Art. -Nr.: HY-W005629

Leelamine

Name: Leelamine
Brand: MedChemExpress
SKU: HY-W005629
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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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Reinheit : 95.69%
CAS. Nr.: 1446-61-3
Formel: C₂₀H₃₁N
Molecular Weight:285.48

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Leelamine Chemical Structure

CAS. Nr.: 1446-61-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

CB1

CB2

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Cellular Effect

Cell Line	Type	Value	Description	References
5637	IC₅₀	8.7 μM Compound: 3	Cytotoxicity against human 5637 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human 5637 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707051]
A2780	EC₅₀	3.8 μM Compound: Dehydroabietylamine	Cytotoxicity against human A2780 cells after 96 hrs by sulforhodamine-B assay Cytotoxicity against human A2780 cells after 96 hrs by sulforhodamine-B assay	[PMID: 30056282]
A549	IC₅₀	5.02 μM Compound: L0	Antiproliferative activity against human A549 cells after 36 hrs by MTT assay Antiproliferative activity against human A549 cells after 36 hrs by MTT assay	[PMID: 29407970]
A549	IC₅₀	5.02 μM Compound: L0	Antineoplastic activity against human A549 cells measured after 36 hrs by MTT assay Antineoplastic activity against human A549 cells measured after 36 hrs by MTT assay	[PMID: 30746067]
EJ	IC₅₀	4.82 μM Compound: 3	Cytotoxicity against human EJ cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human EJ cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707051]
FaDu	EC₅₀	3.9 μM Compound: Dehydroabietylamine	Cytotoxicity against human FADU cells after 96 hrs by sulforhodamine-B assay Cytotoxicity against human FADU cells after 96 hrs by sulforhodamine-B assay	[PMID: 30056282]
HeLa	IC₅₀	2.02 μM Compound: L0	Antiproliferative activity against human HeLa cells after 36 hrs by MTT assay Antiproliferative activity against human HeLa cells after 36 hrs by MTT assay	[PMID: 29407970]
HeLa	IC₅₀	2.02 μM Compound: L0	Antineoplastic activity against human HeLa cells measured after 36 hrs by MTT assay Antineoplastic activity against human HeLa cells measured after 36 hrs by MTT assay	[PMID: 30746067]
HeLa	IC₅₀	7.68 μM Compound: 3	Cytotoxicity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707051]
HepG2	IC₅₀	2.56 μM Compound: L0	Antiproliferative activity against human HepG2 cells after 36 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 36 hrs by MTT assay	[PMID: 29407970]
HepG2	IC₅₀	2.56 μM Compound: L0	Antineoplastic activity against human HepG2 cells measured after 36 hrs by MTT assay Antineoplastic activity against human HepG2 cells measured after 36 hrs by MTT assay	[PMID: 30746067]
HT-29	EC₅₀	2.1 μM Compound: Dehydroabietylamine	Cytotoxicity against human HT-29 cells after 96 hrs by sulforhodamine-B assay Cytotoxicity against human HT-29 cells after 96 hrs by sulforhodamine-B assay	[PMID: 30056282]
HUVEC	IC₅₀	1.27 μM Compound: L0	Cytotoxicity against HUVEC assessed as reduction in cell viability after 36 hrs by MTT assay Cytotoxicity against HUVEC assessed as reduction in cell viability after 36 hrs by MTT assay	[PMID: 29407970]
HUVEC	IC₅₀	1.27 μM Compound: L0	Cytotoxicity against HUVEC measured after 36 hrs by MTT assay Cytotoxicity against HUVEC measured after 36 hrs by MTT assay	[PMID: 30746067]
J774	CC₅₀	14.5 μM Compound: 6	Cytotoxicity against mouse J774 cells assessed as reduction of cell viability after 48 hrs by resazurin dye-based fluorometric method Cytotoxicity against mouse J774 cells assessed as reduction of cell viability after 48 hrs by resazurin dye-based fluorometric method	[PMID: 27318121]
Jurkat	IC₅₀	4.85 μM Compound: 3	Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human Jurkat cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707051]
L6	IC₅₀	6.5 μM Compound: 1; TCI D1588	Cytotoxicity against rat L6 cells after 72 hrs by AlamarBlue dye based fluorimetric method Cytotoxicity against rat L6 cells after 72 hrs by AlamarBlue dye based fluorimetric method	[PMID: 26849852]
L6	IC₅₀	7.4 μM Compound: 1; TCI D1588	Antitrypanosomal activity against trypomastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ gene infected in rat L6 cells after 96 hrs by photometric method Antitrypanosomal activity against trypomastigote form of Trypanosoma cruzi Tulahuen C2C4 expressing LacZ gene infected in rat L6 cells after 96 hrs by photometric method	[PMID: 26849852]
MCF7	EC₅₀	3 μM Compound: Dehydroabietylamine	Cytotoxicity against human MCF7 cells after 96 hrs by sulforhodamine-B assay Cytotoxicity against human MCF7 cells after 96 hrs by sulforhodamine-B assay	[PMID: 30056282]
MCF7	IC₅₀	19.45 μM Compound: L0	Antiproliferative activity against human MCF7 cells after 36 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 36 hrs by MTT assay	[PMID: 29407970]
MCF7	IC₅₀	19.45 μM Compound: L0	Antineoplastic activity against human MCF7 cells measured after 36 hrs by MTT assay Antineoplastic activity against human MCF7 cells measured after 36 hrs by MTT assay	[PMID: 30746067]
NIH3T3	EC₅₀	2.4 μM Compound: Dehydroabietylamine	Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by sulforhodamine-B assay Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by sulforhodamine-B assay	[PMID: 30056282]
PC-3	IC₅₀	7.88 μM Compound: 3	Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23707051]
SW-1736	EC₅₀	4.2 μM Compound: Dehydroabietylamine	Cytotoxicity against human SW1736 cells after 96 hrs by sulforhodamine-B assay Cytotoxicity against human SW1736 cells after 96 hrs by sulforhodamine-B assay	[PMID: 30056282]

