MI-192 |
| Catalog No.GC11949 |
Le MI-192 est un inhibiteur sélectif de HDAC2 et HDAC3 avec des IC50 de 30 nM et 16 nM, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1415340-63-4
Sample solution is provided at 25 µL, 10mM.
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MI-192 is a histone deacetylases (HDACs) inhibitor that preferentially inhibits HDAC2 and HDAC3 with IC50 values of 30 nM and 16 nM, respectively [1].
Histone acetylation is the most commonly employed mechanism utilized by transcription factors to activate gene expression. Conversely, histone deacetylation is the most common mechanism used to inactivate genes. Histone deacetylase inhibitors (HDACIs) are in advanced clinical development as cancer therapeutic agents [1].
MI-192 is a novel benzamide-based compound that had marked selectivity for the class I enzymes, HDAC2 and HDAC3. In HeLa cell extracts, MI-192 inhibited HDAC activity with IC50 value of 1.5 μM. MI-192 selectively inhibited recombinant HDAC2 and HDAC3 with IC50 values of 30 nM and 16 nM, respectively over HDAC1, 4, 6, 7, and 8 (IC50s = 4.8, 5, >10, 4.1, and >10 μM, respectively). MI-192 showed the greatest growth inhibitory effect against the leukemic cell lines with an effective dose of 0.1-0.4 μM. MI-192 was cytotoxic and promoted apoptosis and differentiation in leukaemic cell lines [1]. In the human prostate cancer cell line PC3, MI-192 significantly increased tubulin acetylation and ablated the dynamic behaviour of microtubules in live cells [2].
References:
[1]. Boissinot, M.,Inman, M.,Hempshall, A., et al. Induction of differentiation and apoptosis in leukaemic cell lines by the novel benzamide family histone deacetylase 2 and 3 inhibitor MI-192. Leukemia Research 36, 1304-1310 (2012).
[2]. Bacon T, Seiler C, Wolny M, et al. Histone deacetylase 3 indirectly modulates tubulin acetylation. Biochem J. 2015 Dec 15;472(3):367-77.
| Cas No. | 1415340-63-4 | SDF | |
| Chemical Name | N-(2-aminophenyl)-4-[(3,4-dihydro-4-methylene-1-oxo-2(1H)-isoquinolinyl)methyl]-benzamide | ||
| Canonical SMILES | O=C1N(CC2=CC=C(C(NC3=CC=CC=C3N)=O)C=C2)CC(C4=CC=CC=C41)=C | ||
| Formula | C24H21N3O2 | M.Wt | 383.4 |
| Solubility | ≤5mg/ml in DMSO;1mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6082 mL | 13.0412 mL | 26.0824 mL |
| 5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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