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XL01126

Pricing Availability   Qty
Description: Potent and selective degrader of LRRK2
Chemical Name: (2S,4R)-1-((R)-3-((((1r,4R)-4-((4-(4-((5-Chloro-4-(methyl-λ2-azaneyl)pyrimidin-2-yl)amino)-3-methoxybenzoyl)piperazin-1-yl)methyl)cyclohexyl)methyl)thio)-2-(1-fluorocyclopropane-1-carboxamido)-3-methylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98%
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for XL01126

XL01126 is a fast and potent degrader of LRRK2 in multiple cell lines (DC50 values within 15-72 nM, Dmax values range from 82-90%).

XL01126 exhibits high cell permeability and forms a positively cooperative ternary complex with VHL and LRRK2, which compensates for a substantial loss of binary binding affinities to VHL and LRRK2, underscoring its strong degradation performance in cells.

XL01126 is orally bioavailable (F=15%) and can penetrate the blood brain barrier after either oral or parenteral dosing in mice.

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license

Licensing Information

Sold under licence from the University of Dundee

Technical Data for XL01126

M. Wt 1019.69
Formula C50H64ClFN10O6S2
Storage Store at -20°C
Purity ≥98%
CAS Number 3011029-58-3
PubChem ID 165412689
InChI Key HKSBXNVKPFTBIG-SHFRUIRLSA-N
Smiles O=C(C1(CC1)F)N[C@@H](C(C)(C)SC[C@H]2CC[C@@H](CC2)CN3CCN(CC3)C(C4=CC(OC)=C(C=C4)NC5=NC=C(Cl)C(NC)=N5)=O)C(N6[C@@H](C[C@H](C6)O)C(NCC7=CC=C(C8=C(N=CS8)C)C=C7)=O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for XL01126

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 101.97 100

Preparing Stock Solutions for XL01126

The following data is based on the product molecular weight 1019.69. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.98 mL 4.9 mL 9.81 mL
5 mM 0.2 mL 0.98 mL 1.96 mL
10 mM 0.1 mL 0.49 mL 0.98 mL
50 mM 0.02 mL 0.1 mL 0.2 mL

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References for XL01126

References are publications that support the biological activity of the product.

Liu et al (2022) Discovery of XL01126: a potent, fast, cooperative, selective, orally bioavailable, and blood-brain barrier penetrant PROTAC degrader of leucine-rich repeat kinase 2. JACS 144 16930 PMID: 36007011


If you know of a relevant reference for XL01126, please let us know.

View Related Products by Target

Keywords: XL01126, XL01126 supplier, Degrader, degrades, LRRK2, Parkinson, Disease, PD, neurodegenerative, neuroscience, VHL, TPD, targeted, protein, degradation, cooperative, selective, PROTAC, PROTACS, in, vivo, orally, bioavailable, BBB, penetrant, Other, Degraders, 8968, Tocris Bioscience

Citations for XL01126

Citations are publications that use Tocris products.

Currently there are no citations for XL01126. Do you know of a great paper that uses XL01126 from Tocris? Please let us know.

Reviews for XL01126

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia