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Diprovocim

Cat. No. M25485

All AbMole products are for research use only, cannot be used for human consumption.

Diprovocim Structure

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Quality Control & Documentation
Biological Activity

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.

Chemical Information
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
References

[1] Xianyang Wang, et al. Eur J Med Chem. Identification and immunological evaluation of novel TLR2 agonists through structural optimization of Diprovocim

[2] Ming-Hsiu Yang, et al. J Med Chem. Next-Generation Diprovocims with Potent Human and Murine TLR1/TLR2 Agonist Activity That Activate the Innate and Adaptive Immune Response

[3] Lijing Su, et al. J Med Chem. Structural Basis of TLR2/TLR1 Activation by the Synthetic Agonist Diprovocim

[4] Matthew D Morin, et al. J Am Chem Soc. Diprovocims: A New and Exceptionally Potent Class of Toll-like Receptor Agonists

[5] Ying Wang, et al. Proc Natl Acad Sci U S A. Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti-PD-L1 to eliminate melanoma in mice

[6] Ying Wang, et al. Proc Natl Acad Sci U S A. Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti-PD-L1 to eliminate melanoma in mice

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Keywords: Diprovocim supplier, TLR, inhibitors, activators

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