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MGCD0103 (Mocetinostat) is a novel HDAC inhibitor, highly specific for classes I and IV HDACs. It is well-tolerated and exhibits favorable pharmacokinetic and pharmacodynamic profiles, demonstrating target inhibition and clinical responses. MGCD0103 (Mocetinostat) has been recently shown to exhibit various effects on non-histone targets on cancer cells. The latest preclinical studies have demonstrated that MGCD0103 can induce both cell death and autophagy.
FEBS J. 2024 Sep 09.
MOF-mediated acetylation of CDK9 promotes global transcription by modulating P-TEFb complex formation
MGCD0103 purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | HCT116, HCT15, HT29, DU145, MDA-mb231, A549 cells line |
| Preparation method | Cell Viability Assay Cells in 96-well plates were incubated with compounds at various concentrations for 72 h at 37°C in 5% CO2. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) was added at a final concentration of 0.5 mg/mL and incubated with the cells for 4 h before an equal volume of solubilization buffer [50% N,N-dimethylformamide, 20% SDS (pH 4.7)] was added. After overnight incubation, solubilized dye was quantified by reading at 570 nm using a reference at 630 nm. Absorbance values were converted to cell numbers according to a standard growth curve of the relevant cell line. The concentration which reduced cell numbers to 50% relative to DMSO-treated cells was determined as MTT IC50. |
| Concentrations | 0~100 μ M |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Female CD-1 nude mice |
| Formulation | PBS acidified with 0.1 N HCl or PEG400/0.2 N HCl saline, 40:60 |
| Dosages | daily for at least 2 weeks |
| Administration | p.o. |
| Molecular Weight | 396.44 |
| Formula | C23H20N6O |
| CAS Number | 726169-73-9 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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|---|
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| Givinostat hydrochloride monohydrate
ITF2357 (Givinostat, Gavinostat) is a histone deacetylase inhibitor. The IC50 values for maize HDAC preparations HD2, HD-1B and HD-1A are 10, 7.5 and 16 nM respectively. |
| Niltubacin
Niltubacin, as an inactive derivative of Tubacin, is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6. |
| Tubacin
Tubacin (Tubulin Acetylation Inducer) is a highly potent and selective, reversible cell-permeable inhibitor of HDAC6 with IC50 of 0.004µM. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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