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Submit ReviewXL01126 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
Sold under licence from the University of Dundee
| 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.
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 101.97 | 100 |
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.
| 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 |
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.
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
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:
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