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Lck Inhibitor

Catalog No.
A3539
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Lck inhibitor
Grouped product items
SizePriceStock Qty
5mg
$183.00
Ship with 10-15 days
10mg
$292.00
Ship with 10-15 days
50mg
$1,167.00
Ship with 10-15 days
100mg
$2,095.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

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Background

Lck Inhibitor is a small-molecule inhibitor of with IC50 value of 7 nM [1].
The lymphocyte specific kinase which expressed in NK cells and T-cells is a member of the Src kinase family. It takes participate in the T-cell receptor (TCR) signal transduction and affects the expression of genes associated with cell proliferation, cytokine release and T-cell survival. Therefore small-molecule inhibitors of Lck with potent activities and bioavailable efficacies have been designed and developed as therapeutic agents for the treatment for T-cell-mediated autoimmune and organ transplant rejection [1].
Lck Inhibitor showed high selectivity against Lck over another Src family kinase Src and the kinases related to inflammation and angiogenesis such as p38 and VEGFR-2 with IC50 values of 0.12, > 10 and 5.1 μM, respectively. Lck Inhibitor also showed more than 1000-fold greater selectivity over CDK, MAPK and the RSK family. In cultured human mixed lymphocytes, the inhibitor significantly suppressed the activation of T-cells with IC50 value of 47 nM. Besides that, this compound inhibited IL-2 secretion induced by T-cell receptor with IC50 value of 0.46 μM. The good potency and selectivity of the Lck Inhibitor were due to the critical aniline side chain within a N-methylpiperazine moiety. It extended to the ATP-binding pocket of the enzyme and formed hydrogen bond interactions with the linker region [1].
In rats model with arthritis induced by the injection of porcine type II collagen, oral administration of the compound dose-dependently suppressed the inflammation with ED50 value of 3.2 mg/kg. While in the adjuvant-induced arthritis model, oral administration of Lck Inhibitor also displayed significant anti- arthritis effects with ED50 value of 24 mg/kg [1].
References:
[1] Martin M W, Newcomb J, Nunes J J, et al. Structure-Based Design of Novel 2-Amino-6-phenyl-pyrimido [5', 4': 5, 6] pyrimido [1, 2-a] benzimidazol-5 (6 H)-ones as Potent and Orally Active Inhibitors of Lymphocyte Specific Kinase (Lck): Synthesis, SAR, and In Vivo Anti-Inflammatory Activity. Journal of medicinal chemistry, 2008, 51(6): 1637-1648.   

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt530.62
Cas No.847950-09-8
FormulaC31H30N8O
SolubilitySoluble in DMSO
Chemical Name6-(2,6-dimethylphenyl)-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)benzo[4,5]imidazo[1,2-a]pyrimido[5,4-e]pyrimidin-5(6H)-one
SDFDownload SDF
Canonical SMILESO=C1N(C2=C(C([H])([H])[H])C([H])=C([H])C([H])=C2C([H])([H])[H])C3=NC4=C([H])C([H])=C([H])C([H])=C4N3C5=NC(N([H])C6=C([H])C([H])=C(C([H])=C6[H])N7C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C7([H])[H])=NC([H])=C51
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Biological Activity

Description Lck Inhibitor is a cell-permeable and ATP-competitive inhibitor of Lck with IC50 values of < 1 nM, 2 nM, 70 nM, 1.57 µM and 1.98 µM for Lck (64-509), Lckcd, Src, Kdr and Tie-2, respectively.
Targets Lck (64-509) Lckcd Src Kdr Tie-2  
IC50 < 1 nM 2 nM 70 nM 1.57 µM 1.98 µM  

Quality Control

Quality Control & MSDS

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Chemical structure

Lck Inhibitor