GRP78-IN-3

Names

[ Name ]:
GRP78-IN-3

Biological Activity

[Description]:

GRP78-IN-3 is a selective Grp78 (HSPA5) inhibitor with an IC50 of 0.59 μM. GRP78-IN-3 is 7-fold selective for HspA5 compared to HspA9 (IC50 of 4.3 μM) and >20-fold selective for HspA5 compared to HspA2 (IC50 of 13.9 μM)[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> Metabolic Enzyme/Protease >> HSP

Signaling Pathways >> Cell Cycle/DNA Damage >> HSP

[Target]

HSPA5:0.59 μM (IC50)

[In Vitro]

GRP78-IN-3 (compound 8) is a potent small-molecule-competitive inhibitor of Hsp70 substrate binding. GRP78-IN-3 (0.1-100 μM) shows more potent inhibition efffects in a spheroid tumor model (U251 glioblastoma cells and H520 lung cancer cells)[1].

[References]

[1]. Andrew J Ambrose, et al. Discovery and Development of a Selective Inhibitor of the ER Resident Chaperone Grp78. J Med Chem. 2022 Dec 14.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₇H₁₈N₄O₂S

[ Molecular Weight ]:
342.42

GRP78-IN-3

Names

Biological Activity

Chemical & Physical Properties

Related Compounds