1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. L17E

L17E is an attenuated cationic amphiphilic lytic (ACAL) peptide that can be used to deliver a variety of macromolecules, including proteins, antibodies, and DNA nanostructures. L17E inserts and cleaves the membrane structure through electrostatic interaction, enabling intracellular escape. The efficiency of L17E-mediated delivery is strongly correlated with the expression level of KCNN4 (the gene encoding the calcium-activated potassium channel KCa3.1). L17E also promotes the cellular uptake of macromolecules by inducing micropinocytosis. L17E can be further optimized and improved through dimerization strategies and in combination with other delivery systems, such as nuclear localization signal peptides and cell membrane-coated nanoparticles.

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L17E

L17E Chemical Structure

CAS No. : 1898254-09-5

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Based on 1 publication(s) in Google Scholar

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Description

L17E is an attenuated cationic amphiphilic lytic (ACAL) peptide that can be used to deliver a variety of macromolecules, including proteins, antibodies, and DNA nanostructures. L17E inserts and cleaves the membrane structure through electrostatic interaction, enabling intracellular escape. The efficiency of L17E-mediated delivery is strongly correlated with the expression level of KCNN4 (the gene encoding the calcium-activated potassium channel KCa3.1). L17E also promotes the cellular uptake of macromolecules by inducing micropinocytosis. L17E can be further optimized and improved through dimerization strategies and in combination with other delivery systems, such as nuclear localization signal peptides and cell membrane-coated nanoparticles[1][2][3][4][5][6].

In Vitro

L17E (40-80 μM) suppresses TS5-p45 translocation to the nucleus in HUVECs by disrupting the integrity of the late endosome (LE) membrane[1].
L17E (50-100 μM, 25 h) eliminates the pro-apoptotic activity of TS5-p45 (TS5-p45 must enter the cell nucleus in order to trigger the apoptotic process) in HUVECs[1].
L17E causes approximately 50% of the cells to exhibit strong cytoplasmic signals in Hela cells and its ability to lyse negatively charged membranes is much stronger than that on neutral membranes with no significant pH dependence[2].
L17E (40μM, 1-24 h) exhibits almost 90% cell viability when treated in serum-free medium for one hour or serum-supplemented medium for 24 hours[2][3].
L17E (40 μM, 7 h) efficiently delivers the ribosome inactivating protein (Saporin), resulting in approximately 80% Hela cell death; while without it, the cell death rate is only approximately 15%[2].
L17E (40 μM, 25 h) delivers the Cre recombinase and initiates the expression of EGFP in Hela cells[2].
L17E (40 μM, 1.5 h) delivers anti-His6-IgG to the cytoplasmic side and successfully bound to the intracellular target in Hela cells[2].
L17E (40 μM, 0.5 h) with anti-GR antibody treatment is able to significantly inhibit the upregulation of the MT1E gene induced by Dexamethasone (Dex) (HY-14648G)[2].
L17E (40 μM, 49 h) enhances the efficacy of exosome-mediated intracellular delivery in Hela cells[2].
L17E (20-40 μM, 1 h) enhances the internalization of Dex by inducing macropinocytosis, and achieves cytoplasmic release by specifically lysing the endosomal membrane[2].
L17E coating enables efficient endosomal release of tetrahedral DNA frameworks (TDFs) in RAW264.7 cells[4].
L17E coating substantially enhances the stability of TDFs and improves their uptake efficiency into RAW264.7 cells through endocytosis and macropinocytosis[4].
L17E (12 h)-coated TDF to deliver osteogenic growth peptide (OGF) exerts powerful antioxidant and anti-inflammatory functions within the RAW264.7 cells[4].

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

Apoptosis Analysis[1]

Cell Line: HUVECs
Concentration: 50, 75, 100 μM
Incubation Time: Pretreat for 1 h and with TS5-p45 for 24 h
Result: Diminished the TS5-p45 induced apoptosis in a dose-dependent manner.
In Vivo

L17E-TDF-OGP (situ injection, single dose) inhibits efficiently periodontitis in mice[4].
DNase@BSNP-NLS/L17E-M (with L17E encapsulated) (10 mg/mL, i.v., once every two days for 5 times) homologously deliveres functional proteins to cancer cell nuclei in Hela-xenografted mice and exhibits significant anti-tumor properties[5].

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

Molecular Weight

2859.42

Formula

C134H220N38O31

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Ile-Trp-Leu-Thr-Ala-Leu-Lys-Phe-Leu-Gly-Lys-His-Ala-Ala-Lys-His-Glu-Ala-Lys-Gln-Gln-Leu-Ser-Lys-Leu-NH2

Sequence Shortening

IWLTALKFLGKHAAKHEAKQQLSKL-NH2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

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

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (34.97 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.3497 mL 1.7486 mL 3.4972 mL
5 mM 0.0699 mL 0.3497 mL 0.6994 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.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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
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 (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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O 1 mM 0.3497 mL 1.7486 mL 3.4972 mL 8.7430 mL
5 mM 0.0699 mL 0.3497 mL 0.6994 mL 1.7486 mL
10 mM 0.0350 mL 0.1749 mL 0.3497 mL 0.8743 mL
15 mM 0.0233 mL 0.1166 mL 0.2331 mL 0.5829 mL
20 mM 0.0175 mL 0.0874 mL 0.1749 mL 0.4372 mL
25 mM 0.0140 mL 0.0699 mL 0.1399 mL 0.3497 mL
30 mM 0.0117 mL 0.0583 mL 0.1166 mL 0.2914 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.

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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.

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