Powder: -20°C for 3 years | In solvent: -80°C for 1 year
HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor targeting HDAC6 and Hsp90, exhibiting IC50 values of 105.7 nM and 61 nM, respectively. It is primarily utilized in cancer research [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 1,520.00 | |
50 mg | 10-14 weeks | $ 1,980.00 | |
100 mg | 10-14 weeks | $ 2,500.00 |
Description | HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor targeting HDAC6 and Hsp90, exhibiting IC50 values of 105.7 nM and 61 nM, respectively. It is primarily utilized in cancer research [1]. |
In vitro | HDAC6/HSP90-IN-2 (compound 6e), at concentrations ranging from 0.05 to 2 μM over a 24-hour period, dose-dependently affects HSP90, HDAC6, and Hsp90-regulated signaling pathways. At a concentration of 2 μM for 24 hours, it promotes HSP90 acetylation. Additionally, this compound inhibits the growth of H1975 non-small cell lung cancer cells in a concentration range of 0-100 μM over periods of 24 to 72 hours, and induces apoptosis in these cells at 0-2 μM over 24 hours. Western blot analyses reveal that HDAC6/HSP90-IN-2 inhibits Hsp90 and HDACs in a dose-dependent manner, increases Hsp70 and Hsp90 expression likely through HSF1 activation at concentrations of 0.05, 0.1, 0.5, 1, and 2 μM over 24 hours, and enhances acetylation at the K294 residue of Hsp90 at 2 μM. Apoptosis analysis shows dose-dependent induction of early and late apoptosis in H1975 cells at concentrations of 0, 0.5, 1, and 2 μM over 24 hours. A cell viability assay demonstrates the compound's ability to inhibit cell growth with a GI50 value of 1.7 μM. |
In vivo | HDAC6/HSP90-IN-2 (compound 6e), administered at a dosage of 25-50 mg/kg via intraperitoneal injection on weekdays for six weeks, demonstrated significant antitumor activity in NOD-scid IL2Rgammanull (NSG) mice xenografted with H1975 cells. The treatment not only delayed tumor growth after two weeks but also effectively reduced tumor growth rates in the mice [1]. |
Molecular Weight | 358.39 |
Formula | C19H22N2O5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
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HDAC6/HSP90-IN-2 inhibitor inhibit