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Purity: ≥98%
CP21R7 (also known CP21) is a potent and highly selective GSK-3β inhibitor that can potently activate canonical Wnt signalling with IC(50) of 0.6nM for GSK-3β. It is a maleimide analog with the incorporation of polar groups which afforded compounds with good bioavailability. CP21R7 has an IC50 of 0.6nM for GSK-3β, and is over 100-fold more selective for GSK-3β than a panel of other kinases, and CP21R7 shows efficacy in an in vivo rat osteoporosis models. The X-ray structure of GSK-3β protein with CP21R7 bound revealed the binding mode of the template and provided insights for future optimization opportunities.
| ln Vitro |
With an IC50 of 1.8 nM, CP21R7 (Compound 9) is a selective inhibitor of GSK-3β; its IC50 against PKCα is 1900 nM[1]. With maximum activity, CP21R7 (CP21, 3 μM) strongly stimulates canonical Wnt signaling. CP21 considerably raises intracellular β-catenin total levels. BMP4 and CP21 together cause hPSCs to commit to mesoderm[2].
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| References |
[1]. Gong L, et al. Discovery of potent and bioavailable GSK-3beta inhibitors. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1693-6.
[2]. Patsch C, et al. Generation of vascular endothelial and smooth muscle cells from human pluripotent stem cells. Nat Cell Biol. 2015 Aug;17(8):994-1003. |
| Molecular Formula |
C19H15N3O2
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| Molecular Weight |
317.34
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| CAS # |
125314-13-8
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| SMILES |
O=C(C(C1=CC=CC(N)=C1)=C2C3=CN(C)C4=C3C=CC=C4)NC2=O
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1512 mL | 15.7560 mL | 31.5119 mL | |
| 5 mM | 0.6302 mL | 3.1512 mL | 6.3024 mL | |
| 10 mM | 0.3151 mL | 1.5756 mL | 3.1512 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Canonical Wnt activation by GSK3ß inhibitors and mesoderm induction.Nat Cell Biol.2015 Aug;17(8):994-1003. |
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VEGF and PDGF-BB-mediated differentiation of hPSCs into vascular endothelial or vascular smooth muscle cells.Nat Cell Biol.2015 Aug;17(8):994-1003. |
In vitrocharacterization of hPSC-ECs and hPSC-VSMCs.Nat Cell Biol.2015 Aug;17(8):994-1003. |
Global transcriptome and metabolomic analyses confirm vascular cell identity of differentiated hPSCs.Nat Cell Biol.2015 Aug;17(8):994-1003. |
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Co-culture experiments andin vivocharacterization of hPSC-ECs.Nat Cell Biol.2015 Aug;17(8):994-1003. |
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