1. TGF-beta/Smad
  2. TGF-β Receptor
  3. LSKL, Inhibitor of Thrombospondin (TSP-1)

LSKL, Inhibitor of Thrombospondin (TSP-1) 

Cat. No.: HY-P0299 Purity: 98.46%
Handling Instructions

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

For research use only. We do not sell to patients.

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LSKL, Inhibitor of Thrombospondin (TSP-1) Chemical Structure

LSKL, Inhibitor of Thrombospondin (TSP-1) Chemical Structure

CAS No. : 283609-79-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 108 In-stock
Estimated Time of Arrival: December 31
10 mg USD 156 In-stock
Estimated Time of Arrival: December 31
25 mg USD 312 In-stock
Estimated Time of Arrival: December 31
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Description

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

IC50 & Target

TGF-β1[1]

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[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.
Molecular Weight

458.60

Formula

C₂₁H₄₂N₆O₅

CAS No.

283609-79-0

Sequence

Leu-Ser-Lys-Leu

Sequence Shortening

LSKL

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (218.05 mM)

H2O : 50 mg/mL (109.03 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.45 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

LSKL, Inhibitor of Thrombospondin (TSP-1)TGF-β ReceptorTransforming growth factor beta receptorsTGF-β1TSP-1p-Smad2p-Smad3hepaticfibrosishydrocephalusLAPneurocognitiveBBBInhibitorinhibitorinhibit

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LSKL, Inhibitor of Thrombospondin (TSP-1)
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HY-P0299
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