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Diprovocim is a potent human and mouse Toll-like receptor (TLR)1/TLR2 agonist, which exhibited an EC50 of 110 pM in human THP-1 cells and 1.3 nM in primary mouse peritoneal macrophages. Diprovocim activates downstream MAPK and NF-κB signaling pathway.
Diprovocim (5 nM in THP-1 and 500 nM in mouse peritoneal macrophage; 15-120 mins) induces phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα in THP-1 cells and mouse peritoneal macrophages.
In mice, Diprovocim-adjuvanted ovalbumin immunization promoted antigen-specific humoral and CTL responses and synergized with anti-PD-L1 treatment to inhibit tumor growth, generating long-term antitumor memory, curing or prolonging survival of mice engrafted with the murine melanoma B16-OVA. Diprovocim induced greater frequencies of tumor-infiltrating leukocytes than alum, of which CD8 T cells were necessary for the antitumor effect of immunization plus anti-PD-L1 treatment.
| Molecular Weight | 909.08 |
| Formula | C56H56N6O6 |
| CAS Number | 2170867-89-5 |
| Solubility (25°C) | DMSO 20 mg/mL (ultrasonic and warming) |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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