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LSKL is a potent and peptide-based inhibitor of Thrombospondin TSP-1 with the potential to be used for treating hypertrophic scar. LSKL peptide was able to inhibit the overexpression of extracellular matrix and contractile ability of HTS (Hypertrophic scar) fibroblasts. In vivo, LSKL could attenuate the thickness of HTS, distortion of collagen alignment and fibrogenesis. Further, LSKL peptide not only remarkably attenuated cell proliferation and migration, but also induced cell apoptosis of HTS fibroblasts. In addition, LSKL peptide significantly suppressed the phosphorylation of PI3K, AKT, and mTOR, while not affecting the phosphorylation of Smad2/3 and MEK/ERK. LSKL might be a promising anti-fibrosis agent to HTS through modulating the PI3K/AKT/mTOR signaling pathway.
| ln Vitro |
The KTFR sequence in ADAMTS1 is responsible for binding with LSKL (thrombospondin inhibitor (TSP-1)) (LSKL peptide) in the latent form of TGF-β, resulting to its activation. There is a stable binding mechanism between thrombospondin inhibitor (TSP-1) LSKL and ADAMTS1 KTFR sequence, which is defined by 3 salt bridges and 2 hydrogen bonds [2].
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| ln Vivo |
Sprague-Dawley male rats administered intraperitoneally with 1 mg/kg of LSKL, a thrombospondin inhibitor (TSP-1) are able to effectively suppress hydrocephalus, avoid subarachnoid fibrosis, and decrease ventricular hypertrophy. Thrombuspondin inhibitor (TSP-1) therapy in LSKL suppresses TGF-β1 expression and consequent Smad2/3 signaling [1]. LSKL, a thrombospondin (TSP-1) inhibitor (30 mg/kg, i.p.) effectively prevented the activation of transforming growth factor (TGF) β-Smad signaling that was induced by partial hepatectomy. Rather of decreasing TSP-1 protein expression, the thrombospondin (TSP-1) inhibitor LSKL effectively inhibited TGF-β-Smad signaling activation. Following liver resection, hepatocyte proliferation can be accelerated by LSKL, a thrombospondin inhibitor (TSP-1) [3].
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| Animal Protocol |
Animal/Disease Models: 103 male SD (SD (Sprague-Dawley)) rats (6 weeks old; 160-180 g) [1] with subarachnoid hemorrhage (SAH) [1]
Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Yes Subarachnoid fibrosis, reducing ventricular enlargement and effectively inhibiting hydrocephalus. |
| 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.
[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. [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. |
| Molecular Formula |
C21H42N6O5
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|---|---|
| Molecular Weight |
458.5954
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| CAS # |
283609-79-0
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| Related CAS # |
LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA);2828433-17-4
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| SMILES |
O=C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H])N([H])C([C@]([H])(C([H])([H])O[H])N([H])C([C@]([H])(C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H])N([H])[H])=O)=O)N([H])[C@]([H])(C(N([H])[H])=O)C([H])([H])C([H])(C([H])([H])[H])C([H])([H])[H]
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~218.05 mM)
H2O : ~50 mg/mL (~109.03 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 100 mg/mL (218.05 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2181 mL | 1.0903 mL | 2.1805 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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