2. Cell Cycle/DNA Damage Epigenetics Apoptosis
  3. HDAC Apoptosis Caspase
  4. 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.

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HDAC-IN-100

HDAC-IN-100 Chemical Structure

CAS No. : 2390474-88-9

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HDAC-IN-100 Related Antibodies

Top Publications Citing Use of Products

View All HDAC Isoform Specific Products:

View All Isoforms
HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

View All Caspase Isoform Specific Products:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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Description

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[1].

IC50 & Target[1]

HDAC1

0.038 μM (IC50)

HDAC2

0.283 μM (IC50)

HDAC3

0.586 μM (IC50)

Caspase-3

 

Caspase-7

 

Cellular Effect
Cell Line Type Value Description References
A2780 IC50
0.48 μM
Compound: 2a
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
[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.

HDAC-IN-100 Related Antibodies

Cell Viability Assay[1]

Cell Line: Human tongue squamous cell carcinoma Cal27 cells, cisplatin-resistant Cal27CisR cells
Concentration: 0.5 μM
Incubation Time: 48 h (pretreatment); 72 h (Cisplatin incubation)
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.
Molecular Weight

535.64

Formula

C32H33N5O3
CAS No.
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Purity & Documentation
References
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HDAC-IN-100 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HDAC-IN-1002390474-88-9HDACApoptosisCaspaseHistone deacetylasesHDAC2Cal27CisRovarian cancerA2780caspase 3/7HDAC3histone H3Cal27squamous carcinomaHDAC1Inhibitorinhibitorinhibit

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