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L-Leucyl-L-Leucine methyl ester

Name: L-Leucyl-L-Leucine methyl ester
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(Synonyms: LLOMe; Leu-Leu methyl ester; H-Leu-Leu-OMe)

23 Cited Publications

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Based on 23 publication(s) in Google Scholar

L-Leucyl-L-Leucine methyl ester (LLOMe; Leu-Leu methyl ester; H-Leu-Leu-OMe) is a lysosomal disrupting agent and apoptosis inducer that, through receptor-mediated endocytosis and lysosomal dipeptidyl peptidase I conversion, induces caspase activation, lysosomal membrane permeabilization, and DNA fragmentation, and requires cathepsin C to exert membrane-lytic activity, thereby selectively killing natural killer cells. L-Leucyl-L-Leucine methyl ester can be used for research related to lysosomal function and apoptosis.

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

CAS No.: 13022-42-9
Formula: C₁₃H₂₆N₂O₃
Molecular Weight:258.36

Storage:

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

Data Sheet (290 KB)

L-Leucyl-L-Leucine methyl ester Chemical Structure

CAS No.: 13022-42-9

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
Chemical Information
Publications (23)
Purity & Documentation
References
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Classifications
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Biological Activity

Description

All Caspase Isoforms :

In Vitro

Anti-cancerApoptosisInnate ImmunityLysosomal MetabolismProtein/Amino Acid Metabolism

Anti-cancer

L-Leucyl-L-Leucine methyl ester (200-500 µM; 4 h at 37°C) induces DNA fragmentation in HL-60 cells^[1].
L-Leucyl-L-Leucine methyl ester (1-7 mM; 18 h) induces HeLa cell death only at concentrations above 4 mM after 18 h of continuous exposure^[2].
L-Leucyl-L-Leucine methyl ester (0.5-7 mM; 5 min-1 h) causes rapid concentration- and time-dependent loss of catB/L activity in HeLa cells without releasing active cathepsins into the cytosol^[2].
L-Leucyl-L-Leucine methyl ester (1-5 mM; 15 min-1 h) reduces mature catB, catL, and catC protein levels in HeLa cells within 15 min^[2].
L-Leucyl-L-Leucine methyl ester (1 mM; up to 48 h) enables HeLa cells to reacquire catB/L activity through de novo protein synthesis between 12 and 24 h^[2].

Apoptosis

L-Leucyl-L-Leucine methyl ester (LLOMe; Leu-Leu methyl ester; H-Leu-Leu-OMe) (150-200 µM; 20 min-1 h) induces concentration-dependent apoptosis in HL-60 cells (maximal at 150 µM)^[1].
L-Leucyl-L-Leucine methyl ester (1-4 h) activates caspase-3-like proteases in HL-60 cells from 1 h onward, reaching a specific activity of 611 pmole AMC/min/mg protein at 4 h (approximately 10 times the control of 57 pmole AMC/min/mg protein)^[1].
L-Leucyl-L-Leucine methyl ester (5 mM; 3-10 h) activates caspase-3-like activity in HeLa cells at 3 h, with maximal activity at 10 h^[2].

Innate Immunity

Lysosomal Metabolism

L-Leucyl-L-Leucine methyl ester (> 50 μM; 15 min at room temperature) irreversibly eliminates all NK function of human Mφ-depleted lymphocytes, accompanied by loss of K562 target binding and Leu11b-positive cells, and this toxicity is not prevented by lysosomal inhibitors^[3].

