PI4KIII beta inhibitor 3
Based on 3 publication(s) in Google Scholar
PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC50 of 5.7 nM.
For research use only. We do not sell to patients.
- Purity: 99.36%
- CAS No.: 1245319-54-3
- Formula: C22H22N8OS
- Molecular Weight:446.53
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Storage:
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PI4KIII beta inhibitor 3
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Biological Activity
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PI4KIIIβ 5.7 nM (IC50) |
PI4KIII beta inhibitor 3 is a PI4KIII inhibitor extracted from patent WO/2013034738 A1, the compound of formula 3, has an IC50 of 5.7 nM. PI4KIII beta inhibitor 3 exerts significant immunosuppressive activity, with IC50 value of 3 nM in the mixed lymphocyte reaction (MLR) assay. PI4KIII beta inhibitor 3 inhibits IL2 and IFNy secretion with IC50 values of less than InM in each case. Thus, PI4KIII beta inhibitor 3 is shown to be as effective at inhibiting IL2 and IFNy secretion as conventional immunosuppressants such as cyclosporine A. IC50 on IFNy and IL-2 release of Cyclosporine A are 2nM and less than 1 nM respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1245319-54-3
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Appearance Solid
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Molecular Weight 446.53
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Formula C22H22N8OS
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Color Light yellow to yellow
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SMILES
O=C(N1CCN(C2=C3C(SC(C4=CC=CN=C4)=N3)=NC(N)=N2)CC1)NC5=CC=C(C)C=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)
Publications (3)
Solvent & Solubility
DMSO : 20 mg/mL (44.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocol
Mice[1]
DBA1 male mice, 8-10 weeks old, are distributed in 2 groups according to the treatment. Twelve animals received daily treatment with vehicle (1% methylcellulose), twelve others receive PI4KIII beta inhibitor 3 at 40 mg/kg/d in 1% methylcellulose. The treatment initiation started the day before the intradermal injection at the base of the tail of 100 μg of emulsified chicken collagen II in presence of complete Freund adjuvant and added heat-killed Mycobacterium butyricum. Daily inspection of the mice is performed to weight animals and quantify disease score according to the following scale (score 0: normal; score 1 : redness and/or swelling in one joint; score 2: redness and/or swelling in more than one joint; score 3: redness and/or swelling in the entire paw; score 4: deformity and/or ankylosis). On the day of sacrifice (day 42) serum are collected and anti-collagen II antibody titers are determined by ELISA. Joints are harvested, fixed in 6% paraformaldehyde, decalcified in formic acid 6% for 48 h, sliced and stained by hematoxylin and eosin staining. Hyperplasia of the synovium, infiltration of mono and polymorphonuclear cells and pannus formation parameters are scored blindly.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (protect from light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2395 mL | 11.1975 mL | 22.3949 mL | 55.9873 mL |
| 5 mM | 0.4479 mL | 2.2395 mL | 4.4790 mL | 11.1975 mL | |
| 10 mM | 0.2239 mL | 1.1197 mL | 2.2395 mL | 5.5987 mL | |
| 15 mM | 0.1493 mL | 0.7465 mL | 1.4930 mL | 3.7325 mL | |
| 20 mM | 0.1120 mL | 0.5599 mL | 1.1197 mL | 2.7994 mL | |
| 25 mM | 0.0896 mL | 0.4479 mL | 0.8958 mL | 2.2395 mL | |
| 30 mM | 0.0746 mL | 0.3732 mL | 0.7465 mL | 1.8662 mL | |
| 40 mM | 0.0560 mL | 0.2799 mL | 0.5599 mL | 1.3997 mL |
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