Home Immunology & Inflammation TLR inhibitor Cu-CPT22

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Cu-CPT22 TLR inhibitor

Cat.No.S8677

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).
Cu-CPT22 TLR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 362.37

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Quality Control

Batch: S867701 DMSO]72 mg/mL]false]Ethanol]9 mg/mL]false]Water]Insoluble]false Purity: 99.78%
99.78

Chemical Information, Storage & Stability

Molecular Weight 362.37 Formula

C19H22O7

 Storage (From the date of receipt)
CAS No. 1416324-85-0 -- Storage of Stock Solutions

Synonyms N/A Smiles CCCCCCOC(=O)C1=CC2=C(C(=C(O)C(=C2)OC)O)C(=O)C(=C1)O

Solubility

In vitro
Batch:

DMSO : 72 mg/mL (198.69 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 9 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
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].
References

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