For research use only. Not for therapeutic Use.
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].
| Catalog Number | I019723 |
| CAS Number | 2448286-21-1 |
| Synonyms | 6-methyl-12-[4-(4-methylpiperazin-1-yl)phenyl]-4-(1-methylpyrazol-4-yl)-3,5,8,10-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene;hydrochloride |
| Molecular Formula | C25H27ClN8 |
| Purity | ≥95% |
| InChI | InChI=1S/C25H26N8.ClH/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);1H |
| InChIKey | VBVBAEHNBOTZQV-UHFFFAOYSA-N |
| SMILES | CC1=C2C(=NC(=N1)C3=CN(N=C3)C)C4=C(N2)N=CC(=C4)C5=CC=C(C=C5)N6CCN(CC6)C.Cl |
| Reference | [1]. Vitorino P, et al. MAP4K4 regulates integrin-FERM binding to control endothelial cell motility. Nature. 2015 Mar 26;519(7544):425-30. |
