0
Specifications:
| Application | Protein Biology, Cell Analysis | ||
| Storage Temperature | -20°C | ||
| Product Type | Laboratory Chemical, Enzymes | Forms | Solid |
| Product Brand | Thermo Fisher Scientific™, thermo Scientific | ||
| Product Grade | Analytical grade | Formula | C₂₂H₁₈Cl₂N₈ |
CHIR99021 is a potent, selective, and widely cited Glycogen Synthase Kinase 3 (GSK-3) inhibitor used extensively in stem cell biology and signal transduction studies. It belongs to the aminopyrimidine class of small molecule inhibitors and exhibits high selectivity for GSK-3α (IC₅₀ = 10 nM) and GSK-3β (IC₅₀ = 6.7 nM) with minimal cross-reactivity to CDKs or other kinases.
Thermo Fisher’s CHIR99021 is offered at ≥95% purity, validated by HPLC, MS, and ¹H-NMR, and is supplied as a white to yellow powder or solid.
Key Specifications
| Property | Value |
|---|---|
| Appearance | White to yellow powder/solid |
| HPLC Purity | ≥94% (typically ≥95%) |
| Mass Spectrometry (MS) | Complies |
| ¹H-NMR | Structure confirmed |
| Melting Point | Not specified (solid form stable) |
| Storage Temperature | –20 °C (Freezer) |
| Safety Class | GHS07 – Irritant |
| Unit Size | 100 mg |
Mechanism of Action
CHIR99021 is a highly selective ATP-competitive GSK-3 inhibitor, targeting both GSK-3α and GSK-3β isoforms, which are key negative regulators in several signaling pathways including:
- Wnt/β-catenin pathway
- TGF-β, Notch, and MAPK pathways
- Stem cell proliferation and differentiation
By inhibiting GSK-3, CHIR99021 stabilizes β-catenin, promotes c-Myc activity, and enhances cell cycle progression, making it essential for research in developmental biology, oncology, and cell reprogramming.
Applications in Research
CHIR99021 is widely used as a Wnt signaling agonist and stem cell self-renewal enhancer, with diverse research applications including:
- Maintenance and expansion of embryonic stem cells (ESCs) and induced pluripotent stem cells (iPSCs)
- Directed differentiation of hPSCs into cardiomyocytes
- Neural reprogramming of human lung fibroblasts into neurons
- Blastocyst development in KSOM-supplemented media
- Chronic inhibition of GSK-3 in corticogenesis and neurodevelopment
- Oncology studies in non-small-cell lung cancer (NSCLC) cell lines
Biochemical Actions
- Inhibits GSK-3α and GSK-3β with IC₅₀ values of 10 nM and 6.7 nM respectively
- No cross-reactivity with cyclin-dependent kinases (CDKs)
- Upregulates β-catenin, cyclin A, c-Myc
- Modulates key pathways: Wnt, TGF-β, MAPK, Notch
- Promotes self-renewal and survival in stem cell cultures
- Enhances cellular reprogramming and tissue regeneration research
Use Cases (Cited Applications)
- In cocktail with other small molecules to convert fibroblasts to neurons
- To enhance blastocyst viability in KSOM media
- For chronic GSK-3 inhibition in cortical development studies
- As an agonist of Wnt signaling in ESC/iPSC-derived cardiomyocyte protocols
Thermo Fisher Scientific CHIR99021 (≥95%) is a gold-standard GSK-3 inhibitor and a vital reagent for stem cell research, cell signaling studies, and small molecule screening platforms. Its high purity, validated identity, and proven effectiveness across numerous published protocols make it an essential tool for researchers working in developmental biology, regenerative medicine, neuroscience, and cancer biology.