BAG3/HSP70-IN-1

BAG3/HSP70-IN-1 (compound 16) is the first-in-class BAG3 and HSP70 dual inhibitor. BAG3/HSP70-IN-1 binds to BAG3 full-length, BAG3-BD, and HSP70 proteins with Kds of 33.10 μM, 27.90 μM, and 33.80 μM, respectively. BAG3/HSP70-IN-1 inhibits HeLa cells with an IC50 of 49.46 μM. BAG3/HSP70-IN-1 induces apoptosis by activating caspase 3 and caspase 9 levels in HeLa cells. BAG3/HSP70-IN-1 elevates p21 levels while reduces FOXM1 expression in HeLa cells. BAG3/HSP70-IN-1 decreases ATPase activity[1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; Caspase; HSP

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C(NCCCC)C(C1=CNC(NC1=O)=O)N(CC(C)CC)C(CN2N=NC(C3=CC(C)=C(C)C=C3C)=C2)=O

Molecular Formula

C28H39N7O4

Molecular Weight

537.65

References & Citations

[1]Ruggiero D, et al. Identification of the first-in-class dual inhibitor targeting BAG3 and HSP70 proteins to disrupt multiple chaperone pathways. Eur J Med Chem. 2025 Apr 5;287:117358.