Table 4.
Preclinical studies of targeting HSP70
Compound | Structure | Activity | Mechanism (Sites) |
---|---|---|---|
VER-155008 | ![]() |
bIC50 = 0.50 μM | Pan-HSP70 inhibitor (NBD) |
methylene blue | ![]() |
/ | Pan-HSP70 inhibitor (NBD) |
YK-5 | ![]() |
cIC50 = 0.80 μM (SkBr3 cells) | Pan-HSP70 inhibitor (NBD) |
PES | ![]() |
/ | Pan-HSP70 inhibitor (SBD) |
AEAC | ![]() |
Kd = 149 nM | Pan-HSP70 inhibitor (SBD) |
Apoptozole | ![]() |
HSP70i: Kd = 0.14 μM; HSC70: Kd = 0.21 μM |
HSP70i/HSC70 selective inhibitor (NBD) |
HS-72 | ![]() |
/ | HSP70i selective inhibitor (NBD) |
Pinaverium bromide | ![]() |
cIC50 = 10 μM (A2058 cells) | HSC70 selective inhibitor (NBD) |
EGCG | ![]() |
Kd = 0.70 μM | GRP78 selective inhibitor (NBD) |
HA15 | ![]() |
aIC50 = 25–50 μM | GRP78 selective inhibitor (NBD) |
YUM70 | ![]() |
aIC50 = 1.5 μM | GRP78 selective inhibitor (SBD) |
Hexachlorophene | ![]() |
dIC50 = 9.1 μM | GRP78 selective inhibitor (SBD) |
TPP-apoptozole | ![]() |
/ | GRP75 selective inhibitor (SBD) |
MAL3-101 | ![]() |
/ | HSP70-HSP40 PPI inhibitor (NBD) |
S1g-2 | ![]() |
eIC50 = 0.40 μM; Kd = 0.84 μM |
HSP70-BIM PPI inhibitor (NBD) |
YM-1 | ![]() |
eIC50 = 4.8 μM; Kd = 5.8 μM |
HSP70-BAGs PPI inhibitor (NBD) |
JG-98 | ![]() |
eIC50 = 1.6 μM; Kd = 86 nM |
HSP70-BAGs PPI inhibitor (NBD) |
SY7 | ![]() |
/ | HSP70-HOP PPI inhibitor (SBD) |
SY8 | ![]() |
/ | HSP70-HOP PPI inhibitor (SBD) |
Kd target binding affinity; Ki target binding affinity; aIC50 ATPase inhibitor activity; bIC50 competitive binding activity; cIC50 anti-proliferative activity; dIC50 substrate competitive inhibitory activity; eIC50 PPIs inhibitory activity; “/” indicates no clear reports