2. PROTAC Autophagy
  3. PROTACs LRRK2
  4. XL01126

XL01126 is a potent degrader of LRRK2 with DC50s of 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2), respectively. XL01126 can cross blood-brain barrier and be used as a degrader probe in Parkinson’s disease research. XL01126 exerts function of study of non-catalytic and scaffolding functions of LRRK2.

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XL01126 Chemical Structure

XL01126 Chemical Structure

CAS No. : 3011029-58-3

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Based on 1 publication(s) in Google Scholar

XL01126 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

XL01126 is a potent degrader of LRRK2 with DC50s of 14 nM (G2019S LRRK2) and 32 nM (WT LRRK2), respectively. XL01126 can cross blood-brain barrier and be used as a degrader probe in Parkinson’s disease research. XL01126 exerts function of study of non-catalytic and scaffolding functions of LRRK2[1].

IC50 & Target

DC50: 15-72 nM (LRRK2)[1]
In Vitro

XL01126 (300 nM; 4 h) exhibits strong degradation performance by forming a positively cooperative ternary complex with E3 ubiquitin ligase ligand VHL and target protein LRRK2[1].
XL01126 (10, 30, 100 nM; 24 h) increases mitophagy in immortalized mouse embryonic fibroblasts cells[1].
XL01126 (10 μM; 90 min) displays high permeability in Caco-2 cells[1].
XL01126 (10 μM; 0-60 min; every 15 min interval gradient) exhibits high stability in mouse plasma, liver microsome and hepatocyte[1].
Pharmacokinetic of XL01126 in vitro[1]

Parameter Properties
T1/2 in mouse plasma 108.29 min
T1/2 in mouse liver microsome 3.65 min
Clint in mouse liver microsome 1494.62 mL/min/kg
T1/2 in mose hepatocytes 314.33 min
Clint in mose hepatocytes 26.04 mL/min/kg

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

XL01126 Related Antibodies

Western Blot Analysis[1]

Cell Line: G2019S LRRK2 MEFs (mouse embryonic fibroblasts)
Concentration: 300 nM
Incubation Time: 4 hours
Result: Resulted LRRK2 pSer935, Rab10 pThr73 decrease.
In Vivo

XL01126 (30 mg/kg; p.o.; single dose) shows oral activity with bioavailable value (F) of 15% and can penetrate the blood brain barrier after either oral or parenteral dosing in mice[1].
Pharmacokinetic property of XL01126 in mice[1]

Route Dose
(mg/kg)		 CL
(L/h/kg)		 Vss
(L/kg)		 Tmax
(h)		 Cmax
(ng/mL)		 T1/2
(h)		 AUClast
(h·ng/mL)		 AUCinf
(h·ng/mL)		 MRT
(h)		 F
(%)
p.o. 30 2 3620 21.9 21337 109271 15
i.v. 5 0.208 0.511 1.52 23663 23981 2.45
i.p. 30 0.25 7700 5.2 41434 64068 29.2

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

1019.69

Formula

C50H64ClFN10O6S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(SC[C@@H]3CC[C@@H](CN4CCN(C(C5=CC=C(NC6=NC=C(Cl)C(NC)=N6)C(OC)=C5)=O)CC4)CC3)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (98.07 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9807 mL 4.9035 mL 9.8069 mL
5 mM 0.1961 mL 0.9807 mL 1.9614 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9807 mL 4.9035 mL 9.8069 mL 24.5173 mL
5 mM 0.1961 mL 0.9807 mL 1.9614 mL 4.9035 mL
10 mM 0.0981 mL 0.4903 mL 0.9807 mL 2.4517 mL
15 mM 0.0654 mL 0.3269 mL 0.6538 mL 1.6345 mL
20 mM 0.0490 mL 0.2452 mL 0.4903 mL 1.2259 mL
25 mM 0.0392 mL 0.1961 mL 0.3923 mL 0.9807 mL
30 mM 0.0327 mL 0.1634 mL 0.3269 mL 0.8172 mL
40 mM 0.0245 mL 0.1226 mL 0.2452 mL 0.6129 mL
50 mM 0.0196 mL 0.0981 mL 0.1961 mL 0.4903 mL
60 mM 0.0163 mL 0.0817 mL 0.1634 mL 0.4086 mL
80 mM 0.0123 mL 0.0613 mL 0.1226 mL 0.3065 mL
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XL01126 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

XL011263011029-58-3XL 01126XL-01126PROTACsLRRK2Leucine-rich repeat kinase 2Type 1 kinaseproteolysisblood-brain barrierVHLpermeabilityCaco-2 cellInhibitorinhibitorinhibit

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