GRP78-IN-3

Modify Date: 2024-10-01 18:17:36

GRP78-IN-3 Structure
GRP78-IN-3 structure
Common Name GRP78-IN-3
CAS Number 2707510-30-1 Molecular Weight 342.42
Density N/A Boiling Point N/A
Molecular Formula C17H18N4O2S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GRP78-IN-3


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].

 Names

Name GRP78-IN-3

 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
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
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