LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a tetrapeptide extracted from LAP-TGFβ and is a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits/disrupts the binding of TSP-1 to LAP and reduces renal interstitial fibrosis and liver fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits subarachnoid fibrosis by inhibiting TSP-1-mediated TGF-β1 activity, preventing the occurrence of chronic hydrocephalus and improving long-term neurocognition after subarachnoid hemorrhage. aware of defects. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA readily crosses the BBB (blood-brain barrier).

Physicochemical Properties

Molecular Formula	C23H43F3N6O7
Molecular Weight	572.62
Exact Mass	572.314
CAS #	2828433-17-4
Related CAS #	LSKL, Inhibitor of Thrombospondin (TSP-1);283609-79-0
PubChem CID	145707571
Appearance	White to off-white solid powder
Hydrogen Bond Donor Count	8
Hydrogen Bond Acceptor Count	12
Rotatable Bond Count	16
Heavy Atom Count	39
Complexity	697
Defined Atom Stereocenter Count	4
SMILES	[C@@H](C(=O)N)(CC(C)C)NC(=O)[C@@H](NC([C@H](CO)NC(=O)[C@@H](N)CC(C)C)=O)CCCCN.OC(=O)C(F)(F)F
InChi Key	FULCVSARTMWAGA-SITLLQIKSA-N
InChi Code	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
Chemical Name	(2S)-6-amino-N-[(2S)-1-amino-4-methyl-1-oxopentan-2-yl]-2-[[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-3-hydroxypropanoyl]amino]hexanamide;2,2,2-trifluoroacetic acid
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	TGF-β1[1]
ln Vitro	The activation of TGF-β from its latent state is attributed to the interaction between the KTFR sequence from ADAMTS1 and the LSKL, Inhibitor of Thrombospondin (TSP-1) (LSKL peptide). Three salt bridges and two hydrogen bonds define a stable binding mechanism between the ADAMTS1 KTFR sequence and LSKL, an inhibitor of thrombospondin (TSP-1)[2].
ln Vivo	In male Sprague-Dawley rats, intraperitoneal administration of LSKL, Inhibitor of Thrombospondin (TSP-1) (1 mg/kg), attenuates ventriculomegaly, and effectively reduces hydrocephalus. The administration of LSKL, an inhibitor of thrombospondin (TSP-1), suppresses TGF-β1 activity and the ensuing Smad2/3 signaling[1]. ?LSKL, or Inhibitor of Thrombospondin (TSP-1) (30 mg/kg, ip), effectively prevents partial hepatectomy-induced activation of the transforming growth factor (TGF) β-Smad signal. Thrombospondin (TSP-1) inhibitor LSKL effectively inhibits TGF-β-Smad signal activation by opposing TSP-1, but not by lowering TSP-1 protein expression. Following a hepatectomy, hepatocyte proliferation is accelerated by LSKL, an inhibitor of thrombospondin (TSP-1)[3].
Animal Protocol	Animal/Disease Models: 103 male SD (Sprague-Dawley) rats (6 weeks of age; 160-180 g) with subarachnoid hemorrhage (SAH)[1] Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Was protective against subarachnoid fibrosis, attenuated ventriculomegaly and effectively suppressed hydrocephalus.
References	[1]. 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. [2]. 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. [3]. 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.

Solubility Data

Solubility (In Vitro)

DMSO: 250 mg/mL (436.59 mM) H2O: 100 mg/mL (174.64 mM）

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (3.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 3: 100 mg/mL (174.64 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.7464 mL	8.7318 mL	17.4636 mL
	5 mM	0.3493 mL	1.7464 mL	3.4927 mL
	10 mM	0.1746 mL	0.8732 mL	1.7464 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.