Lysosomal Metabolism

L-Leucyl-L-Leucine methyl ester (100-500 µM; 1 h) causes loss of lysosomal membrane integrity in HL-60 cells at 200 and 500 µM but not at 100 µM, as shown by Acridine Orange (HY-101879) staining^[1].
L-Leucyl-L-Leucine methyl ester (0.25 mM; 10 min) causes complete loss of the lysosomal proton gradient in HeLa cells within 10 min^[2].
L-Leucyl-L-Leucine methyl ester (1-5 mM; 30 min) permeabilizes HeLa lysosomes to molecules with a molecular weight of up to at least 4.4K, but does not permeabilize molecules with a molecular weight of 10K or greater^[2].
L-Leucyl-L-Leucine methyl ester (1-5 mM; 15 min-1 h) retains cathepsin in HeLa lysosomes but inactivates it^[2].
L-Leucyl-L-Leucine methyl ester (1-5 mM; 6 h) reduces lysosomal glycosidase activity in HeLa cells, with β-D-galactosidase being the most affected^[2].
L-Leucyl-L-Leucine methyl ester (1 mM; up to 24 h) causes a transient loss of lysosomal acidity in HeLa cells, with reacidification beginning at 30 min and exceeding control levels at 4 h^[2].
L-Leucyl-L-Leucine methyl ester (1 mM; up to 48 h) causes transient enlargement and perinuclear aggregation of LAMP-1-positive lysosomes in HeLa cells^[2].
L-Leucyl-L-Leucine methyl ester (1 mM; 30 min-48 h) transiently enlarges HeLa lysosomes, increasing their volume 3-fold at 24 h and returning to normal at 48 h^[2].

Protein/Amino Acid Metabolism

L-Leucyl-L-Leucine methyl ester (1 mM; 10 h) reduces long-lived protein degradation in HeLa cells within 10 h^[2].

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

Apoptosis Analysis^[1]

Cell Line:

human HL-60 cells
Concentration:

up to 150 µM; 200 µM
Incubation Time:

20 min (room temperature, then further incubation); 1 h (200 µM)
Result:

Induced apoptosis in a concentration-dependent manner, with maximum level at 150 µM.
Decrease in cell size was detected as early as 1 h after incubation with 200 µM, with 40% apoptotic cells at this time point.
With longer incubation, the percentage of apoptotic cells gradually increased.

Apoptosis Analysis^[1]

Cell Line:

human HL-60 cells
Concentration:

200 µM; 500 µM
Incubation Time:

4 h (37°C)
Result:

DNA fragmentation was observed in HL-60 cells.
Lane 4 showed DNA fragmentation in cells incubated with 500 µM, and lane 2 showed DNA fragmentation with 200 µM.
The DPPI inhibitor (GFCHN2) suppressed DNA fragmentation.

Cell Viability Assay^[2]

Cell Line:

HeLa cells
Concentration:

1, 2, 3, 4, 5, 6, 7 mM
Incubation Time:

18 h
Result:

Both crystal violet and LDH assays agreed that cell death was induced only at concentrations above 4 mM after 18 h of continuous exposure.

Immunofluorescence^[2]

Cell Line:

HeLa cells
Concentration:

1 or 5 mM (15 min after BMV109 pre-labeling; or 1 h BMV109 after prior exposure)
Incubation Time:

15 min; 1 h
Result:

Cells labeled with BMV109 for 1 h then exposed to 1 or 5 mM for 15 min showed preserved puncta representing cysteine cathepsin-positive lysosomes, indicating that cysteine cathepsins remained in lysosomes.
When cells were exposed first to 1 or 5 mM and then incubated with BMV109 for another hour, they showed no labeling, indicating that cysteine cathepsins were no longer active.

Western Blot Analysis^[2]

Cell Line:

HeLa cells
Concentration:

1, 3, 5 mM
Incubation Time:

15 min; 1 h
Result:

Compared to control cells, protein levels for the mature forms of catB, catL, and catC were visibly reduced already 15 min after exposure to 1, 3, or 5 mM, and even more so after 1 h.
This indicates that exposure-mediated loss of cysteine cathepsin activities was due to a decrease in total enzyme amount rather than only changes in enzyme kinetics.

Immunofluorescence^[2]

Cell Line:

HeLa cells
Concentration:

1 mM
Incubation Time:

1, 2, 3, 6, 12, 24, 36, 48 h
Result:

Following continuous culture with 1 mM, LAMP-1-positive vesicles became enlarged and localized to the perinuclear region.
By 48 h after exposure, the pattern of LAMP-1 labeling reversed and resembled the appearance of lysosomes in untreated cells.

Related Protocols :

Chemical Information

CAS No. 13022-42-9
Molecular Weight 258.36
Formula C₁₃H₂₆N₂O₃
SMILES

CC(C)C[C@H](N)C(N[C@@H](CC(C)C)C(OC)=O)=O
Synonyms

LLOMe; Leu-Leu methyl ester; H-Leu-Leu-OMe
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Publications (23)

All IPIFCell Imaging/Staining

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Journal Impact Factor

Cell Res

Repair of damaged lysosomes by TECPR1-mediated membrane tubulation during energy crisis. [Abstract]

2026 Jan;36(1):51-71. PMID: 41478856
Autophagy

2026 Jul 10:1-21. PMID: 42410910
Autophagy

PRRSV utilizes MALT1-regulated autophagy flux to switch virus spread and reserve. [Abstract]

2024 Dec;20(12):2697-2718. PMID: 39081059
Adv Sci (Weinh)

Loss of VMP1 Impairs Tight Junction Recycling and Aggravates Intestinal Barrier Dysfunction in Inflammatory Bowel Disease. [Abstract]

2026 May;13(25):e21681. PMID: 41757559
Biomaterials

In-situ cascade assembled peptide-drug conjugate for the treatment of bladder cancer by enhancing membrane-entry and lysosome destabilization. [Abstract]

2026 Jun 27:335:124405. PMID: 42372507
Biomaterials

Engineered cell membrane vesicles loaded with lysosomophilic drug for acute myeloid leukemia therapy via organ-cell-organelle cascade-targeting. [Abstract]

2025 Jun:317:123091. PMID: 39778270
Environ Chem Ecotoxicol

2025 Nov 19;8:267-280.
Pharmacol Res

2026 Nov:233:108478. PMID: 42764063
J Neuroinflammation

Immune subversion by Leishmania infantum parasites suppresses NLRP3-driven inflammatory responses in amyloid-β-activated microglia. [Abstract]

2025 Oct 29;22(1):252. PMID: 41162989
EMBO J

S-palmitoylation modulates ATG2-dependent non-vesicular lipid transport during starvation-induced autophagy. [Abstract]

2025 May;44(9):2596-2619. PMID: 40128367

L-Leucyl-L-Leucine methyl ester purchased from MedChemExpress. Usage Cited in: EMBO J. 2025 May;44(9):2596-2619. [Abstract]

S-palmitoylation of HA-ATG2A detected by ABE assay in HEK293T cells treated with 1 mM LLOMe for indicated times.
World J Gastroenterol

Wogonin derivative V8 enhances bortezomib efficacy in gastric carcinoma by disrupting lysosome-mediated drug resistance. [Abstract]

2026 Feb 28;32(8):113299. PMID: 41809875
J Cell Biol

JIP4 and RILPL1 utilize opposing motor force to dynamically regulate lysosomal tubulation. [Abstract]

2025 Nov 3;224(11):e202404018. PMID: 40990465

L-Leucyl-L-Leucine methyl ester purchased from MedChemExpress. Usage Cited in: J Cell Biol. 2025 Nov 3;224(11):e202404018. [Abstract]

U2OS cells were transfected with HaloTag-LRRK2 for 36 h. Cells were then treated with DMSO, LLOME (1 mM), or LLOME+MLi2 for 2 h before fixation. Cells were then stained for RILPL1 and LAMP2.

L-Leucyl-L-Leucine methyl ester purchased from MedChemExpress. Usage Cited in: J Cell Biol. 2025 Nov 3;224(11):e202404018. [Abstract]

Quantification of the RILPL1 lysosomes per cell. Cells were treated with DMSO, LLOME (1 mM), or LLOME+MLi2 for 2 h.

L-Leucyl-L-Leucine methyl ester purchased from MedChemExpress. Usage Cited in: J Cell Biol. 2025 Nov 3;224(11):e202404018. [Abstract]

HEK293FT cells were transfected with 3xflag-LRRK2 and mCherry-RILPL1 for 24 h. Cells were treated or not with LLOME (1 mM) for 2 h, and lysates were subjected to immunoprecipitation with anti-RFP antibodies. RFP, LRRK2, and pT73-RAB10 were blotted.

L-Leucyl-L-Leucine methyl ester purchased from MedChemExpress. Usage Cited in: J Cell Biol. 2025 Nov 3;224(11):e202404018. [Abstract]

HEK293T cells stably expressing GFP-LRRK2 and TMEM192-3xHA were seeded and treated with DMSO, LLOME (1 mM), or LLOME + MLi2 24 h later. Lysosomes were purified with anti-HA beads following the LYSO-IP technique. Lysosomes were then lysed, and their content was analyzed via immunoblotting.
PLoS Pathog

A non-canonical activation of the host's ESCRT machinery is required for the scission of parasitophorous vacuoles and the replication of Leishmania donovani. [Abstract]

2025 Sep 16;21(9):e1013513. PMID: 40956840
PLoS Pathog

The HN protein of Newcastle disease virus induces cell apoptosis through the induction of lysosomal membrane permeabilization. [Abstract]

2024 Feb 14;20(2):e1011981. PMID: 38354122
Toxicol Appl Pharmacol

Honokiol ameliorates hepatic fibrosis by inducing lysosomal membrane permeabilization and impairing lipophagy in hepatic stellate cells. [Abstract]

2026 Jan:506:117632. PMID: 41207513
Int Immunol

Helicobacter urease suppresses cytotoxic CD8+ T-cell responses through activating Myh9-dependent induction of PD-L1. [Abstract]

2021 Aug 23;33(9):491-504. PMID: 34297096
FEBS Lett

The ubiquitin ligase RNF115 is required for the clearance of damaged lysosomes. [Abstract]

2026 Apr 24. PMID: 42032884
Traffic

Current methods to analyze lysosome morphology, positioning, motility and function. [Abstract]

2022 May;23(5):238-269. PMID: 35343629
bioRxiv

2026 Apr 21.
SSRN

2025 Aug 13.
Preprints

2025 Jul 8.
bioRxiv

2024 July 07.
bioRxiv

Autophagosome turnover requires Arp2/3 complex-mediated maintenance of lysosomal integrity. [Abstract]

2024 Mar 13:2024.03.12.584718. PMID: 38559247

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 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)

References

[1]. Uchimoto T, Nohara H, Kamehara R, Iwamura M, Watanabe N, Kobayashi Y. Mechanism of apoptosis induced by a lysosomotropic agent, L-Leucyl-L-Leucine methyl ester. Apoptosis. 1999 Oct;4(5):357-62.

[2]. Urska Repnik, et al. L-leucyl-L-leucine methyl ester does not release cysteine cathepsins to the cytosol but inactivates them in transiently permeabilized lysosomes. J Cell Sci 15 September 2017; 130 (18): 3124-3140.

[3]. Thiele DL, et al. Regulation of cellular function by products of lysosomal enzyme activity: elimination of human natural killer cells by a dipeptide methyl ester generated from L-leucine methyl ester by monocytes or polymorphonuclear leukocytes. Proceedings of the National Academy of Sciences of the United States of America. 1985 Apr;82(8):2468-72.

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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.

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L-Leucyl-L-Leucine methyl ester

23 Cited Publications

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L-Leucyl-L-Leucine methyl ester

Publications Citing Use of MedChemExpress (MCE) L-Leucyl-L-Leucine methyl ester

All Caspase Isoforms

Biological Activity

Description

In Vitro

Chemical Information

Publications (23)

Purity & Documentation

References

Calculators

Help & FAQs

Bioz

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L-Leucyl-L-Leucine methyl ester

Publications Citing Use of MedChemExpress (MCE) L-Leucyl-L-Leucine methyl ester

All Caspase Isoforms

Biological Activity

Description

In Vitro

Chemical Information

Publications (23)

Purity & Documentation

References

Calculators

Help & FAQs