GNE-220( GNE220 )

Catalog No. M10715 CAS No. 1199590-75-4

COA

Datasheet

HNMR

HPLC

MSDS

Handing Instructions

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Product Name

GNE-220
Note

Research use only, not for human use.
Brief Description

GNE-220 is a potent and selective inhibitor of MAP4K4 with IC50 of 7 nM.
Description

GNE-220 is a potent and selective inhibitor of MAP4K4 with IC50 of 7 nM, also inhibits MINK (MAP4K6), DMPK and KHS1 (MAP4K5) with IC50 of 9 nM, 476 nM and 1,110 nM; alters HUVEC sprout morphology, shifts the distribution of subcellular protrusion and increases total protrusions, dose-dependently increases the number of β1-integrin in long focal adhesions.
In Vitro

GNE-220 also inhibits a few other kinases with IC50s of 9nM, 476 nM and 1.1μM 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).
In Vivo

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Synonyms

GNE220
Pathway

MAPK/ERK Signaling
Target

MAP4K
Recptor

MAP4K
Research Area

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Indication

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CAS Number

1199590-75-4
Formula Weight

438.539
Molecular Formula

C25H26N8
Purity

>98% (HPLC)
Solubility

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SMILES

CC1=C2C(=NC(=N1)C3=CN(N=C3)C)C4=C(N2)N=CC(=C4)C5=CC=C(C=C5)N6CCN(CC6)C
Chemical Name

4-Methyl-8-[4-(4-methyl-1-piperazinyl)phenyl]-2-(1-methyl-1H-pyrazol-4-yl)-5H-pyrido[3',2':4,5]pyrrolo[3,2-d]pyrimidine

1. Vitorino P, et al. Nature. 2015 Mar 26;519(7544):425-30. 2. Gao X, et al. Cell Biosci. 2016 Oct 28;6:56. eCollection 2016.

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