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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
HDAC 194 nM (IC50) |
HSP90α 153 nM (IC50) |
HSP70 |
Cellular Effect
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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.
Protocols
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RNA extraction experimental
By lysing cells, releasing RNA, and removing impurities such as proteins and DNA, high-purity RNA products are finally obtained. The commonly used traditional method is the guanidine isothiocyanate/phenol/chloroform method (Trizol), which is suitable for a variety of animal materials including animal tissues, microorganisms, cultured cells, etc., and most plant materials.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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