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

LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 

Art. -Nr.: HY-P0299A Reinheit: 99.51%
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LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 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) TFA can readily crosse the blood-brain barrier.

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CAS. Nr. : 2828433-17-4

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Based on 17 publication(s) in Google Scholar

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

Top Publications Citing Use of Products

    LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 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) TFA 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) TFA 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) TFA 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) TFA 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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    Beschreibung

    LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 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) TFA 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.
    Molekulargewicht

    458.60 (free base)

    Formel

    C21H42N6O5·xC2HF3O2

    CAS. Nr.
    Appearance

    Solid

    Color

    White to off-white

    Sequence

    Leu-Ser-Lys-Leu-NH2

    Sequence Shortening

    LSKL-NH2

    Versand

    Room temperature in continental US; may vary elsewhere.

    Speicherung

    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)

    Lösungsmittel & Löslichkeit
    In Vitro: 

    DMSO : ≥ 100 mg/mL

    H2O : 100 mg/mL (Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    • Molaritätsrechner

    • Verdünnungsrechner

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL; Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL; Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 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; Clear solution; Need ultrasonic

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

    Dosage

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    Dosing volume
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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).
    Reinheit & Dokumentation

    Purity: 99.51%

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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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    Produktname:
    LSKL, Inhibitor of Thrombospondin (TSP-1) TFA
    Art. -Nr.:
    HY-P0299A
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