E0249New |
Pseudolaric Acid A
|
Pseudolaric acid A, a Hsp90 inhibitor with an IC50 of 0.60 μM, 2.72 μM, 1.36 μM, 2.92 μM and 6.16 μM in HL-60, A549, SMMC-7721, HeLa and SW480 cells respectively, is the main bioactive ingredient in Pseudolarix cortex, and induces cell cycle arrest at G2/M phase and promotes cell death through caspase-8/caspase-3 pathway, demonstrating potent antiproliferation and anticancer activities. |
|
|
S1069 |
Luminespib (NVP-AUY922)
|
Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2. |
-
Biomedicines, 2022, 10(3)624
-
Cell Death Discov, 2022, 8(1):86
-
Cell Rep, 2021, 34(11):108870
|
|
S1141 |
Tanespimycin (17-AAG)
|
Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3. |
-
Blood Cancer J, 2022, 12(3):39
-
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
-
J Cell Mol Med, 2022, 10.1111/jcmm.17210
|
|
S1142 |
Alvespimycin (17-DMAG) HCl
|
Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2. |
-
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
-
Biomedicines, 2022, 10(3)624
-
SLAS Discov, 2022, 27(3):175-184
|
|
S1159 |
Ganetespib (STA-9090)
|
Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3. |
-
Biomedicines, 2022, 10(3)624
-
Nat Commun, 2021, 12(1):5919
-
Cell Death Dis, 2021, 12(1):126
|
|
S1163 |
Onalespib (AT13387)
|
Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2. |
-
SLAS Discov, 2022, 27(3):175-184
-
Cell Chem Biol, 2021, S2451-9456(21)00221-X
-
Transl Res, 2021, 235:1-14
|
|
S1175 |
BIIB021
|
BIIB021 (CNF2024) is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2. |
-
SLAS Discov, 2022, 27(3):175-184
-
Front Oncol, 2021, 11:620907
-
SLAS Technol, 2019, 24(1):28-40
|
|
S1498 |
NVP-BEP800
|
NVP-BEP800 (VER82576) is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1. |
-
Blood Cancer J, 2021, 11(3):61
-
Cell Death Dis, 2021, 12(1):114
-
Cell Death Dis, 2021, 12(1):114
|
|
S2639 |
SNX-2112 (PF-04928473)
|
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. |
-
SLAS Discov, 2022, 27(3):175-184
-
Cell Chem Biol, 2021, S2451-9456(21)00221-X
-
PLoS Negl Trop Dis, 2020, 17;14(4):e0008224
|
|
S2656 |
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. |
-
ACS Chem Neurosci, 2019, 10(6):2890-2902
-
Endocrine, 2016, 51(2):274-82
-
Antimicrob Agents Chemother, 2014, 58(7):4138-44
|
|
S2685 |
KW-2478
|
KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1. |
-
Clin Exp Med, 2019, 10.1007/s10238-019-00587-2
|
|
S2713 |
Geldanamycin (NSC 122750)
|
Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses. |
-
ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
-
Anal Chem, 2022, 10.1021/acs.analchem.1c05455
-
Cell Chem Biol, 2021, S2451-9456(21)00221-X
|
|
S2930 |
Pifithrin-μ
|
Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy. |
-
Chin Med J (Engl), 2022, 135(5):606-618
-
Shock, 2021, 55(1):74-82
-
Radiat Res, 2020, 193(2):119-129
|
|
S3604 |
Triptolide (PG490)
|
Triptolide (PG490, NSC 163062) is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway. |
-
Ann N Y Acad Sci, 2022, 10.1111/nyas.14760
-
Sci Adv, 2021, 7(7)eabd2645
-
EMBO Rep, 2021, e52023
|
|
S5369 |
Ethoxyquin
|
Ethoxyquin (Santoquin, Santoflex, Quinol) is an antioxidant used as a food preservative. Ethoxyquin is an antioxidant which has been used in animal feed for many years and also an inhibitor of heat shock protein 90 (Hsp90). |
|
|
S6193 |
YUM70
|
YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. |
|
|
S6721 |
JG98
|
JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. JG-98 induces classical apoptosis features, including morphological changes consistent with programmed cell death and positive annexin staining. JG-98 exhibits anticancer activity. |
|
|
S7097 |
HSP990 (NVP-HSP990)
|
HSP990 (NVP-HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. NVP-HSP990 induces cell cycle arrest and apoptosis. |
-
Mol Cancer Res, 2020, 18(7):1004-1017
-
Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669
-
Theranostics, 2020, 10(18):8415-8429
|
|
S7122 |
XL888
|
XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1. |
-
SLAS Discov, 2022, 27(3):175-184
-
Cell Chem Biol, 2016, 23(6):716-26
-
Oncotarget, 2016, 7(31):49597-49610
|
|
S7282 |
NMS-E973
|
NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases. |
-
SLAS Discov, 2022, 27(3):175-184
-
J Exp Clin Cancer Res, 2021, 40(1):170
-
Immunity, 2020, 52(2):328-341
|
|
S7340 |
CH5138303
|
CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
|
|
|
S7428 |
Rocaglamide
|
Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity. |
|
|
S7458 |
VER-49009
|
VER-49009 (CCT0129397) is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β. |
-
SLAS Discov, 2022, 27(3):175-184
-
Cell Chem Biol, 2021, S2451-9456(21)00221-X
|
|
S7459 |
VER-50589
|
VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
|
-
Cell Chem Biol, 2021, S2451-9456(21)00221-X
-
PLoS Negl Trop Dis, 2014, 8(2):e2699
|
|
S7716 |
Pimitespib (TAS-116)
|
Pimitespib (TAS-116) is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L). |
|
|
S7750 |
KNK437
|
KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
|
-
Biosci Rep, 2020, 40(3)
-
Br J Haematol, 2013, 161(5):667-76
-
Oncol Rep, 2012, 28(6):1953-8
|
|
S7751 |
VER155008
|
VER155008 (C07) is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins. |
-
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
-
EMBO J, 2021, e106183
-
Oncogene, 2021, 10.1038/s41388-021-01914-2
|
|
S8039 |
Zelavespib (PU-H71)
|
Zelavespib (PU-H71, NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1. |
-
Nat Cancer, 2021, 2(6):598-610
-
Cancers (Basel), 2020, 7;12(4)
-
Mol Cell Biol, 2020,
|
|
S8365 |
Apoptozole
|
Apoptozole (Apoptosis Activator VII) is an inhibitor of heat shock protein 70(HSP70) and Hsc70 with dissociation constants Kd of 0.14 μM and 0.21 μM, respectively. It induces caspase-dependent apoptosis. |
-
Nat Commun, 2018, 9(1):4700
-
Platelets, 2018, 29(6):610-621
|
|
S8402 |
KRIBB11
|
KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1). KRIBB11 induces growth arrest and apoptosis. |
-
Cell Metab, 2021, S1550-4131(21)00183-2
-
Br J Pharmacol, 2021, 178(5):1182-1199
-
Cancers (Basel), 2021, 13(12)2987
|
|
S9806 |
DTHIB
|
DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities. |
|
|
A5110 |
Hsc70 Rabbit Recombinant mAb
|
Hsc70 Rabbit Recombinant mAb detects endogenous levels of total Hsc70. |
|
|
A5260 |
Phospho-HSF1(S326) Rabbit Recombinant mAb
|
Phospho-HSF1(S326) Rabbit Recombinant mAb detects endogenous level of total phospho-HSF1(S326). |
|
|
E0362New |
BiP Inducer X (BIX)
|
BiP Inducer X (BIX) is a selective GRP78 (BiP, HSPA5) inducer. BIX induces BiP only, in a dose-dependent manner, without induction of other molecules involved in the ER stress response.
