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  3. PI4KIII beta inhibitor 3

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.

PI4KIII beta inhibitor 3 Chemical Structure

PI4KIII beta inhibitor 3 Chemical Structure

CAS No. : 1245319-54-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 385 In-stock
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10 mM * 1 mL in DMSO USD 385 In-stock
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Based on 2 publication(s) in Google Scholar

Top Publications Citing Use of Products

2 Publications Citing Use of MCE PI4KIII beta inhibitor 3

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Description

PI4KIII beta inhibitor 3 is a novel and high effective PI4KIIIβ inhibitor with IC50 of 5.7 nM.

IC50 & Target[1]

PI4KIIIβ

5.7 nM (IC50)

In Vitro

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.

In Vivo

PI4KIII beta inhibitor 3 (40 mg/kg per day, n=12) is able to delay the onset of arthritic symptoms and also to decrease symptom severity in a preventive model of arthritis compared to a vehicle control (MC 1%, n=12). PI4KIII beta inhibitor 3 reduces the anti-CII IgG titre and histological scores in the collagen-induced arthritis mouse model. Oral administration of PI4KIII beta inhibitor 3 results in prolonged graft survival in 3 out of 6 grafts in each group at day 30. Several grafts continued beating after withdrawal of the treatment (up to 60 days), indicating the induction of a certain type of graft tolerance. To evaluate the operational tolerance phenotype, animals with functional graft at day 60 are challenged with a second graft from the same donor strain or from a third party. No treatment is applied. The second grafts from the third party are rejected at day 8 (n=2) whereas second grafts from the same donor strain are functional for more than 90 days (n=2)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

446.53

Formula

C22H22N8OS

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(N1CCN(C2=C3C(SC(C4=CC=CN=C4)=N3)=NC(N)=N2)CC1)NC5=CC=C(C)C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 2 years; -20°C, 1 year (protect from light)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2395 mL 11.1975 mL 22.3949 mL
5 mM 0.4479 mL 2.2395 mL 4.4790 mL
View the 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.

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Animal Administration
[1]

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PI4KIII beta inhibitor 3
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