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GSK J5

رقم الكتالوجGC17118 Copy One-Click Copy Product Info

inactive isomer of GSK J4, KDM inhibitor

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GSK J5 التركيب الكيميائي

Cas No.: 1394854-51-3

الحجم السعر المخزون الكميّة
1mg
39٫00
متوفر
5mg
147٫00
متوفر
10mg
255٫00
متوفر
50mg
1078٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.



Description of GSK J5

The histone H3 lysine 27 (H3K27) demethylase JMJD3 plays important roles in the transcriptional regulation of cell differentiation, development, the inflammatory response, and cancer.[1],[2]. GSK-J4 is a cell-permeable prodrug which is modified by intracellular esterases to give GSK-J1, an inhibitor of JMJD3. GSK-J5 is a pyridine regio-isomer of GSK-J4. Like GSK-J4, this isomer is cell-permeable and hydrolyzed to a free base.3 However, the free base is a weak inhibitor of JMJD3 (IC50 > 100 μM), making it an ideal inactive control molecule for elucidating the functional role of JMJD3 inhibition.[3]

Reference:
[1]. Agger, K., Cloos, P.A.C., Christensen, J., et al. UTX and JMJD3 are histone H3K27 demethylases involved in HOX gene regulation and development. Nat.Lett. 449(7163), 731-734 (2011).
[2]. Hübner, M.R., and Spector, D.L. Role of H3K27 demethylases Jmjd3 and UTX in transcriptional regulation. Cold Spring Harb.Symp.Quant.Biol. 75, 43-49 (2010).
[3]. Kruidenier, L., Chung, C.W., Cheng, Z., et al. A selective jumonji H3K27 demethylase inhibitor modulates the proinflammatory macrophage response. Nature 488, 404-408 (2012).

Chemical Properties of GSK J5

Cas No. 1394854-51-3 SDF
Chemical Name ethyl 3-((6-(4,5-dihydro-1H-benzo[d]azepin-3(2H)-yl)-2-(pyridin-3-yl)pyrimidin-4-yl)amino)propanoate
Canonical SMILES CCOC(CCNC1=CC(N2CCC3=CC=CC=C3CC2)=NC(C4=CN=CC=C4)=N1)=O
Formula C24H27N5O2 M.Wt 417.5
الذوبان 20mg/mL in ethanol, 30mg/mL in DMSO or in DMF Storage Store at RT
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 GSK J5

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.3952 mL 11.976 mL 23.9521 mL
5 mM 479 μL 2.3952 mL 4.7904 mL
10 mM 239.5 μL 1.1976 mL 2.3952 mL
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In vivo Formulation Calculator (Clear solution) of GSK J5

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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.

Product Documents

Quality Control & SDS

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Review for GSK J5

Average Rating: 5 ★★★★★ (Based on Reviews and 9 reference(s) in Google Scholar.)

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