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.

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.

Related Protocols :

Chemical Information

CAS. Nr. 1446-61-3
Appearance <44.5°C Solid,>44.5°C Liquid
Molecular Weight 285.48
Formel C₂₀H₃₁N
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (350.29 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.5029 mL

17.5144 mL

35.0287 mL

5 mM

0.7006 mL

3.5029 mL

7.0057 mL

10 mM

0.3503 mL

1.7514 mL

3.5029 mL

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 5 mg/mL (17.51 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 5 mg/mL (17.51 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 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 (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 5 mg/mL (17.51 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Merarchi M, et, al. A Brief Overview of the Antitumoral Actions of Leelamine. Biomedicines. 2019 Jul 19;7(3):53. [Content Brief]

[2]. Kuzu OF, Gowda R, Sharma A, Robertson GP. Leelamine mediates cancer cell death through inhibition of intracellular cholesterol transport. Mol Cancer Ther. 2014;13(7):1690-1703. [Content Brief]

[3]. Aicher TD, et al. Triterpene and diterpene inhibitors of pyruvate dehydrogenase kinase (PDK). Bioorg Med Chem Lett. 1999 Aug 2;9(15):2223-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.5029 mL	17.5144 mL	35.0287 mL	87.5718 mL
	5 mM	0.7006 mL	3.5029 mL	7.0057 mL	17.5144 mL
	10 mM	0.3503 mL	1.7514 mL	3.5029 mL	8.7572 mL
	15 mM	0.2335 mL	1.1676 mL	2.3352 mL	5.8381 mL
	20 mM	0.1751 mL	0.8757 mL	1.7514 mL	4.3786 mL
	25 mM	0.1401 mL	0.7006 mL	1.4011 mL	3.5029 mL
	30 mM	0.1168 mL	0.5838 mL	1.1676 mL	2.9191 mL
	40 mM	0.0876 mL	0.4379 mL	0.8757 mL	2.1893 mL
	50 mM	0.0701 mL	0.3503 mL	0.7006 mL	1.7514 mL
	60 mM	0.0584 mL	0.2919 mL	0.5838 mL	1.4595 mL
	80 mM	0.0438 mL	0.2189 mL	0.4379 mL	1.0946 mL
	100 mM	0.0350 mL	0.1751 mL	0.3503 mL	0.8757 mL

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Leelamine

Alle Cannabinoid Receptor Isoform-spezifische Produkte anzeigen