CU-CPT22 |
| Catalog No.GC14254 |
CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58µM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1416324-85-0
Sample solution is provided at 25 µL, 10mM.
CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58µM[1].
CU-CPT22 (4-8µM) inhibited NO production in RAW 264.7 macrophages in a dose-dependent manner, and CU-CPT22 at a concentration of 8µM could inhibit approximately 60% of TNF-α and 95% of IL-1β[1]. CU-CPT22 (2-8µM) blocks the increased expression of inflammatory cytokines IL6 and TNF-α produced after TLR2 activation caused by viral infection of N9 microglia and inhibits TLR2 signaling[2].
CU-CPT22 (3mg/kg) inhibits the TLR2 pathway, improves autonomic dysfunction symptoms in MPTP mice, and protects the vagus nerve from p-α-syn-mediated myelin destruction in Parkinson’s disease[3]. In a colorectal cancer tumor model, CU-CPT22 (2.5mg/kg) significantly reduced the effect of oxaliplatin, leading to a decrease in tumor-infiltrating immune cells, including CD4+, CD8+, and IFNγ+ CD8+ cells[4]. CU-CPT22 (3mg/kg) administered before Myocardial Infarction significantly suppressed Myocardial Infarction-induced upregulation of KIM-1, TLR2, TLR4, MyD88, and chemokine (C-C motif) ligand 2 levels and activation of NF-κB, whereas NGAL levels and IL-6 and TNF-α expression levels were unchanged[5].
References:
[1]. Cheng K, Wang X, Zhang S, et al. Discovery of small molecule inhibitors of the TLR1-TLR2 complex[J]. Angewandte Chemie (International ed. in English), 2012, 51(49): 12246.
[2]. Sharma K B, Chhabra S, Aggarwal S, et al. Proteomic landscape of Japanese encephalitis virus-infected fibroblasts[J]. Journal of General Virology, 2021, 102(9): 001657.
[3]. Li Y, Tong Q, Wang Y, et al. Phosphorylated α-synuclein deposited in Schwann cells interacting with TLR2 mediates cell damage and induces Parkinson’s disease autonomic dysfunction[J]. Cell Death Discovery, 2024, 10(1): 52.
[4] Huang K C Y, Ke T W, Chen J Y, et al. Dysfunctional TLR1 reduces the therapeutic efficacy of chemotherapy by attenuating HMGB1-mediated antitumor immunity in locally advanced colorectal cancer[J]. Scientific Reports, 2023, 13(1): 19440.
[5] Ohno K, Kuno A, Murase H, et al. Diabetes increases the susceptibility to acute kidney injury after myocardial infarction through augmented activation of renal Toll-like receptors in rats[J]. American Journal of Physiology-Heart and Circulatory Physiology, 2017, 313(6): H1130-H1142.
| Cell experiment [1]: | |
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Cell lines |
N9 cells |
|
Preparation Method |
N9 cells were treated with DMSO or 2-8µM CU-CPT22 for 24h. |
|
Reaction Conditions |
2-8µM; 24h |
|
Applications |
CU-CPT22 blocks the increased expression of inflammatory cytokines IL6 and TNF-α produced after TLR2 activation caused by viral infection of N9 microglia and inhibits TLR2 signaling. |
| Animal experiment [2]: | |
|
Animal models |
MPTP(1-methyl-4phenyl-1,2,3,6-tetrahydropyridine) modle |
|
Preparation Method |
The C57BL/6 mice were divided into control, MPT, CU-CPT22, and MPTP + CU-CPT22 groups using a random number table. MPTP (20mg/kg) was injected twice a week for 5 weeks, and an equal amount of saline was administered to the control group. CU-CPT22 (3mg/kg) was administered daily for 35 days. |
|
Dosage form |
3mg/kg; ip; 35 days |
|
Applications |
CU-CPT22 improves autonomic dysfunction and protects the vagus nerve from p-α-syn-mediated myelin destruction in Parkinson’s disease. |
| Kinase experiment [3]: | |
|
Preparation Method |
CU-CPT22 was dissolved in DMSO at 10mM and tested at concentrations of 5μM. Each compound was first evaluated for false positive against split luciferase. If they did not inhibit luciferase control, then they were profiled in duplicate against the following kinases: PDGFRB, MET, DDR2, SRC, MAPK1, PAK1, AKT1, PKC-γ, CAMK1, and PLK4. |
|
Reaction Conditions |
5μM |
|
Applications |
CU-CPT22 demonstrated 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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References: |
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| Cas No. | 1416324-85-0 | SDF | |
| Chemical Name | hexyl 3,4,5-trihydroxy-2-methoxy-6-oxo-6H-benzo[7]annulene-8-carboxylate | ||
| Canonical SMILES | CCCCCCOC(C(C=C1C=C(OC)C(O)=C(O)C1=C2O)=CC2=O)=O | ||
| Formula | C19H22O7 | M.Wt | 362.37 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7596 mL | 13.7981 mL | 27.5961 mL |
| 5 mM | 551.9 μL | 2.7596 mL | 5.5192 mL |
| 10 mM | 276 μL | 1.3798 mL | 2.7596 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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