名称 | LSKL TFA |
描述 | LSKL TFA (H-Leu-Ser-Lys-Leu-NH2 TFA) is a LAP-TGFβ derivative and a TGF-β1 antagonist that can cross the blood-brain barrier, inhibits the binding of TSP-1 to LAP and reduces renal interstitial fibrosis and liver fibrosis, inhibits subarachnoid fibrosis by inhibiting TSP-1-mediated TGF-β1 activity, prevents the occurrence of chronic hydrocephalus and improves long-term neurocognitive deficits after subarachnoid hemorrhage. |
体外活性 | LSKL TFA from the latent form of TGF-β is responsible for the interaction with the KTFR sequence from ADAMTS1, leading to TGF-β 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. [3] |
体内活性 | Intraperitoneal injection of 1 mg/kg LSKL TFA, into male rats exerted a protective effect against subarachnoid fibrosis, attenuated ventricular enlargement, and effectively inhibited the development of hydrocephalus. [1]
Intraperitoneal injection of 30 mg/kg LSKL TFA, was able to successfully inhibit the Smad signaling pathway activated by transforming growth factor-β (TGF-β) after partial hepatectomy. LSKL effectively attenuated the activation of TGF-β-Smad signaling by antagonizing TSP-1 rather than reducing TSP-1 protein expression. [2] |
存储条件 | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 200 mg/mL, (349.27 mM.), Sonication is recommended. H2O : 80 mg/mL (139.71 mM.), Sonication is recommended.
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关键字 | LSKL, Inhibitor of Thrombospondin (TSP 1) (TFA) | LSKL, Inhibitor of Thrombospondin (TSP-1) | LSKL, Inhibitor of Thrombospondin (TSP1) (TFA) |
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