1. TGF-beta/Smad
  2. TGF-β Receptor
  3. LSKL, Inhibitor of Thrombospondin (TSP-1)

LSKL, Inhibitor of Thrombospondin (TSP-1) 

Cat. No.: HY-P0299 Purity: 99.34%
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LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier.

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

Custom Peptide Synthesis

CAS No. : 283609-79-0

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Customer Review

Based on 17 publication(s) in Google Scholar

Other Forms of LSKL, Inhibitor of Thrombospondin (TSP-1):

Top Publications Citing Use of Products

    LSKL, Inhibitor of Thrombospondin (TSP-1) purchased from MedChemExpress. Usage Cited in: Sci Rep. 2025 Dec 23.  [Abstract]

    In HCT116 cells, after transfecting the over-expression plasmid for 48 h, LSKL (an inhibitor of the TGF-β1 pathway, 5 µmol/L) was added and the cells were incubated for an additional 24 h. In HT29 cells, after transfecting siRNA for 48 h, 10 ng/mL TGF-β1 (an activator of the TGF - β1 pathway) was added. After these treatments for both types of cells, the protein expression levels of Smad 2/3, p-Smad 2/3, and TGF-β1 were detected by Western blot assay.

    LSKL, Inhibitor of Thrombospondin (TSP-1) purchased from MedChemExpress. Usage Cited in: PLoS One. 2024 Oct 7;19(10):e0311594.  [Abstract]

    A549 and BEAS-2B cells were treated with 5 ng/mL TGF-β1 and/or 20 μM LSKL for 48 h. The expression of proteins associated with TGF-β1 downstream signaling was assessed by western blotting.

    LSKL, Inhibitor of Thrombospondin (TSP-1) purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2023 Nov 21;12(12):2024.

    ICR mice were randomized into four groups: Control, LSKL, BLM + Control and BLM + LSKL. Protein levels of Grp78 and CHOP in lung tissues.

    LSKL, Inhibitor of Thrombospondin (TSP-1) purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2023 Nov 21;12(12):2024.

    ICR mice were randomized into four groups: Control, LSKL, BLM + Control and BLM + LSKL. Representative images of Masson’s trichrome staining of lung fibrosis.

    LSKL, Inhibitor of Thrombospondin (TSP-1) purchased from MedChemExpress. Usage Cited in: Cancers. 2019 Dec 5;11(12):1946.  [Abstract]

    mRNA transcription level of occludin, ZO-1, VE-cadherin, in HUVECs treated with different amount of LSKL (0-100 μM).

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    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier[1][2].

    IC50 & Target

    TGF-β1[1]

    In Vitro

    The KTFR sequence from ADAMTS1 is responsible for the interaction with the LSKL, Inhibitor of Thrombospondin (TSP-1) (LSKL peptide) from the latent form of TGF-β, leading to its activation. There is a stable binding mode between LSKL, Inhibitor of Thrombospondin (TSP-1) and ADAMTS1 KTFR sequence, characterized by 3 salt bridges and 2 hydrogen bonds[2].

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

    In Vivo

    LSKL, Inhibitor of Thrombospondin (TSP-1) (1 mg/kg; intraperitoneal injection; male Sprague-Dawley rats) is protective against subarachnoid fibrosis, attenuates ventriculomegaly and effectively suppresses hydrocephalus. LSKL, Inhibitor of Thrombospondin (TSP-1) treatment inhibits TGF-β1 activity and subsequent Smad2/3 signaling[1].
    LSKL, Inhibitor of Thrombospondin (TSP-1) (30 mg/kg, i.p.) successfully inhibits transforming growth factor (TGF) β-Smad signal activation induced by partial hepatectomy. LSKL, Inhibitor of Thrombospondin (TSP-1) successfully attenuates TGF-β-Smad signal activation by antagonizing TSP-1, but not by reducing TSP-1 protein expression. LSKL, Inhibitor of Thrombospondin (TSP-1) accelerates hepatocyte proliferation after hepatectomy[3].

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

    Animal Model: 103 male Sprague-Dawley rats (6 weeks of age; 160-180 g) with subarachnoid hemorrhage (SAH)[1]
    Dosage: 1 mg/kg
    Administration: Intraperitoneal injection
    Result: Was protective against subarachnoid fibrosis, attenuated ventriculomegaly and effectively suppressed hydrocephalus.
    Molecular Weight

    458.60

    Formula

    C21H42N6O5

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    Sequence

    Leu-Ser-Lys-Leu-NH2

    Sequence Shortening

    LSKL-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: 

    DMSO : 100 mg/mL (218.05 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 50 mg/mL (109.03 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1805 mL 10.9027 mL 21.8055 mL
    5 mM 0.4361 mL 2.1805 mL 4.3611 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)

    Mass
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    Concentration
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    Volume (final)

    V2

    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    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.45 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 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 2

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

      Solubility: ≥ 2.5 mg/mL (5.45 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.

    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 (218.05 mM); Clear solution; Need ultrasonic

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

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    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: 99.84%

    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 / DMSO 1 mM 2.1805 mL 10.9027 mL 21.8055 mL 54.5137 mL
    5 mM 0.4361 mL 2.1805 mL 4.3611 mL 10.9027 mL
    10 mM 0.2181 mL 1.0903 mL 2.1805 mL 5.4514 mL
    15 mM 0.1454 mL 0.7268 mL 1.4537 mL 3.6342 mL
    20 mM 0.1090 mL 0.5451 mL 1.0903 mL 2.7257 mL
    25 mM 0.0872 mL 0.4361 mL 0.8722 mL 2.1805 mL
    30 mM 0.0727 mL 0.3634 mL 0.7268 mL 1.8171 mL
    40 mM 0.0545 mL 0.2726 mL 0.5451 mL 1.3628 mL
    50 mM 0.0436 mL 0.2181 mL 0.4361 mL 1.0903 mL
    60 mM 0.0363 mL 0.1817 mL 0.3634 mL 0.9086 mL
    80 mM 0.0273 mL 0.1363 mL 0.2726 mL 0.6814 mL
    100 mM 0.0218 mL 0.1090 mL 0.2181 mL 0.5451 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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      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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    Product Name:
    LSKL, Inhibitor of Thrombospondin (TSP-1)
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