1. MAPK/ERK Pathway
  2. MAP4K

GNE 220 Hydrochloride 

Cat. No.: HY-U00428A Purity: 98.32%
Handling Instructions

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

For research use only. We do not sell to patients.

GNE 220 Hydrochloride Chemical Structure

GNE 220 Hydrochloride Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 715 In-stock
Estimated Time of Arrival: December 31
5 mg USD 650 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2600 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Other Forms of GNE 220 Hydrochloride:

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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

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

IC50 & Target

MAP4K4

7 nM (IC50)

MAP4K5

9 nM (IC50)

MAP4K6

1.1 μM (IC50)

DMPK

476 nM (IC50)

In Vitro

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].

Solvent & Solubility
In Vitro: 

DMSO : 5.4 mg/mL (11.37 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.54 mg/mL (1.14 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.54 mg/mL (1.14 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.54 mg/mL (1.14 mM); Clear solution

References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

474.99

Formula

C₂₅H₂₇ClN₈

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
GNE 220 Hydrochloride
Cat. No.:
HY-U00428A
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GNE 220 Hydrochloride

Cat. No.: HY-U00428A