[CAS NO. 2448286-21-1] GNE 220 hydrochloride
PRODUCTS SPECIFICATIONS [2448286-21-1]
DESCRIPTION [2448286-21-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 474.99 |
| Molecular 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 |
Summary
GNE 220 (hydrochloride) is a potent and selective inhibitor of MAP4K4 , with an IC 50 of 7 nM.
IC50 & Target
|
MAP4K4 7 nM (IC 50 ) |
MAP4K5 9 nM (IC 50 ) |
MAP4K6 1.1 μM (IC 50 ) |
DMPK 476 nM (IC 50 ) |
In Vitro
GNE-220 also inhibits a few other kinases with IC 50 s 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 5.4 mg/mL ( 11.37 mM ; Need ultrasonic)
H 2 O : 5 mg/mL ( 10.53 mM ; Need ultrasonic)
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 |
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1.
Add each solvent one by one: PBS
Solubility: 11.11 mg/mL (23.39 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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2.
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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
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 0.54 mg/mL (1.14 mM); Clear solution