| Name | LSKL TFA |
| Description | 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. |
| In vitro | 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] |
| In vivo | 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (8.73 mM), Sonication is recommended.
DMSO : 200 mg/mL (349.27 mM), Sonication is recommended.
H2O : 80 mg/mL (139.71 mM), Sonication is recommended.
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| Keywords | TGF-β1 | TGF-β/Smad | TGF-β Receptor | TGFβ | TGFbeta/Smad | TGF-beta | TGFbeta | TGF-b/Smad | TGFb | Smad | LSKL, Inhibitor of Thrombospondin (TSP1) (TFA) | LSKL, Inhibitor of Thrombospondin (TSP-1) | LSKL, Inhibitor of Thrombospondin (TSP 1) (TFA) |
| Inhibitors Related | Trimethylamine N-oxide | Melamine | SB-431542 | Hydrochlorothiazide | Hippuric acid | Chromenone 1 | Pirfenidone | A 83-01 | Suberic acid | Cetrimonium bromide | Galunisertib | Alantolactone |
| Related Compound Libraries | Osteogenesis Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Ovarian Cancer Compound Library | Peptide Compound Library | CNS-Penetrant Compound Library | Stem Cell Differentiation Compound Library | Bioactive Compounds Library Max | TGF-beta/Smad Compound Library | Neuronal Differentiation Compound Library |
United States