|
|
|
S0279 |
Dimethylenastron
|
Dimethylenastron is a potent, specific and reversible inhibitor of kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) with IC50 of 200 nM. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells. |
|
|
S0294 |
HSF1A
|
HSF1A is a cell-permeable heat shock transcription factor 1 (HSF1) activator. HSF1A protects cells from stress-induced apoptosis, binds TRiC subunits and inhibits TRiC activity without perturbation of ATP hydrolysis. |
|
|
S1238 |
Tamoxifen (ICI 46474)
|
Tamoxifen (ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen) is a selective estrogen receptor modulator (SERM). Tamoxifen enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis. |
-
Blood Cancer J, 2022, 12(3):36
-
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
-
Cancers (Basel), 2021, 13(9)2116
|
|
S1972 |
Tamoxifen (ICI 46474) Citrate
|
Tamoxifen Citrate (ICI 46474) is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy. |
-
Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905
-
Cancers (Basel), 2021, 13(9)2116
-
Cell Death Dis, 2021, 12(6):619
|
|
S6568 |
ML346
|
ML346 is a Hsp70 activator and a novel modulator of proteostasis for protein conformational diseases. |
|
|
S1052 |
Elesclomol (STA-4783)
|
Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3. |
-
J Exp Clin Cancer Res, 2021, 40(1):228
-
Mol Oncol, 2021, 10.1002/1878-0261.13079
-
Nat Commun, 2020, 15;11(1):2423
|
|
S8299 |
HA15
|
HA15 is a molecule that targets specifically HSPA5 (Heat shock 70kDa protein 5) also known as BiP (Immunoglobulin heavy-chain-binding protein) or Grp78 (glucose-regulated protein 78). HA15 displays anti-cancerous activity on all melanoma cells tested, including cells isolated from patients and cells that developed resistance to BRAF inhibitors. |
-
Front Oncol, 2022, 12:842418
-
Bone, 2022, 154:116262
-
Biomedicines, 2021, 9(2)E96
|
|
S8305 |
TRC051384
|
TRC051384 is an inducer of heat shock protein 70 (HSP70) and potent anti-inflammatory agent. |
-
Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
-
Mol Cell Biochem, 2021, 10.1007/s11010-021-04052-1
|
|
S5006 |
Teprenone
|
Teprenone, an acylic polyisoprenoid, that is known as tetraprenylacetone or geranylgeranylacetone, is an anti-ulcer drug, clinically used for gastritis. Teprenone(Geranylgeranylacetone) is an inducer of heat shock proteins (HSPs) expression. |
-
Front Endocrinol (Lausanne), 2021, 12:743202
|
|
E0249New |
Pseudolaric Acid A
|
Pseudolaric acid A, a Hsp90 inhibitor with an IC50 of 0.60 μM, 2.72 μM, 1.36 μM, 2.92 μM and 6.16 μM in HL-60, A549, SMMC-7721, HeLa and SW480 cells respectively, is the main bioactive ingredient in Pseudolarix cortex, and induces cell cycle arrest at G2/M phase and promotes cell death through caspase-8/caspase-3 pathway, demonstrating potent antiproliferation and anticancer activities. |
|
|
S1069 |
Luminespib (NVP-AUY922)
|
Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2. |
- Biomedicines, 2022, 10(3)624
- Cell Death Discov, 2022, 8(1):86
- Cell Rep, 2021, 34(11):108870
|
|
S1141 |
Tanespimycin (17-AAG)
|
Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3. |
- Blood Cancer J, 2022, 12(3):39
- ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
- J Cell Mol Med, 2022, 10.1111/jcmm.17210
|
|
S1142 |
Alvespimycin (17-DMAG) HCl
|
Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2. |
- ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
- Biomedicines, 2022, 10(3)624
- SLAS Discov, 2022, 27(3):175-184
|
|
S1159 |
Ganetespib (STA-9090)
|
Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3. |
- Biomedicines, 2022, 10(3)624
- Nat Commun, 2021, 12(1):5919
- Cell Death Dis, 2021, 12(1):126
|
|
S1163 |
Onalespib (AT13387)
|
Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2. |
- SLAS Discov, 2022, 27(3):175-184
- Cell Chem Biol, 2021, S2451-9456(21)00221-X
- Transl Res, 2021, 235:1-14
