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PKM2-IN-3

Catalog No.GC70831 Copy One-Click Copy Product Info

PKM2-IN-3 est un inhibiteur de la kinase pkm2 avec une IC50 de 4,1 µm.

Products are for research use only. Not for human use. We do not sell to patients.

PKM2-IN-3 Chemical Structure

Cas No.: 2408841-19-8

Taille Prix Stock Qté
5 mg
234,00 $US
En stock
10 mg
342,00 $US
En stock
25 mg
720,00 $US
En stock

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Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.



Description of PKM2-IN-3

PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.

PKM2-IN-3 (compound 10i) inhibits the TNF-α release of LPS-stimulated RAW264.7 macrophages, with an IC50 value of 5.2 μM. PKM2-IN-3 exhibits the lowest toxicity with a CC50 value of 43.6 μM[1].
PKM2-IN-3 (0.1-100 μM; 20 min) inhibits PKM2 kinase activity in a cell-free molecular level with an IC50 value of 4.1 μM[1].

PKM2-IN-3 (1, 10 mg/kg; i.p.; daily for 3 days ) significantly reverses the LPS-induced mice behavior changes in open field test[1].
PKM2-IN-3 (1, 10 mg/kg; i.v.; injected at 4 hours and 24 hours after ischemia onset) reduces the infarct volume and improves neurological deficits of tMCAO rats[1].

References:
[1]. Gao CL, et al. Synthesis and Target Identification of Benzoxepane Derivatives as Potential Anti-Neuroinflammatory Agents for Ischemic Stroke. Angew Chem Int Ed Engl. 2020;59(6):2429-2439.

Chemical Properties of PKM2-IN-3

Cas No. 2408841-19-8 SDF
Formula C21H22O4 M.Wt 338.4
Solubility DMSO : 200 mg/mL (591.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Storage -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of PKM2-IN-3

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1 mg 5 mg 10 mg
1 mM 2.9551 mL 14.7754 mL 29.5508 mL
5 mM 591 μL 2.9551 mL 5.9102 mL
10 mM 295.5 μL 1.4775 mL 2.9551 mL
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In vivo Formulation Calculator (Clear solution) of PKM2-IN-3

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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