Cu-CPT22

Catalog No.S8677

Cu-CPT22 Chemical Structure

Molecular Weight(MW): 362.37

CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM while no significant inhibition to TLR2/6. It demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4).

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Choose Selective TLR Inhibitors

Biological Activity

Description CU-CPT22 shows dose-dependent inhibitory effects blocking Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 ± 0.09 µM while no significant inhibition to TLR2/6. It demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4).
Targets
TLR1/2 [1]
(Cell-free)
0.58 μM
In vitro

CU-CPT22 can compete with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with high inhibitory activity and specificity. The inhibition constant (Ki) is 0.41 ± 0.07 µM. CU-CPT22 inhibits TLR1/2 signaling without affecting other TLRs, showing it is highly selective in intact cells. It has no significant cytotoxicity at various concentrations up to 100 µM in RAW 264.7 cells using MTT assay. Kinase profiling shows that CU-CPT22 demonstrates minimal non-specific inhibition against a panel of 10 representative kinases (PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4). CU-CPT22 suppresses TLR1/2-mediated inflammation response. It inhibits about 60% of TNF-α and 95% of IL-1β at 8 µM in the RAW 264.7 cells[1].

In vivo Cu-CPT22 administered before myocardial infarction (MI) significantly suppresses MI-induced upregulation of kidney injury molecule-1 (KIM-1), TLR2, TLR4, MyD88, and chemokine (C-C motif) ligand 2 levels and activation of NF-κB, whereas neutrophil gelatinase-associated lipocalin (NGAL) levels and IL-6 and TNF-α expression levels are unchanged[2].

Protocol

Cell Research:

[3]

+ Expand
  • Cell lines: MUTZ-3-derived Langerhans cells (MUTZ-LCs)
  • Concentrations: 10 and 25 μM
  • Incubation Time: 1 h
  • Method:

    MUTZ-LCs are seeded in alpha medium without supple-ments and exposed to different microbial and pro-inflammatorystimuli for 24 h (2.5 × 105 cells/ml): 1 μg/ml Pam3CSK4, 1 μg/mlPam2CSK4, 1 μg/ml poly(A:U), 1 μg/ml poly(I:C), 1 μg/ml ultrapurelipopolysaccharide (LPS) from Escherichia coli serotype 0111:B4, 50 ng/ml rh-TNF-α, 30 ng/ml rh-IL-1β, or a cytokine maturation cocktail(CMC) consisting of 50 ng/ml rh-TNF-α, 25 ng/ml rh-IL-1β,100 ng/ml rh-IL-6 and 1 μg/ml PGE2. Cytokines produced in E. coli, contained low endotoxinlevels (≤1.0 EU/μg cytokine) as determined by Limulus Amebo-cyte Lysate (LAL) assay. As control MUTZ-LCs (2.5 × 105 cells/ml) are maintained for 24 hor 48 h in alpha medium only. The TLR2/1 antagonist CU-CPT22 is applied 1 h before stimulation with Pam3CSK4 and Pam2CSK4, respectively.


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: Male LETO and OLETF rats
  • Formulation: 75% DMSO plus 25% distilled water
  • Dosages: 3 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 72 mg/mL (198.69 mM)
Ethanol 9 mg/mL (24.83 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 362.37
Formula

C19H22O7

CAS No. 1416324-85-0
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID