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GR2-128

Chemical Structure : GR2-128

CAS No.:

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GR2-128

Catalog No.: PC-27013Not For Human Use, Lab Use Only.

GR2-128 is a potent, dual Mixed lineage kinase 3 (MLK3) and NAMPT inhibitor with IC50 of 84 nM and 14 nM respectively, inhibits antiproliferative in MDA-MB-468 TNBC cell line with GI50 of 42 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

GR2-128 is a potent, dual Mixed lineage kinase 3 (MLK3) and NAMPT inhibitor with IC50 of 84 nM and 14 nM respectively, inhibits antiproliferative in MDA-MB-468 TNBC cell line with GI50 of 42 nM.
GR2-128 attenuated tumorigenesis in a syngeneic mouse breast cancer model, increasing apoptosis via inhibition of MLK3 and NAMPT, attenuating macrophage and neutrophil infiltration and increasing tumor T-cell markers without change in B-cell count.

Physicochemical Properties

M.Wt 477.53
Formula C27H23N7O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(E)-N-(4-((6-phenoxy-9H-purin-2-yl)amino)phenethyl)-3-(pyridin-3-yl)acrylamide

References

1. Velma GR, et al. J Med Chem. 2026 Jun 10. doi: 10.1021/acs.jmedchem.5c03558.

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