| DC70417 |
Foldamer 33
|
Foldamer 33 is a small molecule HSP110 inhibitor, directly binds to the nucleotide-binding domain (NBD) of HSP110, blocks HSP110 chaperone function and colorectal cancer growth.Foldamer 33 significantly inhibit HSP110 anti-aggregating activity with IC50 of 87.8 uM.Foldamer 33 disrupts HSP110-STAT3 interaction with IC50 of 35.9 uM in competitive BLI assays.Foldamer 33 inhibits SW480 colorectal cancer cell proliferation, and (5 mg/kg) Foldamer 33 displays an anti-tumor effect (TGI of 40% and 60%) in mice bearing a colorectal cancer. |
| DC47938 |
NCT-58
|
NCT58(NCT 58) is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells. |
| DC46184 |
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. |
| DC44513 |
DTHIB
|
DTHIB is a direct and selective heat shock factor 1 (HSF1) inhibitor with a Kd of 160 nM for DTHIB binding to the HSF1 DNA binding domain (DBD). DTHIB inhibits HSF1 cancer gene signature (HSF1 CaSig) and selectively stimulates degradation of nuclear HSF1. DTHIB has potently anticancer activities and can be used for prostate cancer research. |
| DC44512 |
Conglobatin
|
Conglobatin (FW-04-806), a macrolide dilactone, is isolated from the culture of Streptomyces conglobatus. Conglobatin is an orally active Hsp90 inhibitor. Conglobatin can bind to the N-terminal domain of Hsp90 and disrupt Hsp90-Cdc37 complex formation. Conglobatin induces apoptosis in human breast cancer cells and esophageal squamous cell carcinoma cells, and exhibits antitumor activity in vivo. |
| DC40344 |
3-Phenyltoxoflavin
|
3-Phenyltoxoflavin, a derivative of Toxoflavin, is an Hsp90 inhibitor, with a Kd of 585 nM for the interaction of Hsp90-TPR2A. 3-Phenyltoxoflavin has anti-cancer activity. |
| DC5133 |
SNX-2112 (PF-04928473)
|
SNX-2112 selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG. |
| DC7449 |
KW-2478
|
KW-2478 is a nonansamycin HSP90 inhibitor with IC50 of 3.8 nM. Phase 1/2 |
| DC10344 |
HSP70-IN-1
|
HSP70-IN-1 is a heat shock protein (HSP) inhibitor; inhibits the growth of Kasumi-1 cells with an IC50 of 2.3 μM. |
| DC7806 |
Geldanamycin (NSC122750)
|
Geldanamycin is a natural existing HSP90 inhibitor with Kd of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. |
