Biological Activity
CHIR-99021 (CT99021) is a GSK-3 inhibitor used in signaling, cell-state and metabolic research. The inhibitor series blocked human GSK-3, a negative regulator of glycogen synthase and insulin signaling.
In Vitro
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| Target mechanism | Original substituted aminopyrimidine GSK-3 inhibitor study. [1] | The inhibitor series blocked human GSK-3, a negative regulator of glycogen synthase and insulin signaling. |
| Cellular glycogen synthesis | Insulin-receptor-expressing CHO cells and primary rat hepatocytes. [1], abstract | The study series activated glycogen synthase. Compound-specific potency and exposure for CHIR-99021 are not resolved by the abstract. |
| Tissue response | Isolated skeletal muscle from insulin-resistant ZDF and lean Zucker rats. [1], abstract | The inhibitor series enhanced insulin-stimulated glucose transport in resistant ZDF tissue but not insulin-sensitive lean controls. |
In Vivo
No compound-specific animal efficacy result is established by the sources summarized here.
Compound and Evidence Context
| Endpoint | Model / conditions / source | Reported result |
|---|---|---|
| Compound-specific attribution | Multiple inhibitors were examined in the same publication. [1] | Series-level Ki values, cellular concentration ranges and animal doses are not assigned to CHIR-99021 without its corresponding data table. |
Interpretation
The cited study examines multiple inhibitors. Series-level animal doses and potency ranges are not assigned here to CHIR-99021 alone.
