Leelamine

Name: Leelamine
Brand: MedChemExpress
SKU: HY-W005629
Rating: 4.5 (1 reviews)

Cat. No.: HY-W005629 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

Leelamine Chemical Structure

CAS No. : 1446-61-3

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500 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

Other Forms of Leelamine:

Leelamine hydrochloride Get quote

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CB1 CB2

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CB1

CB2

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	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]
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]
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	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	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	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	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]
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]
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 measured after 36 hrs by MTT assay Cytotoxicity against HUVEC measured after 36 hrs by MTT assay	[PMID: 30746067]
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]
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	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]
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	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]
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.

Molecular Weight

285.47

Formula

C₂₀H₃₁N

CAS No.

1446-61-3

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
10 mM	0.3503 mL	1.7515 mL	3.5030 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.76 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:

Dosage

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

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

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

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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Leelamine

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Other Forms of Leelamine:

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Leelamine Related Antibodies

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Complete Stock Solution Preparation Table

Leelamine Related Classifications

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