1. Autophagy
  2. LRRK2

GNE-7915 

Cat. No.: HY-18163 Purity: 98.77%
Data Sheet SDS Handling Instructions

GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.

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GNE-7915 Chemical Structure

GNE-7915 Chemical Structure

CAS No. : 1351761-44-8

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $112 In-stock
10 mg $102 In-stock
50 mg $340 In-stock
100 mg $500 In-stock
200 mg $800 In-stock
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Description

GNE-7915 is a potent, selective and brain-penetrant inhibitor of LRRK2 with an IC50 of 9 nM.

IC50 & Target

IC50: 9 nM[1] (LRRK2)

In Vitro

Maintaining the methoxy/fluoro arrangement at C-2′/C-5′ and varying aminoalkyl R1 substitution resultes in single-digit nanomolar LRRK2 cellular activities for GNE-7915 and compound 19. Expanded Invitrogen kinase profiling (187 kinases) at 0.1 μM for both GNE-7915 (100-fold over LRRK2 Ki) and 19 (250-fold over LRRK2 Ki) resultes in only TTK showing greater than 50% inhibition. Selectivity profiling using the DiscoverX KinomeScan55 competitive binding assay panel, which includes 392 unique kinases, is also performed for GNE-7915 at 0.1 μM. Binding of >50% probe displacement is detected for 10 kinases and of >65% for only LRRK2, TTK, and ALK, further supporting the excellent LRRK2 selectivity for GNE-7915. Cerep receptor profiling, including expanded brain panels, suggestes that GNE-7915 and 19 only inhibite 5-HT2B with >70% inhibition at 10 μM. GNE-7915 and 19 are confirmed to be moderately potent 5-HT2B antagonists in vitro functional assays[2].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.2553 mL 11.2765 mL 22.5530 mL
5 mM 0.4511 mL 2.2553 mL 4.5106 mL
10 mM 0.2255 mL 1.1277 mL 2.2553 mL
Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

443.4

Formula

C₁₉H₂₁F₄N₅O₃

CAS No.

1351761-44-8

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 14.33 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.77%

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GNE-7915
Cat. No.:
HY-18163
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