HDAC-IN-100
HDAC-IN-100 is a histone deacetylase inhibitor with an IC50 of 0.038 μM against HDAC1, 0.283 μM against HDAC2, and 0.586 μM against HDAC3. HDAC-IN-100 acts as a chemosensitizer and apoptosis inducer, activates caspase 3/7, and reverses Cisplatin (HY-17394) resistance. HDAC-IN-100 exerts antiproliferative effects in ovarian cancer cells and squamous cancer cells. HDAC-IN-100 is applicable for research related to ovarian cancer, squamous cell carcinoma, and Cisplatin (HY-17394)-resistant squamous cell carcinoma.
For research use only. We do not sell to patients.
- CAS No.: 2390474-88-9
- Formula: C32H33N5O3
- Molecular Weight:535.64
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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
All Caspase Isoforms
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Biological Activity
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HDAC1 0.038 μM (IC50) |
HDAC2 0.283 μM (IC50) |
HDAC3 0.586 μM (IC50) |
Caspase-3 |
Caspase-7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.48 μM
Compound: 2a
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Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay
Inhibition of HDAC in human A2780 cells using Boc-Lys(epsilon-Ac)-AMC as substrate preincubated for 18 hrs followed by substrate addition and measured after 3 hrs by fluorescence assay
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[PMID: 31762274] |
HDAC-IN-100 (compound 2a) (72 h) reduces the viability of human cancer cells A2780 (IC50 2.40 μM) and Cal27 (IC50 1.60 μM)[1].
HDAC-IN-100 (0-100 μM; 18 h) potently inhibits cellular HDAC activity in human cancer cells A2780 (IC50 0.48 μM) and Cal27 (IC50 0.11 μM)[1].
HDAC-IN-100 (0.5 μM; 48 h) exerts a strong synergistic effect with Cisplatin (HY-17394) to reduce the viability of Cal27 cells and Cisplatin-resistant Cal27CisR cells, and completely reverses the Cisplatin resistance of Cal27CisR cells[1].
HDAC-IN-100 (0.5 μM; 48 h) significantly increases the apoptosis levels in Cal27 cells and cisplatin (HY-17394)-resistant Cal27CisR cells[1].
HDAC-IN-100 (0.5 μM; 24 h) induces hyperacetylation of histone H3 in Cal27 cells and cisplatin (HY-17394)-resistant Cal27CisR cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human tongue squamous cell carcinoma Cal27 cells, cisplatin-resistant Cal27CisR cells
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Concentration:0.5 μM
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Incubation Time:48 h (pretreatment); 72 h (Cisplatin incubation)
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Result:Reduced the cisplatin IC50 from 9.79 μM to 1.26 μM in Cal27 cells.
Reduced the cisplatin IC50 from 63.2 μM to 8.42 μM in Cal27CisR cells,.
Showed synergistic interaction with Cisplatin, with strong synergism observed at multiple concentration combinations.
Chemical Information
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CAS No. 2390474-88-9
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Molecular Weight 535.64
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Formula C32H33N5O3
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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)
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