BCC2125
Geldanamycin
Selective Hsp90 inhibitor; breast cancer stem cell inhibitor,Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association.
BCC1346
Alvespimycin
Alvespimycin (17-DMAG) is a potent inhibitor of Hsp90, binding to Hsp90 with an EC50 of 62 ± 29 nM.
BCC2337
Elesclomol (STA-4783)
Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis.
BCC2123
AUY922 (NVP-AUY922)
Luminespib (NVP-AUY922) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
BCC2121
17-AAG (KOS953)
Tanespimycin (17-AAG) is a potent HSP90 inhibitor with an IC50 of 5 nM, having a 100-fold higher binding affinity for tumour cell derived HSP90 than normal cell derived HSP90. Tanespimycin (17-AAG) depletes cellular STK38/NDR1 and reduces STK38 kinase activity. Tanespimycin (17-AAG) also downregulates the stk38 gene expression.
BCC2127
KW-2478
KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
BCC2129
NVP-BEP800
VER-82576 (NVP-BEP800) is a potent, orally available and selective Hsp90 inhibitor, with an IC50 of 58 nM for Hsp90β; VER-82576 also slightly blocks Grp94 and Trap-1, with IC50s of 4.1 and 5.5 μM, respectively.
BCC2124
BIIB021
BIIB021 is an orally available, fully synthetic inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively.
BCC1889
Retaspimycin
Retaspimycin is a potent and water-soluble inhibitor of Hsp90, with EC50s of 119 nM for both Hsp90 and Grp9.
BCC2126
IPI-504 (Retaspimycin hydrochloride)
Retaspimycin Hydrochloride is a potent and water-soluble inhibitor of Hsp90 with EC50s of 119 nM for both Hsp90 and Grp9.
BCC7968
TRC 051384
TRC051384 is a heat shock protein 70 (HSP70) inducer.
BCC1872
PU-H71
PU-H71 is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
BCC2336
Ganetespib (STA-9090)
Ganetespib is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines.
BCC2132
SNX-2112
SNX-2112 (PF-04928473) selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG.
BCC2130
PF-04929113 (SNX-5422)
PF-04929113 (SNX-5422) is a potent and selective HSP90 inhibitor with Kd of 41 nM and induces Her-2 degradation with IC50 of 37 nM. Phase 1/2.
BCC1297
17-AAG Hydrochloride
17-AAG Hcl is a potent HSP90 inhibitor with IC50 of 5 nM, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells.
BCC2122
AT13387
Onalespib (AT13387) is a long-acting second-generation Hsp90 inhibitor with a Kd of 0.71 nM.
BCC5491
HSP990 (NVP-HSP990)
NVP-HSP990 is a potent and selective Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.