|
|
S1175 |
BIIB021
|
BIIB021 (CNF2024) is an orally available, fully synthetic small-molecule inhibitor of HSP90 with Ki and EC50 of 1.7 nM and 38 nM, respectively. Phase 2. |
- SLAS Discov, 2022, 27(3):175-184
- Front Oncol, 2021, 11:620907
- SLAS Technol, 2019, 24(1):28-40
|
|
S1498 |
NVP-BEP800
|
NVP-BEP800 (VER82576) is a novel, fully synthetic HSP90β inhibitor with IC50 of 58 nM, exhibits>70-fold selectivity against Hsp90 family members Grp94 and Trap-1. |
- Blood Cancer J, 2021, 11(3):61
- Cell Death Dis, 2021, 12(1):114
- Cell Death Dis, 2021, 12(1):114
|
|
S2639 |
SNX-2112 (PF-04928473)
|
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. |
- SLAS Discov, 2022, 27(3):175-184
- Cell Chem Biol, 2021, S2451-9456(21)00221-X
- PLoS Negl Trop Dis, 2020, 17;14(4):e0008224
|
|
S2656 |
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. |
- ACS Chem Neurosci, 2019, 10(6):2890-2902
- Endocrine, 2016, 51(2):274-82
- Antimicrob Agents Chemother, 2014, 58(7):4138-44
|
|
S2685 |
KW-2478
|
KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1. |
- Clin Exp Med, 2019, 10.1007/s10238-019-00587-2
|
|
S2713 |
Geldanamycin (NSC 122750)
|
Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses. |
- ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138
- Anal Chem, 2022, 10.1021/acs.analchem.1c05455
- Cell Chem Biol, 2021, S2451-9456(21)00221-X
|
|
S2930 |
Pifithrin-μ
|
Pifithrin-μ (NSC 303580, PFTμ, 2-Phenylethynesulfonamide) is a specific p53 inhibitor by reducing its affinity to Bcl-xL and Bcl-2, and also inhibits HSP70 function and autophagy. |
- Chin Med J (Engl), 2022, 135(5):606-618
- Shock, 2021, 55(1):74-82
- Radiat Res, 2020, 193(2):119-129
|
|
S3604 |
Triptolide (PG490)
|
Triptolide (PG490, NSC 163062) is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii. It functions as a NF-κB inhibitor with dual actions by disruption of p65/CBP interaction and by reduction of p65 protein. Triptolide (PG490) abrogates the transactivation function of heat shock transcription factor 1 (HSF1). Triptolide inhibits MDM2 and induces apoptosis through a p53-independent pathway. |
- Ann N Y Acad Sci, 2022, 10.1111/nyas.14760
- Sci Adv, 2021, 7(7)eabd2645
- EMBO Rep, 2021, e52023
|
|
S5369 |
Ethoxyquin
|
Ethoxyquin (Santoquin, Santoflex, Quinol) is an antioxidant used as a food preservative. Ethoxyquin is an antioxidant which has been used in animal feed for many years and also an inhibitor of heat shock protein 90 (Hsp90). |
|
|
S6193 |
YUM70
|
YUM70 is a potent inhibitor of glucose-regulated protein 78 (GRP78) inhibitor with an IC50 of 1.5 μM. YUM70 induces endoplasmic reticulum (ER) stress-mediated apoptosis in pancreatic cancer. |
|
|
S6721 |
JG98
|
JG-98 is an allosteric inhibitor of Hsp70 that binds tightly to a deep pocket that is conserved in members of the Hsp70 family. JG-98 induces classical apoptosis features, including morphological changes consistent with programmed cell death and positive annexin staining. JG-98 exhibits anticancer activity. |
|
|
S7097 |
HSP990 (NVP-HSP990)
|
HSP990 (NVP-HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. NVP-HSP990 induces cell cycle arrest and apoptosis. |
- Mol Cancer Res, 2020, 18(7):1004-1017
- Mol Cancer Res, 2020, 10.1158/1541-7786.MCR-19-0669
- Theranostics, 2020, 10(18):8415-8429
|
|
S7122 |
XL888
|
XL888 is an ATP-competitive inhibitor of HSP90 with IC50 of 24 nM. Phase 1. |
- SLAS Discov, 2022, 27(3):175-184
- Cell Chem Biol, 2016, 23(6):716-26
- Oncotarget, 2016, 7(31):49597-49610
|
|
S7282 |
NMS-E973
|
NMS-E973 is a potent and selective Hsp90 inhibitor with DC50 of <10 nM for Hsp90 binding, no activiy against a panel of 52 diverse protein kinases. |
- SLAS Discov, 2022, 27(3):175-184
- J Exp Clin Cancer Res, 2021, 40(1):170
- Immunity, 2020, 52(2):328-341
|
|
S7340 |
CH5138303
|
CH5138303 is an orally available Hsp90 inhibitor with Kd of 0.48 nM.
