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. 2020 Feb 7;10(10):1904–1925. doi: 10.1016/j.apsb.2020.01.018

Table 2.

Structures, mechanisms and activities of HSP70 inhibitors.

Name Year Structure Mechanism In vitro assay In vivo efficacy Ref.
VER-155008 2011 Image 25 ATPase inhibition Kd = 0.08 μmol/L Yesa 85, 86, 87, 88, 89, 90, 91, 92
Apoptozole 2015 Image 26 ATPase inhibition Low μmol/L Yes 93
MAL3-101 2004 Image 27 Disrupt HSP70–HSP40 (allosteric) Mid to high μmol/L Yes 94, 95, 96, 97
JG-231 2000 Image 28 Disrupt HSP70–BAG (allosteric) EC50 = 0.03 μmol/L Yes 98, 99
YK5 2014 Image 29 Allosteric on NBD Low to Mid μmol/L NAb 100
HS-72 2014 Image 30 Allosteric on SBD Mid μmol/L Yes 101
PES 2009 Image 31 Allosteric on SBD Not reported Yes 102
Novolactone 2015 Image 32 Covalently and allosteric on SBD IC50 = 0.25 μmol/L NA 103
a

Effective in vivo.

b

No activity.