Table 5 Preclinical studies of targeting other molecular chaperones

From: Advances in the structures, mechanisms and targeting of molecular chaperones

Compound

Structure

Activity

Mechanism (Sites)

Compound 2H

cIC50 = 5.0 µM

HSP110 Inhibitor (/)

iHSP110-33

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bIC50 = 58 μM

HSP110 Inhibitor (NBD)

GdnHCl

Kd ≈ 600 μM

ClpB Inhibitor (NTD)

DBeQ

aIC50 ≈ 5.0 μM

ClpB Inhibitor (NTD)

Mizoribine

/

HSP60 inhibitor (NBD)

ETB

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cIC50 = 1.1 μM

HSP60 inhibitor (Cys442 covalent site)

MC

/

HSP60 inhibitor (/)

O-carboranyl-phenoxyacetanilide

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cIC50 = 0.74 μM

HSP60 inhibitor (NBD)

[Au(TPP)Cl]

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cIC50 = 1.1 μM

HSP60 inhibitor (/)

KHS101

cIC50 = 14 μM

HSP60 inhibitor (/)

RP101

/

HSP27 inhibitor (Phe29 and Phe33)

J2

cIC50 = 99 μM

HSP27 inhibitor (Cysteine-thiol group)

MK-933

/

HSP27 inhibitor (NTD)

  1. Kd target binding affinity, aIC50 ATPase inhibitor activity, bIC50 competitive binding activity, cIC50 inhibitory activity on molecular chaperone functions, “/” indicates no clear reports