PI4KIII beta inhibitor 3

Name: PI4KIII beta inhibitor 3
Brand: MedChemExpress
SKU: HY-15679
Rating: 5.0 (2 reviews)

Cat. No.: HY-15679 Purity: 99.77%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 1245319-54-3

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 385	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 385	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 350	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1400	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

2 Publications Citing Use of MCE PI4KIII beta inhibitor 3

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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.

1245319-54-3

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
10 mM	0.2239 mL	1.1197 mL	2.2395 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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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.77%

Select Batch:

Data Sheet (277 KB) SDS (252 KB)

COA (251 KB) HNMR (258 KB) RP-HPLC (240 KB) LCMS (101 KB)

Handling Instructions (2659 KB)

References

[1]. Jean Herman, et al. Autoimmune and inflammatory disorder therapy. From PCT Int. Appl. (2013), WO 2013034738 A1

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

[1]. Jean Herman, et al. Autoimmune and inflammatory disorder therapy. From PCT Int. Appl. (2013), WO 2013034738 A1

Complete Stock Solution Preparation Table

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