LSKL, Inhibitor of Thrombospondin (TSP-1)
Based on 18 publication(s) in Google Scholar
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.
- Purity: 99.34%
- CAS No.: 283609-79-0
- Formula: C21H42N6O5
- Molecular Weight:458.60
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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)
Publications Citing Use of MedChemExpress (MCE) LSKL, Inhibitor of Thrombospondin (TSP-1)
More- J Exp Clin Cancer Res. 2022 Aug 26;41(1):259. [Abstract]
- Cell Death Dis. 2022 Jul 30;13(7):663. [Abstract]
- J Immunother Cancer. 2026 Feb 24;14(2):e013655. [Abstract]
- Sci China Life Sci. 2025 Mar;68(3):746-763. [Abstract]
- Antioxidants (Basel). 2023 Nov 21;12(12):2024. [Abstract]
- Environ Pollut. 2020 Apr:259:113915. [Abstract]
- Front Immunol. 2022 Mar 18;13:853894. [Abstract]
- Life Sci. 2026 Feb 1:386:124156. [Abstract]
- J Am Heart Assoc. 2021 Oct 19;10(20):e022701. [Abstract]
- Front Cell Dev Biol. 2021 Feb 18:8:601521. [Abstract]
- Sci Rep. 2025 Dec 23. [Abstract]
- Cancer Sci. 2024 Aug;115(8):2718-2728. [Abstract]
- Cancers. 2019 Dec 5;11(12):1946. [Abstract]
- iScience. 2026 Jun 19;29(7). [Abstract]
- Cell Tissue Res. 2022 May;388(2):259-271. [Abstract]
- PLoS One. 2024 Oct 7;19(10):e0311594. [Abstract]
- bioRxiv. 2025 June 03.
- Ann Transl Med. 2021 Dec;9(23):1738. [Abstract]
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Histological Imaging/Staining
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RT-PCR
Biological Activity
TGF-β1[1]
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.
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.
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Animal Model:103 male Sprague-Dawley rats (6 weeks of age; 160-180 g) with subarachnoid hemorrhage (SAH)[1]
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection
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Result:Was protective against subarachnoid fibrosis, attenuated ventriculomegaly and effectively suppressed hydrocephalus.
Chemical Information
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CAS No. 283609-79-0
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Appearance Solid
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Molecular Weight 458.60
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Formula C21H42N6O5
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Color White to off-white
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Sequence
Leu-Ser-Lys-Leu-NH2
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Sequence Shortening
LSKL-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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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)
Publications (18)
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Journal Impact Factor
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Most Recent
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J Exp Clin Cancer Res
Irradiation induces DJ-1 secretion from esophageal squamous cell carcinoma cells to accelerate metastasis of bystander cells via a TGF-β1 positive feedback loop. [Abstract]2022 Aug 26;41(1):259. PMID: 36008860 -
Cell Death Dis
Sestrin2 remedies podocyte injury via orchestrating TSP-1/TGF-β1/Smad3 axis in diabetic kidney disease. [Abstract]2022 Jul 30;13(7):663. PMID: 35908070 -
J Immunother Cancer
Macrophage Mtdh deficiency discordantly regulated tumor growth and metastasis through increased thrombospondin-1 production. [Abstract]2026 Feb 24;14(2):e013655. PMID: 41734995 -
Sci China Life Sci
Integrating spatial transcriptomics and single-nucleus RNA-seq revealed the specific inhibitory effects of TGF-β on intramuscular fat deposition. [Abstract]2025 Mar;68(3):746-763. PMID: 39422812 -
Antioxidants (Basel)
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. [Abstract]2023 Nov 21;12(12):2024. PMID: 38136144
LSKL, Inhibitor of Thrombospondin (TSP-1) purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2023 Nov 21;12(12):2024. [Abstract]
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. [Abstract]
ICR mice were randomized into four groups: Control, LSKL, BLM + Control and BLM + LSKL. Representative images of Masson’s trichrome staining of lung fibrosis.
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Environ Pollut
Exposure to Benzo[a]pyrene impairs the corpus luteum vascular network in rats during early pregnancy. [Abstract]2020 Apr:259:113915. PMID: 32023792 -
Front Immunol
Intraperitoneally Delivered Mesenchymal Stem Cells Alleviate Experimental Colitis Through THBS1-Mediated Induction of IL-10-Competent Regulatory B Cells. [Abstract]2022 Mar 18;13:853894. PMID: 35371051 -
Life Sci
LSKL mitigates dehydroepiandrosterone-induced apoptosis and oxidative stress by THBS1/PI3K/AKT pathway in rat granulosa cells. [Abstract]2026 Feb 1:386:124156. PMID: 41412276 -
J Am Heart Assoc
Inhibition of Aryl Hydrocarbon Receptor Attenuates Hyperglycemia-Induced Hematoma Expansion in an Intracerebral Hemorrhage Mouse Model. [Abstract]2021 Oct 19;10(20):e022701. PMID: 34622690 -
Front Cell Dev Biol
THBS1/CD47 Modulates the Interaction of γ-Catenin With E-Cadherin and Participates in Epithelial-Mesenchymal Transformation in Lipid Nephrotoxicity. [Abstract]2021 Feb 18:8:601521. PMID: 33681182 -
Sci Rep
SLC11A1 can activate TGF-β1 signaling pathway to resist ferroptosis in colorectal cancer. [Abstract]2025 Dec 23. PMID: 41436829
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.
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Cancer Sci
Afatinib plus PEM and CBDCA overcome osimertinib resistance in EGFR-mutated NSCLC with high thrombospondin-1 expression. [Abstract]2024 Aug;115(8):2718-2728. PMID: 38941131 -
Cancers
Exosomal Thrombospondin-1 Disrupts the Integrity of Endothelial Intercellular Junctions to Facilitate Breast Cancer Cell Metastasis. [Abstract]2019 Dec 5;11(12):1946. PMID: 31817450
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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iScience
Proteomics and human microchips identify Thrombospondin-1 as a potential biomarker for calciphylaxis stem cell therapy. [Abstract]2026 Jun 19;29(7). PMID: 42382992 -
Cell Tissue Res
Tsp-1 is involved in DNA stability through Tgf-β1 activation domain in cone photoreceptor 661 W cells. [Abstract]2022 May;388(2):259-271. PMID: 35260935 -
PLoS One
miR-335-3p attenuates transforming growth factor beta 1-induced fibrosis by suppressing Thrombospondin 1. [Abstract]2024 Oct 7;19(10):e0311594. PMID: 39374214
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.
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Ann Transl Med
Thrombospondin-1 aggravates colonic mucosal inflammatory injuries via promoting the differentiation of CD11c+ macrophages with lysosomal activity limited in colitis. [Abstract]2021 Dec;9(23):1738. PMID: 35071432
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (218.05 mM); Clear solution; Need ultrasonic
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Liao F, 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. Epub 2016 Aug 31. [Content Brief]
[2]. Laurent MA, et al. In silico characterization of the interaction between LSKL peptide, a LAP-TGF-beta derived peptide, and ADAMTS1. Comput Biol Chem. 2016 Apr;61:155-61. [Content Brief]
[3]. Kuroki H, et al. Effect of LSKL peptide on thrombospondin 1-mediated transforming growth factor β signal activation and liver regeneration after hepatectomy in an experimental model. Br J Surg. 2015 Jun;102(7):813-25. [Content Brief]
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.