|
|
|
S7428 |
Rocaglamide
|
Rocaglamide (Roc-A), isolated from Aglaia species, is a potent inhibitor of heat shock factor 1 (HSF1) activation with IC50 of ~50 nM for HSF1. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also inhibits NF-κB activity. Rocaglamide exhibits anti-tumor activity. |
|
|
S7458 |
VER-49009
|
VER-49009 (CCT0129397) is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β. |
- SLAS Discov, 2022, 27(3):175-184
- Cell Chem Biol, 2021, S2451-9456(21)00221-X
|
|
S7459 |
VER-50589
|
VER-50589 is a potent HSP90 inhibitor with IC50 of 21 nM for HSP90β.
|
- Cell Chem Biol, 2021, S2451-9456(21)00221-X
- PLoS Negl Trop Dis, 2014, 8(2):e2699
|
|
S7716 |
Pimitespib (TAS-116)
|
Pimitespib (TAS-116) is a novel, small-molecule HSP90 inhibitor which inhibits geldanamycin-FITC binding to HSP90 proteins with Ki values of 34.7 nmol/L, 21.3 nmol/L, >50,000 nmol/L, and >50,000 nmol/L for HSP90α, HSP90β, GRP94, and TRAP1, respectively. Furthermore, TAS-116 does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L). |
|
|
S7750 |
KNK437
|
KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
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- Biosci Rep, 2020, 40(3)
- Br J Haematol, 2013, 161(5):667-76
- Oncol Rep, 2012, 28(6):1953-8
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S7751 |
VER155008
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VER155008 (C07) is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins. |
- Exp Mol Med, 2022, 10.1038/s12276-022-00745-9
- EMBO J, 2021, e106183
- Oncogene, 2021, 10.1038/s41388-021-01914-2
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S8039 |
Zelavespib (PU-H71)
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Zelavespib (PU-H71, NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1. |
- Nat Cancer, 2021, 2(6):598-610
- Cancers (Basel), 2020, 7;12(4)
- Mol Cell Biol, 2020,
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S8365 |
Apoptozole
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Apoptozole (Apoptosis Activator VII) is an inhibitor of heat shock protein 70(HSP70) and Hsc70 with dissociation constants Kd of 0.14 μM and 0.21 μM, respectively. It induces caspase-dependent apoptosis. |
- Nat Commun, 2018, 9(1):4700
- Platelets, 2018, 29(6):610-621
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S8402 |
KRIBB11
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KRIBB11 abolishes the heat shock-induced luciferase activity with an IC50 of 1.2 μM. It is an inhibitor of the transcription factor Heat Shock Factor 1 (HSF1). KRIBB11 induces growth arrest and apoptosis. |
- Cell Metab, 2021, S1550-4131(21)00183-2
- Br J Pharmacol, 2021, 178(5):1182-1199
- Cancers (Basel), 2021, 13(12)2987
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S9806 |
DTHIB
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DTHIB (Direct Targeted HSF1 InhiBitor) is a direct and selective inhibitor of heat shock factor 1 (HSF1) with Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB exhibits potently anticancer activities. |
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