| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
PI4KIIIβ (phosphatidylinositol 4-kinase III beta).
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|---|---|
| ln Vitro |
MI 14 (compound 36t) exhibits antiviral activity in HeLa cells against HCV 1b (EC50=0.087 µM), CVB3 (EC50=0.145 µM), HRVM (EC50=1.03 µM), and HVC 2a (EC50=10.6 µM) [1]. MI 14 does not inhibit phosphatidylinositol 3Δ (PI3Ka, PI3Kb, PI3Kd, and PI3Kg), with an IC50 as high as 10 µM[1].
MI-14 is a potent and selective PI4KIIIβ inhibitor with an IC50 of 54 nM. It exhibits >1,800-fold selectivity for PI4KIIIβ over PI4KIIIα and PI4KIIα (IC50 >100 µM for both). The compound shows antiviral activity against single-stranded positive-sense RNA viruses in HeLa cell-based assays, including HCV 1b, CVB3, HRV, and HCV 2a. MI-14 inhibits glycogen synthase kinase-3 (GSK-3) and resistance develops through kinase domain mutations. |
| ln Vivo |
In vivo efficacy data for MI-14 is limited. The compound is primarily used as an in vitro tool for studying PI4KIIIβ biology and viral replication. As a PI4KIIIβ inhibitor, it has potential applications in studying host-directed antiviral strategies, as PI4KIIIβ is a host factor required for the replication of several positive-sense RNA viruses. Further in vivo studies would be needed to assess its therapeutic potential.
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| Enzyme Assay |
The in vitro enzyme assay for PI4KIIIβ inhibition uses recombinant human PI4KIIIβ enzyme and a lipid substrate (phosphatidylinositol). The reaction mixture contains PI4KIIIβ, phosphatidylinositol, ATP (including γ-33P-ATP), and varying concentrations of MI-14 (typically 0.1 nM to 100 µM). After incubation at 30°C for 30-60 minutes, the reaction is stopped with EDTA. The phosphorylated product (phosphatidylinositol 4-phosphate) is separated by TLC or filter-binding assay. Radioactivity is measured by scintillation counting. The IC50 is calculated from dose-response curves. Selectivity is determined by profiling against PI4KIIIα, PI4KIIα, and other lipid kinases.
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| Cell Assay |
In vitro cellular assays are performed using HeLa cells infected with single-stranded positive-sense RNA viruses such as HCV, CVB3, or HRV. Cells are treated with MI-14 at concentrations ranging from 0.01 to 100 µM for 24-72 hours. Viral replication is quantified by measuring viral RNA levels using quantitative RT-PCR or by assessing viral titers via plaque assays. Cytotoxicity is assessed using MTT or CellTiter-Glo assays to determine the selectivity index (SI = CC50/EC50). The compound's effect on host cell PI4KIIIβ activity is confirmed by measuring cellular phosphatidylinositol 4-phosphate levels.
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| Animal Protocol |
In vivo animal model data for MI-14 is not extensively reported in the literature. As a research tool for studying viral replication and host-directed antiviral strategies, the compound would typically be evaluated in small animal models of viral infection, such as mouse models of HCV or coxsackievirus infection. Pharmacokinetic studies would assess oral bioavailability, plasma half-life, and tissue distribution. Standard efficacy studies would involve viral challenge followed by compound administration, with viral load and survival as primary endpoints.
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| ADME/Pharmacokinetics |
MI-14 has a molecular weight of 450.94 g/mol and molecular formula C19H23ClN6O3S. It is soluble in DMSO (9.02 mg/mL) and should be stored at +4°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-14. As a research compound, it is not intended for human use and has not undergone formal toxicological evaluation. Standard preclinical safety assessments for kinase inhibitors typically include selectivity profiling against a panel of kinases to assess off-target effects, hERG channel inhibition for cardiac safety, and CYP450 enzyme inhibition for drug-drug interaction potential. The compound is stable for up to 12 months when stored frozen.
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| References | |
| Additional Infomation |
MI-14 is a research-grade chemical probe for studying PI4KIIIβ biology and host-directed antiviral mechanisms. It is not approved for clinical use. The compound is supplied as a solid with ≥98% purity and should be stored at +4°C. It inhibits glycogen synthase kinase-3 (GSK-3) and resistance develops through kinase domain mutations. MI-14 can be co-applied with RdRP or protease inhibitors to achieve dual inhibition of viral replication and host signaling pathways.
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| Molecular Formula |
C19H23CLN6O3S
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|---|---|
| Molecular Weight |
450.94
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| Exact Mass |
450.124
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| CAS # |
1715934-43-2
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| PubChem CID |
91758319
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.661
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| LogP |
1.97
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
703
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C=C(C2=NC(C)=C(C3=CC=CC(=C3)S(N(C)C)(=O)=O)N2N=1)NCCNC(C)=O
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| InChi Key |
PSTAJIONBVMKLA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H23ClN6O3S/c1-12-18(14-6-5-7-15(10-14)30(28,29)25(3)4)26-19(23-12)16(11-17(20)24-26)22-9-8-21-13(2)27/h5-7,10-11,22H,8-9H2,1-4H3,(H,21,27)
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| Chemical Name |
N-[2-[[6-chloro-3-[3-(dimethylsulfamoyl)phenyl]-2-methylimidazo[1,2-b]pyridazin-8-yl]amino]ethyl]acetamide
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| Synonyms |
MI14; MI 14; MI-14
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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 | 2.2176 mL | 11.0879 mL | 22.1759 mL | |
| 5 mM | 0.4435 mL | 2.2176 mL | 4.4352 mL | |
| 10 mM | 0.2218 mL | 1.1088 mL | 2.2176 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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