1. Apoptosis Epigenetics Cell Cycle/DNA Damage
  2. Apoptosis HDAC
  3. HDAC4-IN-1

HDAC4-IN-1 (compound 1a) is a class IIa HDACI inhibitor (IC50=0.077 μM). HDAC4-IN-1 can enhance Caspase-induced Apoptosis. HDAC4-IN-1 has anticancer activity. HDAC4-IN-1 can be used in the research of drug combination against cancer.

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HDAC4-IN-1 Chemical Structure

HDAC4-IN-1 Chemical Structure

CAS No. : 1418293-39-6

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Description

HDAC4-IN-1 (compound 1a) is a class IIa HDACI inhibitor (IC50=0.077 μM). HDAC4-IN-1 can enhance Caspase-induced Apoptosis. HDAC4-IN-1 has anticancer activity. HDAC4-IN-1 can be used in the research of drug combination against cancer[1].

IC50 & Target

HDAC2

6.13 μM (IC50)

HDAC4

0.012 μM (IC50)

HDAC6

5.79 μM (IC50)

HDAC8

4.26 μM (IC50)

In Vitro

HDAC4-IN-1 can significantly inhibits class IIa HDAC (IC50=0.077 μM)[1].
HDAC4-IN-1 (100 μM; 72 h) has very low cytotoxicity in THP-1 cells (IC50=9.2 μM), but has a strong synergistic effect in combination with BTZ and enhances the cytotoxic effect of BTZ on cells [1].
HDAC4-IN-1 (5μM; 48 h) combines with BTZ (7.9 nM) can induce Caspase-mediated apoptosis in THP-1 cells[1].
HDAC4-IN-1 (5μM; 24 h) combines with BTZ (7.9 nM) can enhance the expression of p21 protein in THP-1 cells [1].
HDAC4-IN-1 (5μM; 72 h) inhibits cell proliferation in cancer cell line Cal27_HDAC4 [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: THP-1
Concentration: 100 μM
7.9 nM for BTZ
Incubation Time: 72 h
Result: Revealed relatively low cytotoxicity than pan and class I inhibitors.
Enhanced the cytotoxic effect of BTZ on cells in combination with BTZ.

Apoptosis Analysis[1]

Cell Line: THP-1
Concentration: 5 μM
7.9 nM for BTZ
Incubation Time: 48 h
Result: Significantly enhanced the activation of caspase 3/7 in combination with BTZ.

Western Blot Analysis[1]

Cell Line: THP-1
Concentration: 5 μM
7.9 nM for BTZ
Incubation Time: 24 h
Result: Enhanced the protein expression of p21 in combination with BTZ.
Molecular Weight

356.34

Formula

C16H19F3N4O2

CAS No.
SMILES

O=C(NCCN(CC)CC)C1=CC=C(C2=NOC(C(F)(F)F)=N2)C=C1

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Storage

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

Purity & Documentation
References
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HDAC4-IN-1 Related Classifications

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  • 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.

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HDAC4-IN-1
Cat. No.:
HY-149721
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