LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) |
Catalog No.GC39398
One-Click Copy Product Info
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LSKL, Inhibitor of Thrombospondin TSP-1, is a tetrapeptide derived from Latency-Associated Protein (LAP)-TGFβ. LSKL competitively binds to and inhibits TGF-β1.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
LSKL, Inhibitor of Thrombospondin TSP-1, is a tetrapeptide derived from Latency-Associated Protein (LAP)-TGFβ. LSKL competitively binds to and inhibits TGF-β1[1-2]. LSKL is utilized in research areas such as liver fibrosis, renal interstitial fibrosis, hydrocephalus following subarachnoid hemorrhage, and liver regeneration[3-4].
In vitro, HK-2 renal tubular epithelial cells were pretreated with LSKL (50µM) for 12 hours, followed by stimulation with OX-LDL (25µg/ml). LSKL significantly suppressed the OX-LDL-induced fibrotic response, reducing the expression of fibrosis and inflammation markers, potentially by interfering with the TGF-β pathway[5]. KYSE-150 esophageal squamous cell carcinoma cells were treated with LSKL (17.46µM). LSKL significantly reduced the cell migration and invasion induced by DJ-1 (recombinant protein) stimulation and attenuated the phosphorylation and nuclear aggregation of Smad3[6].
In vivo, in a bleomycin-induced pulmonary fibrosis mouse model, intraperitoneal injection of LSKL (4mg/kg; once daily; for 14 days) significantly alleviated bleomycin-induced intrapulmonary collagen deposition, increased hydroxyproline content, and reduced the expression of endoplasmic reticulum stress-related proteins (such as Grp78, CHOP) and fibrosis markers (such as α-SMA, fibronectin), thereby improving the fibrotic process[7]. In a streptozotocin-induced diabetic erectile dysfunction rat model, intraperitoneal injection of LSKL (30mg/kg; twice weekly; for four weeks) significantly increased the ratio of maximal intracavernous pressure to mean arterial pressure, improving erectile function, and alleviated corpus cavernosum fibrosis. LSKL reduced collagen deposition, an altered collagen I/collagen III ratio, an increased smooth muscle/collagen ratio, and decreased expression levels of thrombospondin-1, active TGF-β1, phosphorylated SMAD2/3, and collagen IV in the corpus cavernosum[8].
References:
[1] Liao F, Li G, Yuan W, et al. LSKL peptide alleviates subarachnoid fibrosis and hydrocephalus by inhibiting TSP1-mediated TGF-β1 signaling activity following subarachnoid hemorrhage in rats. Exp Ther Med. 2016 Oct;12(4):2537-2543.
[2] Song S, Shi C, Bian Y, et al. Sestrin2 remedies podocyte injury via orchestrating TSP-1/TGF-β1/Smad3 axis in diabetic kidney disease. Cell Death Dis. 2022 Jul 30;13(7):663.
[3] Zhang L, Wang C, Liu Y, et al. LSKL mitigates dehydroepiandrosterone-induced apoptosis and oxidative stress by THBS1/PI3K/AKT pathway in rat granulosa cells. Life Sci. 2026 Feb 1;386:124156.
[4] Ren R, Lu Q, Sherchan P, et al. Inhibition of Aryl Hydrocarbon Receptor Attenuates Hyperglycemia-Induced Hematoma Expansion in an Intracerebral Hemorrhage Mouse Model. J Am Heart Assoc. 2021 Oct 19;10(20):e022701.
[5] Gao L, Yang TT, Zhang JS, et al. THBS1/CD47 Modulates the Interaction of γ-Catenin With E-Cadherin and Participates in Epithelial-Mesenchymal Transformation in Lipid Nephrotoxicity. Front Cell Dev Biol. 2021 Feb 18;8:601521.
[6] Gu J, Sun Y, Song J, et al. Irradiation induces DJ-1 secretion from esophageal squamous cell carcinoma cells to accelerate metastasis of bystander cells via a TGF-β1 positive feedback loop. J Exp Clin Cancer Res. 2022 Aug 26;41(1):259.
[7] Zhan JH, Wei J, Liu L, et al. Investigation of a UPR-Related Gene Signature Identifies the Pro-Fibrotic Effects of Thrombospondin-1 by Activating CD47/ROS/Endoplasmic Reticulum Stress Pathway in Lung Fibroblasts. Antioxidants (Basel). 2023 Nov 21;12(12):2024.
[8] Xia M, Yuan Y, Fang D, et al. Blocking TSP1 Ameliorates Diabetes Mellitus-Induced Erectile Dysfunction by Inhibiting the TGF-β/SMAD Pathway. World J Mens Health. 2025 Jul;43(3):580-594.
| Cell experiment [1]: | |
Cell lines | KYSE-150 cells (human esophageal squamous cell carcinoma cell line) |
Preparation Method | KYSE-150 cells were cultured in RPMI1640 medium supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. In the migration and invasion assays, unirradiated bystander KYSE-150 cells were indirectly co-cultured with irradiated cells (8Gy ionizing X-ray) or stimulated with recombinant DJ-1 protein (800pg). The TSP1 inhibitor LSKL (17.46µM) was added to the culture medium. |
Reaction Conditions | 17.46µM; 24 hours co-culture/invasion period. |
Applications | The LSKL significantly reduced the DJ-1-induced migration and invasion of KYSE-150 cells in Transwell and 3D tumor spheroid invasion assays. The study indicates that LSKL blocks the TSP1/TGF-β1/Smad3 positive feedback loop, which is the core pathway promoting ESCC metastasis in the radiation-induced bystander effect. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rats with streptozotocin-induced diabetes mellitus-induced erectile dysfunction (DMED) |
Preparation Method | After eight weeks following the induction of diabetes mellitus, the rats in the DMED+LSKL group were subjected to intraperitoneal injections of LSKL (30mg/kg) twice weekly for four weeks. Erectile function was evaluated by measuring the maximum intracavernous pressure (ICP) to mean arterial pressure (MAP) ratio. Corpus cavernosum (CC) tissues were harvested for histological and protein analysis. |
Dosage form | 30mg/kg; i.p.; Twice weekly for four weeks. |
Applications | LSKL administration significantly increased the maximum ICP-to-MAP ratio, indicating improved erectile function. LSKL also attenuated corpus cavernosum fibrosis, as evidenced by an increased smooth muscle to collagen ratio, a modified collagen I to collagen III ratio, and reduced expression of fibrosis markers (collagen IV, fibronectin). Furthermore, LSKL treatment downregulated the levels of thrombospondin-1 (TSP1), active TGF-β1, and phosphorylated SMAD2/3 in the penile tissue. |
References: | |
| Cas No. | SDF | ||
| Formula | C23H43F3N6O7 | M.Wt | 572.62 |
| Solubility | Water: 100 mg/mL (174.64 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7464 mL | 8.7318 mL | 17.4636 mL |
| 5 mM | 349.3 μL | 1.7464 mL | 3.4927 mL |
| 10 mM | 174.6 μL | 873.2 μL | 1.7464 mL |
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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 35 reference(s) in Google Scholar.)