
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
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 2448286-21-1 | SDF | |
| Canonical 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 |
| 溶解度 | DMSO : 5.4 mg/mL (11.37 mM) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1053 mL | 10.5265 mL | 21.0531 mL |
| 5 mM | 0.4211 mL | 2.1053 mL | 4.2106 mL |
| 10 mM | 0.2105 mL | 1.0527 mL | 2.1053 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet