Leupeptin hemisulfate

Name: Leupeptin hemisulfate
Brand: MedChemExpress
SKU: HY-18234A
Rating: 5.0 (61 reviews)

Cat. No.: HY-18234A Purity: 99.39%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Leupeptin hemisulfate is a broad-spectrum, membrane-permeable protease inhibitor. Leupeptin hemisulfate potently inhibits serine, cysteine and threonine proteases. Leupeptin hemisulfate inhibits M^pro (the main protease of SARS-CoV-2) and also has anti-inflammatory activity.

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

CAS No. : 103476-89-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 61 publication(s) in Google Scholar

Other Forms of Leupeptin hemisulfate:

Leupeptin Ac-LL hydrochloride In-stock
Leupeptin Ac-LL Get quote
Leupeptin Get quote
Leupeptin hemisulfate (Standard) Get quote

61 Publications Citing Use of MCE Leupeptin hemisulfate

: Leupeptin hemisulfate purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2024 Sep 2;17(1):78. [Abstract]; The LTF expression was detected under MG132 (10 μM) or Leupeptin (100 μM) treatment.

: Leupeptin hemisulfate purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Feb;21(2):352-373. [Abstract]; Immunoblotting showing the level of PLCG1 in NPC after treatment with Leu (10 μM), NH4Cl (20 mM), or their combination for 12 h. Right panels represent normalized (/NC) band intensities of interest.

: Leupeptin hemisulfate purchased from MedChemExpress. Usage Cited in: Autophagy. 2025 Feb;21(2):352-373. [Abstract]; Western blot showing PLCG1 levels in NPC treated with a combination of Leu (10 μM) and NH4Cl (N/L) for 3, 6, and 9 h. Right panels represent normalized (/NC) band intensities of interest.

: Leupeptin hemisulfate purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2023 Jan;30(1):137-151. [Abstract]; Western blot analysis of SLC7A11, SOCS2 and tubulin proteins in SK-Hep-1 and HepG2 cells at 4 h after 4 Gy IR. Leupeptin (50 μM) were added before IR.

: Leupeptin hemisulfate purchased from MedChemExpress. Usage Cited in: Autophagy. 2021 Aug;17(8):1873-1888. [Abstract]; 661 W cells were transfected with the indicated siRNA for 24 h. Then, 661 W cells were treated with 10 μg/ml Leupeptin for 24 h. Cell lysates were collected for western blot analysis of LC3B and GAPDH.

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Cathepsin B, Cathepsin H, Cathepsin L, Ser/Thr Protease, Mpro^[1]^[2]^[3].

In Vitro

Leupeptin hemisulfate (0.06-200 µM; 72 h) significantly decreases copy numbers of SARS-CoV-2 viral RNA (vRNA) in Vero cells^[1]
Leupeptin hemisulfate inhibits RNA levels of SARS-CoV-2 in Vero cells, with an EC₅₀ value of 42.34 µM^[1].
Leupeptin hemisulfate has some inhibitory activity against M^pro, with an IC₅₀ value of 127.2 µM^[1].
Leupeptin hemisulfate againsts human coronavirus strain 229E with an IC₅₀ value of 0.4 µg/mL (about 1 µM)^[1].

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

RT-PCR^[1]

Cell Line:	Vero cells
Concentration:	0.06-200 µM
Incubation Time:	72 h
Result:	Significantly decreased copy numbers of SARS-CoV-2 viral RNA (vRNA).

In Vivo

Leupeptin hemisulfate (0, 9, 18, 36 mg/kg; i.p.; single) is well tolerated by the animals and produces a strong, dose-dependent increase in LC3b-II in both the total tissue extracts and the lysosome and autophagosome-enriched pellet fraction^[2].

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

Animal Model:	C57BL/6NCrl male mice (6-8 weeks old, 20-25 g)^[1]
Dosage:	0, 9, 18, 36 mg/kg
Administration:	Intraperitoneal injection; single
Result:	Promoted the accumulation of LC3b-II in mouse liver.

Molecular Weight

475.59

Formula

C₂₀H₃₈N₆O₄.1/2H₂SO₄

CAS No.

103476-89-7

Appearance

Solid

Color

White to off-white

Sequence Shortening

Ac-LLR-CHO

SMILES

O=C[C@@H](NC([C@@H](NC([C@@H](NC(C)=O)CC(C)C)=O)CC(C)C)=O)CCCNC(N)=N.[0.5H2SO4]

Structure Classification

Others

Initial Source

Microorganisms

Microbial Metabolite

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H₂O : 70 mg/mL (147.19 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1027 mL	10.5133 mL	21.0265 mL
5 mM	0.4205 mL	2.1027 mL	4.2053 mL
10 mM	0.2103 mL	1.0513 mL	2.1027 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 100 mg/mL (210.27 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.39%

Select Batch:

Data Sheet (276 KB) SDS (394 KB)

COA (250 KB) HNMR (272 KB) RP-HPLC (250 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo). 1969 Nov;22(11):558-68. [Content Brief]

[2]. Fu L, et al. Mechanism of Microbial Metabolite Leupeptin in the Treatment of COVID-19 by Traditional Chinese Medicine Herbs. mBio. 2021 Oct 26;12(5):e0222021. [Content Brief]

[3]. Haspel J, et al. Characterization of macroautophagic flux in vivo using a leupeptin-based assay. Autophagy. 2011 Jun;7(6):629-42. [Content Brief]

[4]. Aoyagi T, et al. Biological activities of leupeptins. J Antibiot (Tokyo). 1969 Nov;22(11):558-68.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	2.1027 mL	10.5133 mL	21.0265 mL	52.5663 mL
	5 mM	0.4205 mL	2.1027 mL	4.2053 mL	10.5133 mL
	10 mM	0.2103 mL	1.0513 mL	2.1027 mL	5.2566 mL
	15 mM	0.1402 mL	0.7009 mL	1.4018 mL	3.5044 mL
	20 mM	0.1051 mL	0.5257 mL	1.0513 mL	2.6283 mL
	25 mM	0.0841 mL	0.4205 mL	0.8411 mL	2.1027 mL
	30 mM	0.0701 mL	0.3504 mL	0.7009 mL	1.7522 mL
	40 mM	0.0526 mL	0.2628 mL	0.5257 mL	1.3142 mL
	50 mM	0.0421 mL	0.2103 mL	0.4205 mL	1.0513 mL
	60 mM	0.0350 mL	0.1752 mL	0.3504 mL	0.8761 mL
	80 mM	0.0263 mL	0.1314 mL	0.2628 mL	0.6571 mL
	100 mM	0.0210 mL	0.1051 mL	0.2103 mL	0.5257 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.