2. GPCR/G Protein Neuronal Signaling PI3K/Akt/mTOR
  3. Cannabinoid Receptor PDK-1
  4. Leelamine

Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC50 value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells.

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Leelamine Chemical Structure

Leelamine Chemical Structure

CAS No. : 1446-61-3

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Customer Review

Based on 1 publication(s) in Google Scholar

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Leelamine Related Antibodies

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Description

Leelamine is an orally active pyruvate dehydrogenase kinase (PDK) inhibitor with an IC50 value of 9.5 μM, showing a blood glucose lowering effect in the diabetic mouse. Leelamine is also a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine decreases mitotic activity, prostate-specific antigen expression and induces Apoptosis to cell death in cancer cells[1][2][3].

IC50 & Target[1]

CB1

 

CB2

 

In Vitro

Leelamine (3 μM, 3 h) induces vacuolization of cells, accumulation of lipofuscin-like material, formation of web-like membrane whorls and inhibition of autophagic flux in melanoma cells[2].
Leelamine (3 μM, 3 h) induces intracellular cholesterol accumulation and alters cholesterol subcellular localization in UACC 903 or 1205 Lu melanoma cells[2].
Leelamine (3-5 μM, 3-12 h) inhibits signaling pathways driving melanoma cell survival and disrupts RTK signaling via interference with intracellular vesicular transport systems[2].

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

Leelamine Related Antibodies

Western Blot Analysis[2]

Cell Line: Melanoma cells
Concentration: 3-5 μM
Incubation Time: 3-12 h
Result: Significantly decreased phosphorylation of EIF4EBP1 (4E-BP1) and inhibited AKT/mTOR branch of the cascade in melanoma cells.

Immunofluorescence[2]

Cell Line: UACC 903 melanoma cells
Concentration: 3 μM
Incubation Time: 3 h
Result: Induced vacuolization of UACC 903 melanoma cells and autophagosome accumulation, followed by membrane blebbing, cell shrinkage and cell rounding.
Molecular Weight

285.47

Formula

C20H31N
CAS No.
Appearance

<44.5°C Solid,>44.5°C Liquid

Color

Colorless to light yellow

SMILES

NC[C@]1(C)CCC[C@]2(C)C3=C(CC[C@@]12[H])C=C(C(C)C)C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (350.30 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 3.5030 mL 17.5150 mL 35.0299 mL
5 mM 0.7006 mL 3.5030 mL 7.0060 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 (protect from light). 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (8.76 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% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (8.76 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
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 (protect from light)

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

Purity: 98.36%

COA (247 KB) HNMR (124 KB) RP-HPLC (191 KB)

Handling Instructions (2659 KB)
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 (protect from light). 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 3.5030 mL 17.5150 mL 35.0300 mL 87.5749 mL
5 mM 0.7006 mL 3.5030 mL 7.0060 mL 17.5150 mL
10 mM 0.3503 mL 1.7515 mL 3.5030 mL 8.7575 mL
15 mM 0.2335 mL 1.1677 mL 2.3353 mL 5.8383 mL
20 mM 0.1751 mL 0.8757 mL 1.7515 mL 4.3787 mL
25 mM 0.1401 mL 0.7006 mL 1.4012 mL 3.5030 mL
30 mM 0.1168 mL 0.5838 mL 1.1677 mL 2.9192 mL
40 mM 0.0876 mL 0.4379 mL 0.8757 mL 2.1894 mL
50 mM 0.0701 mL 0.3503 mL 0.7006 mL 1.7515 mL
60 mM 0.0584 mL 0.2919 mL 0.5838 mL 1.4596 mL
80 mM 0.0438 mL 0.2189 mL 0.4379 mL 1.0947 mL
100 mM 0.0350 mL 0.1751 mL 0.3503 mL 0.8757 mL
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Leelamine 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:

Leelamine1446-61-3Cannabinoid ReceptorPDK-13-Phosphoinositide-dependent protein kinase 1orally activePDKblood glucose loweringdiabetic mousecannabinoid receptorscancer cellsInhibitorinhibitorinhibit

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