CHIR-99021 (CT99021) inhibits glycogen synthase kinase-3β (GSK3β, IC50 = 6.7 nm) and GSK3α (IC50 = 10 nm), inhibits preadipocyte differentiation (IC50 = 0.3 µM), possibly by blocking induction of C/EBPα and PPARγ, and mimics Wnt signaling in 3T3-L1 preadipocytes. CHIR99021 activates glycogen synthase in CHO-IR cells with EC50 of 763 nM. CHIR99201 does not exhibit cross-reactivity against cyclin-dependent kinases (CDKs) with 350-fold selectivity toward GSK-3β compared to CDKs.
Acta Histochem. 2022 Aug;124(6):151931.
Fibroblast-derived exosomal miRNA-133 promotes cardiomyocyte-like differentiation
CHIR-99021 purchased from AbMole
Mol Biol Cell. 2022 Jul 1;33(8):mbcP22031008.
Deciphering the tumor-specific immunopeptidome in vivo with genetically engineered mouse models
CHIR-99021 purchased from AbMole
Nature. 2022 Jul;607(7917):149-155.
Deciphering the immunopeptidome in vivo reveals new tumour antigens
CHIR-99021 purchased from AbMole
Cancer Cell. 2021 Oct 11;39(10):1342-1360.e14.
The CD155/TIGIT axis promotes and maintains immune evasion in neoantigen-expressing pancreatic cancer
CHIR-99021 purchased from AbMole
bioRxiv. 2021 Jul 1;450516.
Deciphering the tumor-specific immunopeptidome in vivo with genetically engineered mouse models
CHIR-99021 purchased from AbMole
Adv Healthc Mater. 2021 Aug;10(16):e2100821.
Extracellular Matrix Stiffness Regulates DNA Methylation by PKCα-Dependent Nuclear Transport of DNMT3L
CHIR-99021 purchased from AbMole
2020 Sep.
Developing a model to assess the contribution of cytokeratin 19-expressing cells during multipotent stromal cell-induced islet regeneration
CHIR-99021 purchased from AbMole
Stem Cells. 2019 Apr;37(4):516-528.
Human Multipotent Stromal Cell Secreted Effectors Accelerate Islet Regeneration.
CHIR-99021 purchased from AbMole
Cell Experiment | |
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Cell lines | J1 mESCs or F9 mEC cells |
Preparation method | Immunofluorescence staining The expression and subcellular localisation of β-catenin in J1 mESCs treated with 1 μM BIO or 3 μM CHIR for 24 h was detected by immunofluorescence staining. Nuclei were stained with DAPI. J1 mESCs or F9 mEC cells were fixed and permeabilized using immunostaining fixation buffer and then blocked in blocking buffer (Beyotime Institute of Biotechnology). Subsequently, cells were incubated with the indicated primary antibody overnight at 4°C, followed by three washes with washing buffer (Beyotime Institute of Biotechnology) for 5 min and then incubation with an Alexa Fluor 555-conjugated secondary antibody for 2 h at room temperature. Nuclei were stained with DAPI. Cells were photographed under an inverted fluorescence microscope (Nikon, Tokyo, Japan). |
Concentrations | 3µM |
Incubation time | 24h |
Animal Experiment | |
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Animal models | Akita type 1 diabetic mice and wild-type mice |
Formulation | DMSO |
Dosages | 50 mg/kg, daily |
Administration | Intraperitoneal injection |
Molecular Weight | 465.34 |
Formula | C22H18Cl2N8 |
CAS Number | 252917-06-9 |
Solubility (25°C) | DMSO 16 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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