1. Cell Cycle/DNA Damage Epigenetics Cytoskeleton Apoptosis
  2. HDAC Microtubule/Tubulin Apoptosis
  3. 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.

For research use only. We do not sell to patients.

HDAC-IN-54

HDAC-IN-54 Chemical Structure

CAS No. : 2098896-13-8

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Description

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[1].

IC50 & Target

hHDAC1

25 nM (IC50)

HDAC2

66 nM (IC50)

HDAC3

6.5 nM (IC50)

HDAC6

281 nM (IC50)

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.
Molecular Weight

440.54

Formula

C24H32N4O4

CAS No.
SMILES

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

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
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HDAC-IN-54
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HY-153514
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