TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity. 了解更多
SNX-5422 Mesylate (PF-04929113 Mesylate), a prodrug of SNX-2112, is an orally active Hsp90 inhibitor, with a Kd of 41 nM, and also induces Her-2 degradation, with an IC50 of 37?nM. 了解更多
Apoptozole (Apoptosis Activator VII) is an inhibitor of the ATPase domain of Hsc70 and Hsp70, with Kds of 0.21 and 0.14?μM, respectively, and can induce apoptosis. 了解更多
YZ129 is an inhibitor of the HSP90-calcineurin-NFAT pathway against glioblastoma, directly binding to heat shock protein 90 (HSP90) with an IC50 of 820 nM on NFAT nuclear translocation. 了解更多
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. 了解更多
Haruka Wakasa, .et al. Adverse Effects of High Temperature On Mammary Alveolar Development In Vitro, J Mammary Gland Biol Neoplasia, 2022, Jun;27(2):155-170 PMID: 35581442
Col003 is a potent inhibitor of Hsp47, competitively binds to the collagen binding site on Hsp47 (IC50, 1.8 μM), and inhibits collagen secretion by destabilizing the collagen triple helix. 了解更多
JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages. 了解更多
Michael Heider, .et al. The IMiD target CRBN determines HSP90 activity toward transmembrane proteins essential in multiple myeloma, Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
Kale S, .et al. HSP90 inhibitor PU-H71 increases radiosensitivity of breast cancer cells metastasized to visceral organs and alters the levels of inflammatory mediators, Naunyn Schmiedebergs Arch Pharmacol, 2019, Sep 14 PMID: 31522240
Hiroki Murano, .et al. A purine-type heat shock protein 90 inhibitor promotes the heat shock response in Arabidopsis, Plant Biotechnol Rep, 2017, 11:107-113
Yool Lee, .et al. Time-of-day specificity of anticancer drugs may be mediated by circadian regulation of the cell cycle, Sci Adv, 2021, 7
Naoki Shiraishi, .et al. Heat shock protein 90 as a molecular target for therapy in oral squamous cell carcinoma: Inhibitory effects of 17?DMAG and ganetespib on tumor cells, Oncol Rep, 2020, 448-458 PMID: 33416122
Tung-Yun Wu, .et al. Rational design of synthetically tractable HDAC6/HSP90 dual inhibitors to destroy immune-suppressive tumor microenvironment, J Adv Res, 2022, Jun 22;S2090-1232(22)00148-5 PMID: 35752438
Aykut Ozgur, .et al. Investigation of anticancer activities of STA-9090 (ganetespib) as a second generation HSP90 inhibitor in Saos-2 osteosarcoma cells, J Chemother, 2021, Apr 2;1-10 PMID: 33794753
Michael Heider, .et al. The IMiD target CRBN determines HSP90 activity toward transmembrane proteins essential in multiple myeloma, Mol Cell, 2021, Mar 18;81(6):1170-1186 PMID: 33571422
Kosinsky RL, .et al. USP22-dependent HSP90AB1 expression promotes resistance to HSP90 inhibition in mammary and colorectal cancer, Cell Death Dis, 2019, Dec 4;10(12):911 PMID: 31801945
Yamada-Kanazawa S, .et al. Inhibition of heat shock protein 90 exerts an antitumour effect in angiosarcoma: involvement of the vascular endothelial growth factor signalling pathway, Br J Dermatol, 2017, Aug;177(2):456-469 PMID: 28078663
Hiroki Murano, .et al. A purine-type heat shock protein 90 inhibitor promotes the heat shock response in Arabidopsis, Plant Biotechnol Rep, 2017, 11:107-113
Haruka Wakasa, .et al. Adverse Effects of High Temperature On Mammary Alveolar Development In Vitro, J Mammary Gland Biol Neoplasia, 2022, Jun;27(2):155-170 PMID: 35581442
Hiroki Murano, .et al. A purine-type heat shock protein 90 inhibitor promotes the heat shock response in Arabidopsis, Plant Biotechnol Rep, 2017, 11:107-113
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