LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)
(Synonyms: LSKL, 血小板反应蛋白抑制剂 (TSP-1) 三氟醋酸盐) 目录号 : GC39398
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LSKL, Inhibitor of Thrombospondin TSP-1是一种来源于潜伏相关蛋白（LAP）-TGFβ的四肽，可竞争性结合抑制TGF-β1。
Sample solution is provided at 25 µL, 10mM.
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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[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.
LSKL, Inhibitor of Thrombospondin TSP-1是一种来源于潜伏相关蛋白（LAP）-TGFβ的四肽，可竞争性结合抑制TGF-β1[1-2]。LSKL可用于肝纤维化、肾间质纤维化、蛛网膜下腔出血后脑积水及肝再生等相关研究[3-4]。
在体外，LSKL（50μM）预处理HK-2肾小管上皮细胞12小时，随后在OX-LDL（25μg/ml）刺激下培养，LSKL显著抑制OX-LDL诱导的纤维化反应，降低纤维化和炎症标志物的表达，并可能通过干扰TGF-β通路发挥作用[5]。LSKL（17.46μM）处理食管鳞状细胞癌KYSE-150细胞，LSKL显著降低了由DJ-1（重组蛋白）刺激诱导的细胞迁移和侵袭能力，并减弱了Smad3的磷酸化与核聚集[6]。
在体内，在博来霉素诱导的肺纤维化小鼠模型中，腹腔注射LSKL（4mg/kg；每日一次；持续14天）可显著减轻博来霉素诱导的肺内胶原沉积、羟脯氨酸含量升高以及内质网应激相关蛋白（如Grp78、CHOP）和纤维化标志物（α-SMA、纤维连接蛋白）的表达，从而改善肺纤维化进程[7]。链脲佐菌素诱导的糖尿病性勃起功能障碍大鼠模型中，腹腔注射LSKL（30mg/kg；每周两次；持续四周）可显著提高最大海绵体内压与平均动脉压的比值，改善勃起功能，并减轻海绵体纤维化，表现为胶原沉积减少、胶原I/胶原III比值升高以及平滑肌/胶原比值升高，同时降低了海绵体内血栓反应蛋白-1、活化TGF-β1、磷酸化SMAD2/3及胶原IV的表达水平[8]。
| 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 | ||
| 别名 | LSKL, 血小板反应蛋白抑制剂 (TSP-1) 三氟醋酸盐 | ||
| 分子式 | C23H43F3N6O7 | 分子量 | 572.62 |
| 溶解度 | Water: 100 mg/mL (174.64 mM) | 储存条件 | Store at -20°C |
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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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