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RN277

Chemical Structure : RN277

CAS No.:

RN277 (RN-277)

Catalog No.: PC-24723Not For Human Use, Lab Use Only.

RN277 is a potent, selective, type II kinase inhibitor of LRRK2 with IC50 of 135 nM, binds to the kinase domain of LRRK2.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

RN277 is a potent, selective, type II kinase inhibitor of LRRK2 with IC50 of 135 nM, binds to the kinase domain of LRRK2.
RN277 display a strong inhibitory effect on LRRK1 kinase activity.
RN277 inhibits LRRK2RCKW-mediated phosphorylation of Rab8a in vitro with IC50 of 70 nM.
RN277 inhibits phosphorylation of LRRK2 substrate Rabs (such as Rab8a) without affecting the phosphorylation of LRRK2 biomarker site S935.
RN277 inhibits phosphorylation of Rab8a by both the wild-type LRRK2 and mutant kinase G2019S LRRK2.
RN277 rescues kinesin motility in the presence of LRRK2 RCKW in in vitro motility assay.

Physicochemical Properties

M.Wt 585.11
Formula C31H33ClN8O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(3-(tert-butyl)-1-(p-tolyl)-1H-pyrazol-5-yl)-3-(3-(2-chloro-4-morpholino-7H-pyrrolo[2,3-d]pyrimidin-5-yl)phenyl)urea

References

1. Raig ND, et al. Sci Adv. 2025 Jun 6;11(23):eadt2050.

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