HDAC/HSP90-IN-1
HDAC/HSP90-IN-1 (compound 20) is a potent dual inhibitor of HDAC (IC50 = 194 nM) and HSP90 (HSP90α IC50 = 153 nM). HDAC/HSP90-IN-1 induces HSP70 expression, downregulates HSP90 client proteins, and promotes acetylation of α-tubulin and histone H3 in cancer cells. HDAC/HSP90-IN-1 reduces PD-L1 expression in IFN-γ treated H1975 cells. HDAC/HSP90-IN-1 can be used for cancer research, such as lung and colon cancer.
For research use only. We do not sell to patients.
- CAS No.: 2244714-37-0
- Formula: C25H33N3O6
- Molecular Weight:471.55
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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HDAC 194 nM (IC50) |
HSP90α 153 nM (IC50) |
HSP70 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | GI50 |
0.77 μM
Compound: 20
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Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human A549 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay
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[PMID: 31655430] |
| HCT-116 | GI50 |
0.83 μM
Compound: 20
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Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human HCT116 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay
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[PMID: 31655430] |
| HeLa | IC50 |
194.55 μM
Compound: 20
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Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay
Inhibition of HDAC in human HeLa nuclear extract using Boc-Lys(acetyl)-AMC as substrate measured after 30 mins by fluorescence assay
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[PMID: 31655430] |
| NCI-H1975 | GI50 |
0.69 μM
Compound: 20
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Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay
Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition after 48 hrs by sulforhodamine B assay
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[PMID: 31655430] |
| Sf21 | IC50 |
1.19 μM
Compound: 20
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Inhibition of recombinant human GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected sf21 cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorimetry assay
Inhibition of recombinant human GST-tagged HDAC2 (1 to 488 residues) expressed in baculovirus infected sf21 cells using RHK-K(Ac)-AMC as substrate after 60 mins by fluorimetry assay
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[PMID: 31655430] |
Chemical Information
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CAS No. 2244714-37-0
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Molecular Weight 471.55
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Formula C25H33N3O6
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SMILES
O=C(NC1=CC=C(N(C(C2=CC(C(C)C)=C(O)C=C2O)=O)C)C=C1)CCCCCCC(NO)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Mehndiratta S, et al. N-alkyl-hydroxybenzoyl anilide hydroxamates as dual inhibitors of HDAC and HSP90, downregulating IFN-γ induced PD-L1 expression. Eur J Med Chem. 2020 Jan 1;185:111725. doi: 10.1016/j.ejmech.2019.111725. Epub 2019 Sep 24. Erratum in: Eur J Med Chem. 2020 Aug 1;199:112406. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC/HSP90-IN-1 Related Classifications
HY-130273 Related Classifications
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