| Size | Price | Stock | Qty |
|---|---|---|---|
| 500μg |
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| 1mg | |||
| Other Sizes |
| Targets |
HDAC2 and HDAC3 (histone deacetylases 2 and 3).
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|---|---|
| ln Vitro |
MI-192 (0.15-1 μM; 72 h) promotes apoptosis in acute myeloid leukaemic cell lines U937, HL60, and Kasumi-1, which leads to differentiation and is cytotoxic[1].
MI-192 is a potent and selective HDAC2/3 inhibitor with IC50 values of 30 nM for HDAC2 and 16 nM for HDAC3. It exhibits >250-fold selectivity for HDAC2/3 over other HDAC isoforms (HDAC1, 4, 6, 7, 8). The compound promotes apoptosis of leukemia cell lines in vitro and attenuates IL-6 production in rheumatoid arthritis PBMCs. MI-192 has been shown to induce apoptosis in myeloid leukemia cells and possesses neuroprotective properties. |
| ln Vivo |
When photothrombotic stroke is induced in mice, MI-192 (40 mg/kg; ip; once daily; for three days) exhibits neuroprotective effects in the brain[2].
In vivo efficacy data for MI-192 is limited. The compound is primarily used as an in vitro tool for studying HDAC2/3 biology in cancer and inflammation. As an HDAC inhibitor, it has potential applications in oncology and inflammatory diseases. The compound attenuates IL-6 production in rheumatoid arthritis patient samples, suggesting potential anti-inflammatory activity. Further in vivo studies would be needed to assess its therapeutic potential. |
| Enzyme Assay |
The in vitro enzyme assay for HDAC inhibition uses purified recombinant HDAC enzymes (HDAC1-8) and a fluorogenic substrate (e.g., Boc-Lys(Ac)-AMC). MI-192 is incubated with the HDAC enzyme and substrate at varying concentrations (typically 0.1 nM to 100 µM) for 30-60 minutes at 37°C. The reaction is stopped by addition of developer solution containing trypsin, which releases the fluorophore AMC from deacetylated substrate. Fluorescence is measured at excitation 355 nm and emission 460 nm. IC50 values are calculated from dose-response curves. Selectivity is determined by profiling against all HDAC isoforms.
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: HL60 and Kasumi- 1 cells Tested Concentrations: 150 nM, 300 nM, 500 nM, 1 μM Incubation Duration: 72 h Experimental Results: Induced a substantial degree of apoptosis in both HL60 and Kasumi-1 cells. In vitro cellular assays are performed using leukemia cell lines (e.g., U937, HL-60, or K562) or rheumatoid arthritis patient PBMCs. Cells are treated with MI-192 at concentrations ranging from 0.1 to 100 µM for 24-72 hours. Apoptosis is assessed by Annexin V/PI staining and flow cytometry, or by measuring caspase-3/7 activity. Cell proliferation is measured using MTT or CellTiter-Glo assays. HDAC inhibition in cells is confirmed by assessing histone H3 and H4 acetylation levels by Western blot. IL-6 production in PBMCs is measured by ELISA following stimulation with inflammatory stimuli. |
| Animal Protocol |
Animal/Disease Models: Adult male outbred mice CD-1 (20-25 g ) with photothrombotic stroke (PTS)[2]
Doses: 40 mg/kg Route of Administration: ip; one time/day; for 3 days Experimental Results: decreased the volume of the PTS-induced infarction core in the mouse brain, partly restored the functional symmetry in the forelimb use, diminished the level of PTS-induced apoptosis and acetylation of α-tubulin characteristic for stable microtubules, and increased the expression of GAP-43 in the cerebral cortex of the damaged hemisphere. In vivo animal model data for MI-192 is not extensively reported in the literature. As a research tool for studying HDAC2/3 biology in cancer and inflammation, the compound would typically be evaluated in xenograft mouse models of leukemia or in animal models of rheumatoid arthritis. Standard efficacy studies would involve tumor growth inhibition or reduction of inflammatory markers as primary endpoints. Pharmacokinetic studies would assess oral bioavailability, plasma half-life, and tissue distribution. |
| ADME/Pharmacokinetics |
MI-192 has a molecular weight of 383.44 g/mol and molecular formula C24H21N3O2. It is soluble in DMSO and should be stored at -20°C. The compound has ≥98% purity by HPLC. Oral bioavailability and detailed pharmacokinetic parameters have not been extensively characterized in publicly available literature. As a research compound, it is typically used in in vitro assays at concentrations ranging from nanomolar to low micromolar.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is publicly available for MI-192. As a research compound, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments for HDAC inhibitors typically include selectivity profiling against a panel of HDAC isoforms to assess off-target effects, hERG channel inhibition for cardiac safety, and CYP450 enzyme inhibition for drug-drug interaction potential. The compound is supplied as a solid with ≥98% purity and should be stored at -20°C.
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| References |
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| Additional Infomation |
MI-192 is a research-grade chemical probe for studying HDAC2 and HDAC3 biology in cancer and inflammation. It is not approved for clinical use. The compound has been shown to induce apoptosis in myeloid leukemia cells and possesses neuroprotective activities. It attenuates IL-6 production in rheumatoid arthritis PBMCs. MI-192 is supplied as a solid with ≥98% purity and should be stored desiccated at -20°C.
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| Molecular Formula |
C24H21N3O2
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|---|---|
| Molecular Weight |
383.45
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| Exact Mass |
383.163
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| CAS # |
1415340-63-4
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| PubChem CID |
56965342
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
565.0±50.0 °C at 760 mmHg
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| Flash Point |
295.5±30.1 °C
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| Vapour Pressure |
0.0±1.5 mmHg at 25°C
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| Index of Refraction |
1.693
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| LogP |
2.19
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
626
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C=C1CN(C(=O)C2=CC=CC=C12)CC3=CC=C(C=C3)C(=O)NC4=CC=CC=C4N
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| InChi Key |
GTLTXEIKQVWSRF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H21N3O2/c1-16-14-27(24(29)20-7-3-2-6-19(16)20)15-17-10-12-18(13-11-17)23(28)26-22-9-5-4-8-21(22)25/h2-13H,1,14-15,25H2,(H,26,28)
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| Chemical Name |
N-(2-aminophenyl)-4-[(4-methylidene-1-oxo-3H-isoquinolin-2-yl)methyl]benzamide
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| Synonyms |
MI192 MI 192 MI-192
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6079 mL | 13.0395 mL | 26.0790 mL | |
| 5 mM | 0.5216 mL | 2.6079 mL | 5.2158 mL | |
| 10 mM | 0.2608 mL | 1.3040 mL | 2.6079 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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