CHIR99021
CHIR99021 is a highly selective GSK-3 (glycogen synthase kinase 3) inhibitor. It shows no cross-reactivity with CDKs (cyclin-dependent kinases).It is used in differentiation induction processes to generate neural cells, cardiomyocytes, hepatocytes, retinal cells, pancreatic islet β-cells, renal tubular cells, and nephron progenitor cells from human ES/iPS cells.
We provide ISO9001-certified products developed for basic research in drug discovery and regenerative medicine, as well as products for the commercial production of regenerative medicine products compliant with ICH-Q7 (GMP for APIs).
C22H18Cl2N8=465.34
| CHIR99021 Products | Size | Availability/Price |
|---|---|---|
| CHIR99021 (GMP-compliant) | 5 mg | Check Availability & Price |
| 25 mg | ||
| CHIR99021, MF | 5 mg | Check Availability & Price |
| 25 mg | ||
| CultureSure® CHIR99021 | 5 mg | Check Availability & Price |
| 25 mg | ||
| 500 mg | ||
| CultureSure® 10mmol/L CHIR99021 DMSO Solution, Animal-derived-free |
300 μL | Check Availability & Price |
Overview
CHIR99021 is a potent glycogen synthase kinase 3 (GSK3) inhibitor and a compound classified as an aminopyrimidine derivative. It inhibits both GSK3β (IC₅₀ = 6.7 nM) and GSK3α (IC₅₀ = 10 nM) (Ring D, et al., 2003).
GSK3 inhibitors suppress the activity of GSK3 within the Wnt/β-catenin pathway and promote the nuclear translocation of β-catenin by inhibiting its degradation. Since Sato et al. demonstrated in 2004 that activation of the Wnt pathway via GSK-3 inhibition plays a crucial role in maintaining the pluripotency of mouse and human embryonic stem cells (Sato N, et al., 2004), there has been active development of inhibitors and activators related to this signaling pathway. Among these, BIO, SB-216763, and CHIR98014 are known as representative GSK-3 inhibitors; in particular, CHIR99021 is characterized by low cytotoxicity and high ability to activate the Wnt/β-catenin pathway.
CHIR99021 is used for a wide range of applications, including somatic cell reprogramming, maintenance of pluripotent stem cells, promotion of cell proliferation, and even the induction of differentiation into specific tissue cells.
Key Applications of CHIR99021
Maintenance and Self-Renewal of Stem Cells
- When used in combination with PD0325901 in the presence of LIF, CHIR99021 promotes the maintenance of undifferentiated mouse ES cells （Ying QL, et al., 2008）。
- CHIR99021 promotes the proliferation of mouse and human intestinal stem cells（Wang F, et al.,2015）
- CHIR99021 promotes the proliferation of NOD mouse-derived ES cells when used in combination with Wnt3a and Kenpaullone（Hanna J, et al, 2009）。
Reprogramming
- CHIR99021 enables the chemical reprogramming of mouse embryonic fibroblasts when used in combination with Forskolin, Tranylcypromine, Valproic Acid, 3-Deazaneplanocin A, and E-616452（Hou P, et al.,2013）。
- Induction of pluripotent stem cells is possible from non-responsive mouse strains（Garbutt TA et al., 2020）
- When combined with OCT4 and other small molecules, CHIR99021 promotes the reprogramming of human somatic cells into iPS cells（Zhu S, et al., 2010）。
- In combination with Forskolin, ISX-9, SB431542, and I-BET151, CHIR99021 enables direct reprogramming of mouse fibroblasts into mature neurons（Li X, et al., 2015）。
Differentiation Induction
- CHIR99021 promotes the differentiation of human iPS cells into insulin-producing cells.（Kunisada Y, et al., 2012）
- CHIR99021 promotes the differentiation of human ES cells and iPS cells into cardiomyocytes.（Lian X, et al., 2012）
- CHIR99021, when used in combination with SB431542 and human recombinant LIF, induces and maintains neural stem cells derived from human embryonic stem cells.（Li W, et al., 2011）
Chemical Information for CHIR9901
| CAS RN® | 252917-06-9 |
|---|---|
| Chemical Formula | C22H18Cl2N8 |
| Molecular Weight | 465.34 |
| Purity (HPLC) |
CHIR99021 (GMP-compliant) : ≧99.5% CHIR99021, MF：≧98.0% CultureSure® CHIR99021 : ≧97.0% |
| Chemical Name | 6-{2-[4-(2,4-Dichloro-phenyl)-5-(5-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino]-ethylamino}-nicotinonitrile |
Product Information
CHIR99021 (GMP-compliant)
This product is complied with ICH-Q7 (GMP for APIs) and is intended as a raw material for the commercial production of regenerative medicine products. It has been tested for viable count, as well as bacterial endotoxins, mycoplasma contamination, and residual solvent.
- GMP compliant
- Process validation and analytical validation carried out
- No animal-derived ingredients are used as raw materials
CHIR99021, MF
This is an ISO9001-compliant product developed for the commercial manufacturing of regenerative medicine products. It has been tested for viable count, as well as bacterial endotoxins and mycoplasma contamination.
The management and manufacturing standards have been established internally.
- ISO9001 compliant
- Reduction of contamination risk through the use of dedicated equipment for manufacturing culture media additives
- Process validation, analytical validation, and cleaning validation carried out
- No animal-derived ingredients are used as raw materials
CultureSure® CHIR99021
This product was developed for basic research in drug discovery and regenerative medicine. It has been tested for bacterial endotoxins and mycoplasma contamination.
- ISO9001 compliant
- No animal-derived ingredients are used as raw materials
CultureSure® 10mmol/L CHIR99021 DMSO Solution, Animal-derived-free
This product is a 10 mmol/L DMSO solution of CHIR99021. It has been tested for sterility, as well as bacterial endotoxins and mycoplasma contamination. It has been 0.1 μm filter-sterilized and can be added directly to the culture medium.
