| Bioactivity | CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. CZC-54252 attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of ~1 nM. CZC-54252 has a neuroprotective activity[1]. | ||||||||||||
| Target | IC50: 1.28 nM (Wild-type LRRK2) and 1.85 nM (G2019S LRRK2) | ||||||||||||
| Invitro | CZC-54252 inhibits the activity of recombinant human wild-type LRRK2 with an IC50 ranging from ～1 to ～5 nM. The G2019S mutant is inhibited with an IC50 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[1]. G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 with an EC50 of ~1 nM and fully reversed to wild-type levels by CZC-54252 at concentration of 1.6 nM[1]. | ||||||||||||
| Name | CZC-54252 | ||||||||||||
| CAS | 1191911-27-9 | ||||||||||||
| Formula | C22H25ClN6O4S | ||||||||||||
| Molar Mass | 504.99 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
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| Reference | [1]. Ramsden N, et al. Chemoproteomics-based design of potent LRRK2-selective lead compounds that attenuate Parkinson's disease-related toxicity in human neurons. ACS Chem Biol. 2011 Oct 21;6(10):1021-8. |
CZC-54252
CAS: 1191911-27-9 F: C22H25ClN6O4S W: 504.99
CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, re
Data collection：peptidedb@qq.com
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