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.
All Caspase Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
HDAC1 0.038 μM (IC50) |
HDAC2 0.283 μM (IC50) |
HDAC3 0.586 μM (IC50) |
Caspase-3 |
Caspase-7 |
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
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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.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)