LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA)

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.

Product information

Molecular Weight: 572.62

Formula: C23H43F3N6O7

Chemical Name: (S)-6-amino-N-((S)-1-amino-4-methyl-1-oxopentan-2-yl)-2-((S)-2-((S)-2-amino-4-methylpentanamido)-3-hydroxypropanamido)hexanamide 2, 2, 2-trifluoroacetate

Smiles: CC(C)C[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(C)C)C(N)=O.OC(=O)C(F)(F)F

InChiKey: FULCVSARTMWAGA-SITLLQIKSA-N

InChi: InChI=1S/C21H42N6O5.C2HF3O2/c1-12(2)9-14(23)19(30)27-17(11-28)21(32)25-15(7-5-6-8-22)20(31)26-16(18(24)29)10-13(3)4;3-2(4,5)1(6)7/h12-17,28H,5-11,22-23H2,1-4H3,(H2,24,29)(H,25,32)(H,26,31)(H,27,30);(H,6,7)/t14-,15-,16-,17-;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (436.59 mM; Need ultrasonic). H2O : 100 mg/mL (174.64 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

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. 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.

Products are for research use only. Not for human use.