CP21R7
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.
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 317.3 |
| Cas No. | 125314-13-8 |
| Formula | C19H15N3O2 |
| Solubility | insoluble in EtOH; insoluble in H2O; ≥14.25 mg/mL in DMSO |
| Chemical Name | 3-(3-aminophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione |
| SDF | Download SDF |
| Canonical SMILES | NC1=CC=CC(C(C(N2)=O)=C(C3=CN(C)C4=C3C=CC=C4)C2=O)=C1 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Chemical structure
