GNE-0877|cas 1374828-69-9|DC Chemicals|Price|Buy

Cas No.:	1374828-69-9
Chemical Name:	DNL201
Synonyms:	DNL201,DNL-201,DNL 201
SMILES:	CC(N1N=C(C)C(NC2=NC=C(C(F)(F)F)C(NC)=N2)=C1)(C)C#N
Formula:	C₁₄H₁₆F₃N₇
M.Wt:	339.326
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM.Invitrogen kinase-selectivity profiling(188 kinases) of aminopyrazole GNE0877 at 0.1 μM (145-fold overLRRK2 Ki) resulted in only four kinases showing greater than 50% inhibition (Aurora B = 51%, RSK2 = 52%, RSK4 = 62%, and RSK3 = 68%) and suggested that GNE0877 is a highly selective LRRK2 inhibitor. Furthermore, GNE0877 possessed a 212-fold biochemical-selectivity index over TTK (Ki= 150 nM), which was previously highlighted as an off-target kinase of concern because of the suggested role of TTK in themaintenance of chromosomal stability. The in vivo rat clearance for inhibitor GNE0877 was within 2-fold of measured in vitro stability, and good oral bioavailability (88%) was achieved at 50 mg/kg following administration of a methylcellulose/tween (MCT) suspension.

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC9496	HG-10-102-01	HG-10-102-01 is a potent and selective inhibitor of wild-type LRRK2(IC50=23.3 nM) and the G2019S mutant(IC50=3.2 nM)
DC11288	PF-06454589	PF-06454589 is a potent and selective LRRK2 inhibitor.
DC7971	PF-06447475	PF-06447475 is a highly potent, selective, brain penetrant LRRK2 inhibitor with IC0 of 3 nM/11 nM for Wt LRRK2/G2019S LRRK2 respectively.
DC8237	LRRK2-IN-1	LRRK2-IN-1 inhibits both wild-type and G2019S mutant LRRK2 kinase activity with IC50 values of 13 nM and 6 nM , respectively with 0.1 mM ATP in the assay.
DC11440	LRRK2 inhibitor 18	LRRK2 inhibitor 18(Compound 18) is a potent azaindazole leucine-rich repeat kinase 2 (LRRK2) inhibitor with Ki of 4.1 nM.
DC8379	JH-II-127	JH-II-127 is a highly potent, selective, and brain penetrant LRRK2 inhibitor.
DC7852	LRRK2 inhibitor GSK2578215A	GSK2578215A is a potent and highly selective LRRK2 inhibitor; exhibits IC50s of around 10 nM against both wild-type LRRK2 and the G2019S mutant.
DC7629	GNE-9605	GNE-9605 is a highly potent and selective Leucine-rich repeat kinase 2 (LRRK2) inhibitor
DC7419	GNE-7915	GNE-7915 is a highly potent, selective, and brain-penetrable LRRK2 small molecule inhibitor with IC50 of 9 nM in cellular LRRK2 assay; > 100 fold selectivity against a panel of 187 kianses(Ki).
DC7418	DNL201	GNE0877 is a highly potent, selective, and brain-penetrant aminopyrazole leucine-rich repeat kinase 2 (LRRK2) small molecule inhibitor with an IC50 of 3 nM.

DNL201