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. 2015 Oct 16;5(4):2589–2618. doi: 10.3390/biom5042589

Table 1.

Heat shock protein 90 (Hsp90) inhibitor affecting the DNA repair.

Inhibitor Derivatives Structure Pharmacokinetics (nM) Clinical Study Stage References
Geldanamycin (naturally derived from Streptomyces hygroscopicus) graphic file with name biomolecules-05-02589-i001.jpg GI50 = 1.0 × 10−1 nM;
LC50 = 2.1 × 104 nM;
Kd = 1.2 × 103 nM
Preclinical [61,65,69]; www.medchemexpress.net
17-AAG (17-allylamino-17-desmethoxygeldanamycin; tanespimycin) graphic file with name biomolecules-05-02589-i002.jpg IC50 = 5.0 × 101–1.0 × 104 nM Phase I/II/III [70,71,72,73,74,75,76,77,78]; www.clinicaltrials.gov; www.medchemexpress.net
17-DMAG (17-dimethylaminoethylamino-17-demetoxygelanamycin; alvespimycin) graphic file with name biomolecules-05-02589-i003.jpg IC50 = 6.0 × 101–3.0 × 103 nM;
Kd = 3.5 × 102 nM
Phase I/II [72,77,79,80,81]; www.clinicaltrials.gov
PU-H71 graphic file with name biomolecules-05-02589-i004.jpg IC50 = 5.0 × 101–3.0 × 102 nM Phase I [82,83,84]; www.clinicaltrials.gov
NVP-AUY922 graphic file with name biomolecules-05-02589-i005.jpg IC50 = 1.3 × 101 nM (Hsp90α);
IC50 = 2.1 × 101 nM (Hsp90β);
GI50 = 2.0–4.0 × 101 nM;
Kd = 1.7 nM
Phase I/II [85,86,87]; www.medchemexpress.net; www.clinicaltrials.gov
Radicicol (naturally derived from Diheterospora chlamydosporia) graphic file with name biomolecules-05-02589-i006.jpg Kd = 1.9 × 101 nM;
IC50 = 2.0 × 101 nM
Preclinical [65]
STA9090 (Ganetespib) graphic file with name biomolecules-05-02589-i007.jpg IC50 = 1.0–5.0 × 101 nM Phase I/II/III [88,89,90,91]; www.clinicaltrials.gov; www.medchemexpress.net