ChemicalBook CAS DataBase List 2828433-17-4

2828433-17-4

Name	LSKL, INhibitor of Thrombospondin (TSP-1) trifluoroacetate
CAS	2828433-17-4
Molecular Formula	C23H43F3N6O7
Molecular Weight	572.63
MOL File	2828433-17-4.mol

Chemical Properties

form	Solid
color	White to off-white

Hazard Information

Uses

LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA 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) TFA can readily crosse the blood-brain barrier[1][2].

in vivo

LSKL, Inhibitor of Thrombospondin (TSP-1) (1 mg/kg; intraperitoneal injection; male Sprague-Dawley rats) is protective against subarachnoid fibrosis, attenuates ventriculomegaly and effectively suppresses hydrocephalus. LSKL, Inhibitor of Thrombospondin (TSP-1) treatment inhibits TGF-β1 activity and subsequent Smad2/3 signaling^[1].
? 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].

Animal Model:	103 male Sprague-Dawley rats (6 weeks of age; 160-180 g) with subarachnoid hemorrhage (SAH)^[1]
Dosage:	1 mg/kg
Administration:	Intraperitoneal injection
Result:	Was protective against subarachnoid fibrosis, attenuated ventriculomegaly and effectively suppressed 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. DOI:10.3892/etm.2016.3640
[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. DOI:10.1016/j.compbiolchem.2016.01.012
[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. DOI:10.1002/bjs.9765

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