- ISO9001 compliant
- No animal derived-ingredients are used as raw materials
CHIR99021 Comparison Chart
| ICH-Q7 | ISO9001 | Sterility test | Viable count test | No animal-derived ingredients used | Bacterial endotoxin test | Mycoplasma test | Residual solvent | Powder/Liquid | References* | |
|---|---|---|---|---|---|---|---|---|---|---|
| CHIR99021 (GMP-compliant) | ✓ | ✓ | - | ✓ | ✓ | ✓ | ✓ | ✓ | Powder | - |
| CHIR99021, MF | - | ✓ | - | ✓ | ✓ | ✓ | ✓ | - | Powder | - |
| CultureSure ® CHIR99021 | - | ✓ | - | - | ✓ | ✓ | ✓ | - | Powder | □ |
| CultureSure ® 10mmol/L CHIR99021 DMSO Solution, Animal-derived-free | - | ✓ | ✓ | - | ✓ | ✓ | ✓ | - | Liquid | □ |
Applications
CHIR99021 is used for effective differentiation induction of iPS/ES cells.
Based on the latest findings reported in the literature, we introduce examples of the usage steps for our products.
Neural Cells
Cardiomyocytes
Respiratory organoid
Pancreas
Preparing Stock Solutions for CHIR99021
The powder CHIR99021 product has been confirmed to be soluble in DMSO. After dilution, filter sterilize before use. Refer to the protocol at the top of this page for general usage in ES/iPS cell culture.
Amount of solvent and powder when preparing solution
| CHIR99021 (powder) | ||||
|---|---|---|---|---|
| 1 mg | 5 mg | 10 mg | ||
| Concentration | 1 mmol/L | 2.149 mL | 10.745 mL | 21.490 mL |
| 5 mmol/L | 0.430 mL | 2.149 mL | 4.298 mL | |
| 10 mmol/L | 0.215 mL | 1.074 mL | 2.149 mL | |
| 50 mmol/L | 0.043 mL | 0.215 mL | 0.430 mL | |
| Solvent Volume | |||||
|---|---|---|---|---|---|
| 0.3 mL | 1 mL | 5 mL | 10 mL | ||
| Concentration | 1 mmol/L | 0.140 mg | 0.465 mg | 2.327 mg | 4.653 mg |
| 5 mmol/L | 0.698 mg | 2.327 mg | 11.634 mg | 23.267 mg | |
| 10 mmol/L | 1.396 mg | 4.653 mg | 23.267 mg | 46.534 mg | |
| 50 mmol/L | 6.980 mg | 23.267 mg | 116.335 mg | 232.670 mg | |
Resources and Publications
Literature and Education
- Map of Culture Compounds and Cytokines
- Small Molecules Catalog
- On-demand webinar：Impact of ROCK inhibitor in suspension aggregate culture of iPS cells
- FUJIFILM Wako Life Science Webinar Series
Publications
| CultureSure® CHIR99021 |
|---|
| Kitai, Y., et al.: J. Gen. Virol., 106, 002131 (2025). Changes in ORF4 of HCoV-229E under different culture conditions |
| Nakata, Y., et al.: iScience., 28,114105 (2025). Mpox virus OPG175 negatively regulates viral replication by controlling Wnt signaling |
| Umei, TC., et al.: iScience., 28, 112843 (2025). Serine synthesis pathway regulates cardiac differentiation from human pluripotent stem cells |
| Soma, Y., et al.: iScience., 27, 111234 (2024) Metabolic changes of human induced pluripotent stem cell-derived cardiomyocytes and teratomas after transplantation |
| Katayama, M., et al.: PLoS One, 18, e0285356 (2023). Organoids containing neural-like cells derived from chicken iPSCs respond to poly:IC through the RLR family |
| Moriwaki, T., et al.: Cell Rep. Methods, 3, 100666 (2023) Scalable production of homogeneous cardiac organoids derived from human pluripotent stem cells |
| CultureSure® 10mmol/L CHIR99021 DMSO Solution, Animal-derived-free |
|---|
| Inage, Y., et al.: Int J. Mol. Sci., 25, 4793 (2024). Fetal Kidney Grafts and Organoids from Microminiature Pigs: Establishing a Protocol for Production and Long-Term Cryopreservation |
| Yamasaki, S., et al.: iScience, 25, 103657 (2021). A Genetic modification that reduces ON-bipolar cells in hESC-derived retinas enhances functional integration after transplantation |
Glossary
GMP
Good Manufacturing Practice (GMP) is a standard for manufacturing and quality control of pharmaceutical drugs, etc., and should be observed by manufacturers of pharmaceutical drugs, etc.
The GMP standards are based on the following three principles:
- Minimizing human errors during manufacture
- Preventing contamination and quality deterioration of pharmaceutical products
- Designing a system for high quality assurance
ICH-Q7 (GMP for APIs)
International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use (ICH) is an international initiative to create guidelines on pharmaceutical regulations from scientific and technical perspectives by joint efforts of regulatory authorities and representatives of the pharmaceutical industry.
Among these guidelines, ICH-Q7 (GMP for APIs (Active Pharmaceutical Ingredients)) outlines the standard practices for manufacturing management and quality control related to active pharmaceutical ingredients.
ISO9001
ISO stands for the International Organization for Standardization, a non-governmental organization. The standards established by the ISO are referred to as ISO standards. These are internationally agreed-upon criteria established by experts, covering various areas such as product manufacturing, process management, service provision, and material supply.
ISO 9001 is a standard set out for quality management systems. Many companies and organizations are certified to ISO 9001 to ensure that their customers consistently receive good quality products and services.
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