2. Neuronal Signaling Cell Cycle/DNA Damage
  3. Dopamine Transporter CDK
  4. LH2-051

LH2-051, a lysosome-enhancing compound (LYEC), is a brain-penetrant dopamine transporter (DAT) inhibitor (Ki: 0.95 μM). LH2-051 inhibits DAT-mediated dopamine uptake with an IC50 of 3.0 μM. LH2-051 promotes nuclear translocation of TFEB and lysosome biogenesis. LH2-051 improves the memory of amyloid precursor protein (APP)/Presenilin 1 (PS1) mice. LH2-051 can be used for the study of Alzheimer’s disease.

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LH2-051

LH2-051 Chemical Structure

CAS No. : 2358754-22-8

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Based on 1 publication(s) in Google Scholar

LH2-051 Related Antibodies

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Description

LH2-051, a lysosome-enhancing compound (LYEC), is a brain-penetrant dopamine transporter (DAT) inhibitor (Ki: 0.95 μM). LH2-051 inhibits DAT-mediated dopamine uptake with an IC50 of 3.0 μM. LH2-051 promotes nuclear translocation of TFEB and lysosome biogenesis. LH2-051 improves the memory of amyloid precursor protein (APP)/Presenilin 1 (PS1) mice. LH2-051 can be used for the study of Alzheimer’s disease[1].

In Vitro

LH2-051 (3-50 μM, 3-12 h) promotes nuclear translocation of TFEB which is independent of inactivation of mTORC1 or GSK3β[1].
LH2-051 (10-4-10-1 μM) binds directly to DAT (Ki = 0.95 μM) and inhibits DAT-mediated dopamine uptake with an IC50 of 3.0 μM in HEK293 cells[1].
LH2-051 (30 μM, 0-6 h) promotes lysosome biogenesis in HeLa cells and SH-SY5Y cells, which is regulated by CDK9-mediated phosphorylation of TFEB[1].
LH2-051 (30 μM, 3 h) induces the translocation of DAT from the plasma membrane onto lysosomal membranes in SH-SY5Y cells[1].

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

LH2-051 Related Antibodies

Immunofluorescence[1]

Cell Line: HeLa cells and SH-SY5Y cells
Concentration: 3, 5, 10, 30, 50 μM
Incubation Time: 3, 6 h
Result: Promoted the nuclear translocation of TFEB-EGFP in a dose- and time-dependent manner.
Enhanced the staining and protein level of endogenous lysosomal-associated membrane protein 1 (LAMP1).
Enhanced the staining of Boron dipyrromethene difluoride (BODIPY) pepstatin A, which binds to active cathepsin D inside lysosomes.
Promoted translocation of endogenous DAT to lysosomes, and release of both endogenous CDK9 and endogenous TFEB from lysosomes.

Western Blot Analysis[1]

Cell Line: HeLa cells
Concentration: 30 μM
Incubation Time: 6 h
Result: Induced translocation of endogenous TFEB from the cytosol into the nucleus.
Did not inhibit mTORC1 activity.
Did not significantly affect GSK3β phosphorylation at Ser9.

Real Time qPCR[1]

Cell Line: HeLa cells and TFEB KO cells
Concentration: 30 μM
Incubation Time: 12 h
Result: Increased the expression of lysosomal and autophagic genes which was dependent on TFEB. protein 1 (LAMP1).
Enhanced the staining of Boron dipyrromethene difluoride (BODIPY) pepstatin A, which binds to active cathepsin D inside lysosomes.
Promoted translocation of endogenous DAT to lysosomes, and release of both endogenous CDK9 and endogenous TFEB from lysosomes.

Western Blot Analysis[1]

Cell Line: SH-SY5Y cells
Concentration: 30 μM
Incubation Time: 1, 2, 3, 6 h
Result: Reduced the phosphorylation of Rpb1.
In Vivo

LH2-051 (10 mg/kg, i.p., once daily, 30 days) alleviates AD-like symptoms in APP/PS1 mice[1].

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

Animal Model: Five-month-old APP/PS1 mice (male)[1]
Dosage: 10 mg/kg
Administration: i.p. once daily for 30 days
Result: Reduced Aβ load by 63.2% in the cortex and 65.6% in hippocampus compared with age-matched vehicle-injected controls.
Upregulated the expression of lysosomal and autophagic genes in APP/PS1 mouse brains.
Took significantly less time to locate the hidden platform and landed on the platform more often when compared to vehicle-injected controls during the training trial.
Enhanced lysosome biogenesis and Aβ clearance in APP/PS1 mice, and improved their learning, memory, and cognitive function.
Molecular Weight

434.57

Formula

C27H34N2O3
CAS No.
Appearance

Solid

Color

Off-white to light brown

SMILES

COC1=C(OC)C=C(C(CCC2=CNC3=C2C=CC=C3)N(CC4CCOCC4)CC5)C5=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (230.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3011 mL 11.5056 mL 23.0113 mL
5 mM 0.4602 mL 2.3011 mL 4.6023 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Please enter your animal formula composition:
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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 (stored under nitrogen). 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 2.3011 mL 11.5056 mL 23.0113 mL 57.5281 mL
5 mM 0.4602 mL 2.3011 mL 4.6023 mL 11.5056 mL
10 mM 0.2301 mL 1.1506 mL 2.3011 mL 5.7528 mL
15 mM 0.1534 mL 0.7670 mL 1.5341 mL 3.8352 mL
20 mM 0.1151 mL 0.5753 mL 1.1506 mL 2.8764 mL
25 mM 0.0920 mL 0.4602 mL 0.9205 mL 2.3011 mL
30 mM 0.0767 mL 0.3835 mL 0.7670 mL 1.9176 mL
40 mM 0.0575 mL 0.2876 mL 0.5753 mL 1.4382 mL
50 mM 0.0460 mL 0.2301 mL 0.4602 mL 1.1506 mL
60 mM 0.0384 mL 0.1918 mL 0.3835 mL 0.9588 mL
80 mM 0.0288 mL 0.1438 mL 0.2876 mL 0.7191 mL
100 mM 0.0230 mL 0.1151 mL 0.2301 mL 0.5753 mL
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LH2-051 Related Classifications

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  • 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:

LH2-0512358754-22-8Dopamine TransporterCDKDATSLC6A3Cyclin dependent kinaseAlzheimer’s diseaseCDK9dopamine transporterlysosome biogenesisTFEBInhibitorinhibitorinhibit

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