All AbMole products are for research use only, cannot be used for human consumption.
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
 |
Source | Int J Clin Exp Pathol (2015). Figure 3. MGCD0103 |
| Method | i.v. | |
| Cell Lines | liver cells | |
| Concentrations | 20, 40, 80 mg/kg | |
| Incubation Time | 7 days | |
| Results | According to the pathological changes of liver at difference dosage, MGCD0103 is hepatotoxic and its toxity is dosedependent. |
| 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; Sigma) 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 |
| Related HDAC Products |
|---|
| CM-444
CM-444 is an inhibitor for HDAC and DNA methyltransferases (DNMT) with IC50 values of 6 nM-0.6 μM and 1.8-2.3 μM, respectively. CM-444 is an inducer for the differentiation of acute myeloid leukemia cells. CM-444 exhibits anti-leukemic activity and improves the survival rate in mouse models. |
| CM-1758
CM-1758 is a histone deacetylase (HDAC) inhibitor. CM-1758 inhibits tumor growth in vivo. CM-1758 induces acetylation of non-histone proteins in acute myeloid leukemia cells. |
| T-518
T-518 is an orally active, selective, and blood-brain barrier permeable HDAC6 inhibitor with an IC50 value of 36 nM for human HDAC6. |
| SE-7552
SE-7552, a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) derivative, is an orally active, highly selective, non-hydroxamate HDAC6 inhibitor with an IC50 of 33 nM. |
| BRD9757
BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC50 of 30 nM. |
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.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
