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Art. -Nr.: HY-153514

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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. Nr.: 2098896-13-8
Formel: C₂₄H₃₂N₄O₄
Molecular Weight:440.54

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

HDAC-IN-54 Chemical Structure

CAS. Nr.: 2098896-13-8

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

hHDAC1

25 nM (IC₅₀)

HDAC2

66 nM (IC₅₀)

HDAC3

6.5 nM (IC₅₀)

HDAC6

281 nM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.47 μM Compound: 4j	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	[PMID: 28574690]
A2780cisR	IC₅₀	1.62 μM Compound: 4j	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	[PMID: 28574690]
CAL-27	IC₅₀	0.44 μM Compound: 4j	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	[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.

Western Blot Analysis^[1]

Cell Line:

Cal27, Cal27CisR
Concentration:

10 μM
Incubation Time:

24 h
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.

Cell Viability Assay^[1]

Cell Line:

Cal27, Cal27CisR
Concentration:

250 nM, 500 nM
Incubation Time:

48 h (preincubation); 72 h (total incubation)
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.

Apoptosis Analysis^[1]

Cell Line:

Cal27, Cal27CisR
Concentration:

250 nM, 500 nM
Incubation Time:

48 h (preincubation)
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.

Related Protocols :

Chemical Information

CAS. Nr. 2098896-13-8
Molecular Weight 440.54
Formel C₂₄H₃₂N₄O₄
SMILES

O=C(NO)CCCCCN(C(=O)C1=CC=C(C=C1)N(C)C)CC(=O)NCC=2C=CC=CC2
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Krieger V, et al. Design, Multicomponent Synthesis, and Anticancer Activity of a Focused Histone Deacetylase (HDAC) Inhibitor Library with Peptoid-Based Cap Groups. J Med Chem. 2017;60(13):5493-5506. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Reinheit & Dokumentation
Verweise

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HDAC-IN-54

Alle HDAC Isoform-spezifische Produkte anzeigen