HDAC6/HSP90-IN-2
HDAC6/HSP90-IN-2 (compound 6e) is a dual inhibitor of HDAC6 and Hsp90, with IC50s of 105.7 and 61 nM, respectively. HDAC6/HSP90-IN-2 can be used for the research of cancer.
For research use only. We do not sell to patients.
- CAS No.: 2803866-22-8
- Formula: C19H22N2O5
- Molecular Weight:358.39
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
HDAC6 106 nM (IC50) |
HDAC1 654.5 nM (IC50) |
HDAC3 1539 nM (IC50) |
HDAC7 1691 nM (IC50) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | GI50 |
1.7 μM
Compound: 6e
|
Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition incubated upto 72 hrs by CellTiter96 Aqueous One Solution Cell Proliferation assay
Antiproliferative activity against human NCI-H1975 cells assessed as growth inhibition incubated upto 72 hrs by CellTiter96 Aqueous One Solution Cell Proliferation assay
|
[PMID: 35834905] |
HDAC6/HSP90-IN-2 (compound 6e) (0.05-2 μM; 24 h) effects HSP90, HDAC6 and signaling pathways regulated by Hsp90 dose-dependently[1]. HDAC6/HSP90-IN-2 (compound 6e) (2 μM; 24 h) promotes the acetylation of HSP90[1]. HDAC6/HSP90-IN-2 (compound 6e) (0-100 μM; 24-72 h) inhibits the growth of H1975 non-small cell lung cancer cells[1]. HDAC6/HSP90-IN-2 (compound 6e) (0-2 μM; 24 h) induces apoptosis of H1975 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:H1975 cells
-
Concentration:0.05, 0.1, 0.5, 1 and 2 μM
-
Incubation Time:24 hours
-
Result:Showed inhibitory effect to Hsp90 and HDACs dose-dependently and increased the expression levels of Hsp70 and Hsp90 probably by activates HSF1.
-
Cell Line:H1975 cells
-
Concentration:2 μM
-
Incubation Time:24 hours
-
Result:Promoted the acetylation of Hsp90 by inhibiting HDAC6, and increased the acetylation at K294 residue of Hsp90.
-
Cell Line:H1975 cells
-
Concentration:0, 0.5, 1 and 2 μM
-
Incubation Time:24 hours
-
Result:Induced early and late apoptosis of H1975 cells dose-dependently.
-
Cell Line:H1975 cells
-
Concentration:0-100 μM
-
Incubation Time:24, 48 and 72 h
-
Result:Inhibited the growth of H1975 non-small cell lung cancer cells with a GI50 value of 1.7 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:NOD-scid IL2Rgammanull (NSG) mouse with H1975 cells xenograft[1]
-
Dosage:25-50 mg/kg
-
Administration:Intraperitoneal injection; 25-50 mg/kg for every weekdays; for 6 weeks
-
Result:Delayed tumor growth after 2 weeks and reduced the growth rates of tumors in mice.
Chemical Information
-
CAS No. 2803866-22-8
-
Molecular Weight 358.39
-
Formula C19H22N2O5
-
SMILES
OC1=C(C(C)C)C=C(C(N(C)CC2=CC=C(C=C2)C(NO)=O)=O)C(O)=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)