CHIR99021 (Qk1101) Price range: £110.00 through £230.00View product
CHIR99021 (Qk1101)
Price range: £110.00 through £230.00
CHIR99021 is a potent inhibitor of the serine/threonine kinase glycogen synthase kinase (GSK)-3. GSK-3 is a key inhibitor of the Wnt pathway, an import regulatory mechanism in stem cell biology, inhibition of GSK-3 with CHIR99021 activates Wnt promoting stem cell maintenance and differentiation. In cell culture, CHIR99021 is used to stimulate neural and cardiac differentiation in pluripotent stem cells, it can also promote self-renewal in embryonic stem cells (ESCs).
Qkine CHIR99021 (Qk1101) is highly pure and validated in iPSC differentiation into definitive endoderm.
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Price range: £110.00 through £230.00
Sourced from a trusted supplier and order fulfilled by Qkine, 10 mg will be dispatched as 2 x 5 mg
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Summary:
- Cas No. 252917-06-9
- Molecular Weight: 465.34
Chemical name: 6-[[2-[[4-(2,4-Dichlorophenyl)-5-(5-methyl-1H-imidazol-2-yl)-2-pyrimidinyl]amino]ethyl]amino]-3-pyridinecarbonitrile
Formula: C22H18Cl2N8
Storage: powder -20°C for 1 year, in solvent -80°C for 1 year
Solubility in DMSO: 105 mg/ml (225.6 mM)
Featured applications:
Differentiation of iPSC into endoderm
iPSC-derived mesoderm differentiation
Differentiation of midbrain dopaminergic neurons
Self-renewal in mouse and human embryonic stem cells
Frequently used together
- Recombinant human BDNF protein (Qk050)
- Recombinant human GDNF protein (Qk051)
- Recombinant human TGF-β3 protein (Qk054)
- Recombinant human FGF-8a protein (Qk059)
- HiDef® N-2 neural medium supplement
- Recombinant human activin A protein (Qk001)
- Recombinant human BMP-4 protein (Qk038)
- Recombinant FGF2-G3 (145 aa) protein (Qk052)
Further quality assays
>99% purity
HPLC/HNMR: Consistent with structure
We are a company founded and run by scientists to provide a service and support innovation in stem cell biology and regenerative medicine. All our products are exceptionally high purity, with complete characterisation and bioactivity analysis on every lot.
Preparation of CHIR99021 stock solution in DMSO
| 2 mg | 5 mg | 10 mg | |
| 1 mM | 4.30 ml | 10.74 ml | 21.49 ml |
| 2 mM | 2.15 ml | 5.37 ml | 10.74 ml |
| 5 mM | 0.86 ml | 2.15 ml | 4.30 ml |
| 10 mM | 0.04 ml | 1.07 ml | 2.15 ml |
Product background
CHIR99021 is an aminopyrimidine derivative which acts as a potent and selective GSK-3α/β inhibitor (IC50=10/6.7 nM) and activator of the Wnt/β-catenin signaling pathway [1]. This pathway is key in the regulation of embryo development and adult tissue homeostasis and is highly conserved between species [2]. In the absence of Wnt signaling β-catenin is phosphorylated and degraded by a complex containing molecular scaffolds, ligases and protein kinases, including GSK-3α/β [3, 4]. Wnt activation leads to the stabilization of β-catenin, which then accumulates in the nucleus and activates expression of target genes [2]. Wnt/β-catenin target genes involved in negative feedback, such as AXIN2, RNF43 and ZNRF3 and other which further potentiate the signal, such as LGR5 which binds to R-spondin ligands [4].
Activation of the Wnt pathway is essential to maintain the organoids from the human intestine, colon, liver, pancreas and stomach [4]. As a component of stem cell culture medium, CHIR99021 plays an important role in the maintenance of stemness in many stem cell types, including embryonic stem cells (ESCs) [1]. CHIR99021 has also been shown to increase the transdifferentiation potential of mesenchymal stem cells (MSCs) to neurological, hepatogenic and cardiomyocyte lineages [5]. It is also required in differentiation media for induced pluripotent stem cells (iPSCs) into endoderm, mesoderm and dopaminergic neurons.
FAQ
What is CHIR99021?
CHIR99021 is a potent inhibitor of the serine/threonine kinase glycogen synthase kinase (GSK)-3.
What does CHIR99021 inhibit?
Through GSK-3 CHIR99021 inhibits the Wnt signaling pathway, an import regulatory mechanism in stem cell biology.
How does CHIR99021 inhibit GSK-3?
CHIR99021 is ATP competitive and binds to the ATP-binding pocket of the GSK-3 enzyme. This blocks ATP from binding and prevents the kinase from transferring phosphate groups to its target substrates.
How selective is CHIR99021 for GSK-3?
CHIR99021 has high selectivity for GSK-3α and β, with over 500-fold selectivity above other kinases.
What concentration of CHIR99021 should I use?
Studies have shown the IC50 of CHIR99021 against GSK-3β to be 40 nM. In our laboratory we have used CHIR99021 at 3 µM for endoderm and dopaminergic neuron differentiation and 5 µM for mesoderm differentiation.
How is CHIR99021 used in stem cell culture?
In cell culture, CHIR99021 is used to stimulate neural and cardiac differentiation in pluripotent stem cells, it can also promote self-renewal in embryonic stem cells (ESCs).
How do I prepare stock solutions of Qkine small molecules?
- Briefly centrifuge the vial to recover any compound from the cap.
- Add appropriate volume of recommended solvent to the vial to create the desired concentration stock solution (see product page for recommended solvent and volume).
- Vortex to ensure solvent has contacted the walls of the vial to recover all compound.
- To fully solubilize we recommend warming to 37˚C for 5 minutes and/or sonicating in short bursts (10 sec) for up to 5 minutes.
- Vortex thoroughly and prepare stock aliquots, store -20 or -80.
Our products are for research use only and not for diagnostic or therapeutic use. Products are not for resale.
For use in manufacturing of cellular or gene therapy products. Not intended for in vivo applications.
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