HDAC-IN-54
HDAC-IN-54 is a HDAC inhibitor with an IC50 of 25 nM against human HDAC1, 66 nM against HDAC2, 6.5 nM against HDAC3, and 281 nM against HDAC6. HDAC-IN-54 induces acetylation of α-tubulin and histone H3. HDAC-IN-54 acts synergistically with cisplatin to induce cancer cell apoptosis. HDAC-IN-54 can be used in research related to head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma.
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- CAS No.: 2098896-13-8
- Formule: C24H32N4O4
- Masse moléculaire:440.54
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
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hHDAC1 25 nM (IC50) |
HDAC2 66 nM (IC50) |
HDAC3 6.5 nM (IC50) |
HDAC6 281 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| A2780 | IC50 |
0.47 μM
Compound: 4j
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Cytotoxicity against human A2780 cells assessed as cell survival after 72 hrs by MTT assay
Cytotoxicity against human A2780 cells assessed as cell survival after 72 hrs by MTT assay
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[PMID: 28574690] |
| A2780cisR | IC50 |
1.62 μM
Compound: 4j
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Cytotoxicity against human A2780cisR cells assessed as cell survival after 72 hrs by MTT assay
Cytotoxicity against human A2780cisR cells assessed as cell survival after 72 hrs by MTT assay
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[PMID: 28574690] |
| CAL-27 | IC50 |
0.44 μM
Compound: 4j
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Cytotoxicity against human CAL27 cells assessed as cell survival after 72 hrs by MTT assay
Cytotoxicity against human CAL27 cells assessed as cell survival after 72 hrs by MTT assay
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[PMID: 28574690] |
In Vitro
HDAC-IN-54 (Compound 4j) (18 h) inhibits cellular HDAC activity in A2780, A2780CisR, Cal27 and Cal27CisR cells, with IC50 values of 0.48, 0.32, 0.27 and 0.35 μM, respectively[1].
HDAC-IN-54 (72 h) reduces the viability of A2780, A2780CisR, Cal27 and Cal27CisR cells, with IC50 values of 0.47, 1.62, 0.44 and 1.13 μM, respectively[1].
HDAC-IN-54 (90 min) potently inhibits recombinant human HDAC1-3 and HDAC6 enzymes, with the strongest inhibitory activity against HDAC3 (IC50 = 6.5 nM), followed by HDAC1 (25.0 nM), HDAC2 (66 nM), HDAC6 (281 nM), and only weak activity against HDAC8 (2750 nM)[1].
HDAC-IN-54 (10 μM; 24 h) induces acetylation of α-tubulin and histone H3 in Cal27 and Cal27CisR cells, confirming that it inhibits both class I HDAC and HDAC6[1].
HDAC-IN-54 (250-500 nM; 48 h preincubation) enhances the sensitivity of Cal27 and Cal27CisR cells to Cisplatin (HY-17394) in a concentration-dependent manner[1].
HDAC-IN-54 (250-500 nM; 48 h preincubation) synergistically enhances Cisplatin-induced apoptosis in Cal27 and 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:Cal27, Cal27CisR
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Concentration:10 μM
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Incubation Time:24 h
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Result:Induced an increase in acetylation of α-tubulin and histone H3 in both cell lines, with effects more pronounced in Cal27 than in Cal27CisR.
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Cell Line:Cal27, Cal27CisR
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Concentration:250 nM, 500 nM
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Incubation Time:48 h (preincubation); 72 h (total incubation)
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Result:Reduced the IC50 of Cisplatin from 3.01 μM to 1.95 μM (shift factor = 1.5) in Cal27, and from 50.4 μM to 16.1 μM (shift factor = 3.1) in Cal27CisR at 250 nM.
Reduced the IC50 of Cisplatin from 3.01 μM to 0.78 μM (shift factor = 3.9) in Cal27, and from 50.4 μM to 7.37 μM (shift factor = 6.8) in Cal27CisR at 500 nM.
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Cell Line:Cal27, Cal27CisR
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Concentration:250 nM, 500 nM
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Incubation Time:48 h (preincubation)
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Result:Induced a significant increase in apoptotic nuclei in Cal27 when combined with Cisplatin at 250 nM and 500 nM.
Induced a significant increase in apoptotic nuclei in Cal27CisR when combined with Cisplatin at 500 nM.
Chemical Information
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CAS No. 2098896-13-8
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Masse moléculaire 440.54
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Formule C24H32N4O4
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SMILES
O=C(NO)CCCCCN(C(=O)C1=CC=C(C=C1)N(C)C)CC(=O)NCC=2C=CC=CC2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HDAC-IN-54 Related Classifications
HY-153514 Related Classifications
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