2. Apoptosis Epigenetics Cell Cycle/DNA Damage Cytoskeleton NF-κB Metabolic Enzyme/Protease Immunology/Inflammation
  3. Apoptosis HDAC Microtubule/Tubulin Reactive Oxygen Species
  4. Tubulin/HDAC-IN-4

Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity.

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Tubulin/HDAC-IN-4 Chemical Structure

Tubulin/HDAC-IN-4 Chemical Structure

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Tubulin/HDAC-IN-4 Related Antibodies

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Description

Tubulin/HDAC-IN-4 (compound 9n) is a dual Tubulin and HDAC inhibitor with IC50 values of 0.73, 0.43, 0.62, 2.34 µM for HDAC1, HDAC2, HDAC6, HDAC7, respectively. Tubulin/HDAC-IN-4 inhibits the tubulin polymerization by targeting the colchicine binding site. Tubulin/HDAC-IN-4 induces apoptosis and cell cycle arrest at G2/M phase. Tubulin/HDAC-IN-4 induces a significant elevation of intracellular ROS levels. Tubulin/HDAC-IN-4 shows anti-angiogenesis activity and anticancer activity[1].

IC50 & Target[1]

HDAC1

0.73 μM (IC50)

HDAC2

0.43 μM (IC50)

HDAC6

0.62 μM (IC50)

HDAC7

2.34 μM (IC50)

In Vitro

Tubulin/HDAC-IN-4 (compound 9n) (0-10 µM; 72 h) shows cytotoxicity with IC50s of 0.34, 0.29, 0.016, 0.15, 0.16 µM for MDA-MB-231, A549, PC-3, U251, MCF-7 cells, respectively[1].
Tubulin/HDAC-IN-4 (2.5, 5, 10, 20, 40 nM; 24 h) inhibits the colony formation of PC-3 cells in a dose-dependent manner[1].
Tubulin/HDAC-IN-4 (0.2, 1, 5, 25 µM) inhibits tubulin polymerization with an IC50 value of 4.82 µM[1].
Tubulin/HDAC-IN-4 (0.08, 0.16, 0.32; 24 h) increases the expression of Ac-α-tubulin and Ac-Histone H3 in PC-3 cells[1].
Tubulin/HDAC-IN-4 (0.08, 0.16, 0.32 µM; 24 h) induces apoptosis and cell cycle arrest at G2/M phase[1].
Tubulin/HDAC-IN-4 (0.08, 0.16, 0.32 µM; 24 h) induces a significant elevation of intracellular ROS levels[1].

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

Tubulin/HDAC-IN-4 Related Antibodies

Cell Cytotoxicity Assay[1]

Cell Line: MDA-MB-231, A549, PC-3, U251, MCF-7 cells
Concentration: 0-10 µM
Incubation Time: 72 h
Result: Showed cytotoxicity with IC50s of 0.34, 0.29, 0.016, 0.15, 0.16 µM for MDA-MB-231, A549, PC-3, U251, MCF-7 cells, respectively.

Western Blot Analysis[1]

Cell Line: PC-3 cells
Concentration: 0.08, 0.16, 0.32 µM
Incubation Time: 24 h
Result: Increased in both the expression of HDAC6 substrate Ac-α-tubulin and HDAC1/2/3 substrate Ac-Histone H3 in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: PC-3 cells
Concentration: 0.08, 0.16, 0.32 µM
Incubation Time: 24 h
Result: Dose-dependently arrested PC-3 cells at G2/M phase, decreased in expression level of p-Cdc25cSer216, p-Cdc2Thr216 and p-CdcTyr15, increased the expression of Cyclin B1.

Apoptosis Analysis[1]

Cell Line: PC-3 cells
Concentration: 0.08, 0.16, 0.32 µM
Incubation Time: 24 h
Result: Induced apoptosis and increased the expression of cleaved PARP and cleaved Caspase 3, decreased the expression of Bim and Bcl-2.
In Vivo

Tubulin/HDAC-IN-4 (10, 20 mg/kg; i.v.; every two days for 21 days) shows anticancer activity[1].

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

Animal Model: 5-week-old male BALB/c nude mouse (PC-3 cells)[1]
Dosage: 10, 20 mg/kg
Administration: I.v.; every two days for 21 days
Result: Inhibited the growth of tumor with the tumor growth inhibition (TGI) reached 90.07% at 20 mg/kg.
Molecular Weight

438.47

Formula

C24H26N2O6
SMILES

CC1(C)OC2=C(C(/C=C/C3=CC=C(OC)C(NCC(NO)=O)=C3)=O)C=CC(OC)=C2C=C1
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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Tubulin/HDAC-IN-4 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:

Tubulin/HDAC-IN-4ApoptosisHDACMicrotubule/TubulinReactive Oxygen SpeciesHistone deacetylasesapoptosisROS levelsG2/MPC-3 cellsInhibitorinhibitorinhibit

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