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

Product information

CAS Number: 1199590-75-4

Molecular Weight: 438.53

Formula: C25H26N8

Chemical Name: 6-methyl-4-(1-methyl-1H-pyrazol-4-yl)-12-[4-(4-methylpiperazin-1-yl)phenyl]-3,5,8,10-tetraazatricyclo[7.4.0.0²,⁷]trideca-1(13),2,4,6,9,11-hexaene

Smiles: CC1N=C(N=C2C=1NC1=NC=C(C=C21)C1C=CC(=CC=1)N1CCN(C)CC1)C1C=NN(C)C=1

InChiKey: HXIPOURWZRATPT-UHFFFAOYSA-N

InChi: InChI=1S/C25H26N8/c1-16-22-23(30-24(28-16)19-14-27-32(3)15-19)21-12-18(13-26-25(21)29-22)17-4-6-20(7-5-17)33-10-8-31(2)9-11-33/h4-7,12-15H,8-11H2,1-3H3,(H,26,29)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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).

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