CP21R7(CP21) Chemical Properties

Boiling point:

627.4±55.0 °C(Predicted)

Density 

1.37±0.1 g/cm3(Predicted)

storage temp. 

Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

solubility 

insoluble in EtOH; insoluble in H2O; ≥14.25 mg/mL in DMSO

form 

crystalline solid

pka

7.79±0.60(Predicted)

color 

Yellow to orange

InChI

InChI=1S/C19H15N3O2/c1-22-10-14(13-7-2-3-8-15(13)22)17-16(18(23)21-19(17)24)11-5-4-6-12(20)9-11/h2-10H,20H2,1H3,(H,21,23,24)

InChIKey

RGTAEYDIDMGJLX-UHFFFAOYSA-N

SMILES

N1C(=O)C(C2C3=C(N(C)C=2)C=CC=C3)=C(C2=CC=CC(N)=C2)C1=O

CP21R7(CP21) Usage And Synthesis

Uses

CP21R7 is a potent and selective inhibitor of GSK3β.

Biological Activity

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].

IC 50

GSK-3β: 1.8 nM (IC₅₀); PKCα: 1900 nM (IC₅₀)

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.

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