Molecular Formula | C22H25ClN6O4S |
Molar Mass | 504.99 |
Density | 1.452±0.06 g/cm3(Predicted) |
Boling Point | 718.1±70.0 °C(Predicted) |
Solubility | DMSO: 21 mg/mL |
pKa | 8.50±0.10(Predicted) |
Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
In vitro study | CZC-54252 inhibits the activity of recombinant human wild-type LRRK2 with an IC 50 ranging from ~1 to ~5 nM. The G2019S mutant is inhibited with an IC 50 ranging from ~2 to ~7 nM in a TF-FRET assay. In addition, they are screened against a kinase panel of 185 kinases and exhibited good selectivity. G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 with an EC 50 of ~1 nM and fully reversed to wild-type levels by CZC-54252 at concentration of 1.6 nM. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.98 ml | 9.901 ml | 19.802 ml |
5 mM | 0.396 ml | 1.98 ml | 3.96 ml |
10 mM | 0.198 ml | 0.99 ml | 1.98 ml |
5 mM | 0.04 ml | 0.198 ml | 0.396 ml |
biological activity | CZC-54252 is an effective LRRK2 inhibitor with IC50 of 1.28 nM and 1.85 nM for human wild type LRRK2 and G2019S LRRK2 respectively. |
target | TargetValue LRRK2 (WT) (Cell-free say) 1.28 nM LRRK2 (G2019S) (Cell-free say) 1.85 nM |
Target | Value |
LRRK2 (WT) (Cell-free assay) | 1.28 nM |
LRRK2 (G2019S) (Cell-free assay) | 1.85 nM |
in vitro study | CZC-54252 inhibits the activity of recombinant human wild-type LRRK2 with an IC 50 ranging from ~ 1 to ~ 5 nM. The G2019S mutant is inhibited with an IC 50 ranging from ~ 2 to ~ 7 nM in a TF-FRET say. In addition, they are screened against a kinase panel of 185 kinases and exhibited good selectivity. G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 with an EC 50 of ~ 1 nM and fully reversed to wild-type levels by CZC-54252 at concentration of 1.6 nM. |