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CP21R7 GSK3β inhibitor

Catalog No.C4009
Size Price Stock Qty
5mg
$179.00
In stock
10mg
$316.00
In stock
25mg
$683.00
In stock

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Email: [email protected]

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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & MSDS

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Chemical structure

CP21R7

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Chemical Properties

Cas No. 125314-13-8 SDF Download SDF
Chemical Name 3-(3-aminophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione
Canonical SMILES NC1=CC=CC(C(C(N2)=O)=C(C3=CN(C)C4=C3C=CC=C4)C2=O)=C1
Formula C19H15N3O2 M.Wt 317.3
Solubility ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide Storage Store at -20°C
Physical Appearance A crystalline solid Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

CP21R7 is a potent and selective inhibitor of GSK3β.

The glycogen synthase kinase-3β (GSK-3β), a serine/threonine, is a ubiquitous kinase that participates in a multitude of cellular processes, such as cell membrane-to-nucleus signaling, gene transcription, translation, cytoskeletal structuring and cell cycle progression and survival [1].

In vitro: CP21R7 was an inhibitor of GSK3β and PKCα with the IC50 values of 1.8 and 1900 nM, respectively [1]. In the human reporter cell line, CP21R7 potently activated canonical Wnt signallingeven at the dose of 1 μM, with highest activity seen at 3 μM [2]. In human iPSCs exposed to N2B27 medium, supplemented with 1 μM GSK3β inhibitor CP21R7 strongly upregulated the expression of T (also known as Brachyury, T/BRY), a meso-endoderm marker expressed in the primitive streak [2].

References:
[1] Gong L, Hirschfeld D, Tan Y C, et al.  Discovery of potent and bioavailable GSK-3β inhibitors[J]. Bioorganic & medicinal chemistry letters, 2010, 20(5): 1693-1696.
[2] Ciampi O, Iacone R, Longaretti L, et al.  Generation of functional podocytes from human induced pluripotent stem cells[J]. Stem cell research, 2016, 17(1): 130-139.