Diprovocim
Based on 14 publication(s) in Google Scholar
Diprovocim is a potent TLR1/TLR2 agonist. Diprovocim elicits full agonist activity in human THP-1 cells (EC50=110 pM). Diprovocim stimulates the release of TNF-α from mouse macrophages (EC50=1.3 nM). Diprovocim activates downstream MAPK and NF-κB signaling pathway. Diprovocim displays strong adjuvant activity in mice, particularly abetting cellular immune responses.
For research use only. We do not sell to patients.
- Purity: 98.82%
- CAS No.: 2170867-89-5
- Formula: C56H56N6O6
- Molecular Weight:909.08
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
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Publications Citing Use of MedChemExpress (MCE) Diprovocim
More- J Adv Res. 2025 Jun 16:S2090-1232(25)00444-8. [Abstract]
- J Adv Res. 2025 Mar:69:545-563. [Abstract]
- J Neuroinflammation. 2026 Jan 22;23(1):68. [Abstract]
- Food Chem X. 2026 Mar 26:35:103793. [Abstract]
- J Med Chem. 2026 Mar 12;69(5):6158-6178. [Abstract]
- J Med Chem. 2024 Aug 8;67(15):12932-12944. [Abstract]
- Cell Biol Toxicol. 2025 Apr 5;41(1):67. [Abstract]
- Biomolecules. 2024 Aug 14;14(8):1007. [Abstract]
- Int Immunopharmacol. 2023 Oct 9;124(Pt B):111034. [Abstract]
- Neuropharmacology. 2024 Aug 29:110136. [Abstract]
- Mol Neurobiol. 2025 Jun;62(6):8013-8037. [Abstract]
- Aquac Rep. 2025 Sep 15.
- Biomol Ther (Seoul). 2026 Mar 1;34(2):423-433. [Abstract]
- SSRN. 2025 Jun 2.
Customer Validation & Images
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IHC
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IHC
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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RT-PCR
Biological Activity
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TLR1 |
TLR2 |
p38 MAPK |
NF-κB |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| THP-1 | EC50 |
110 pM
Compound: Diprovocim
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Agonist activity at TLR1/2 in human THP-1 cells assessed as increase in TNF-alpha release incubated for 4 hrs by ELISA
Agonist activity at TLR1/2 in human THP-1 cells assessed as increase in TNF-alpha release incubated for 4 hrs by ELISA
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[PMID: 30852386] |
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[2].
Diprovocim (0.01-10000 nM; 4 hours) induces dose-dependent TNF production by THP-1 cells (EC50=110 pM) and human peripheral blood mononuclear cells (PBMC) (EC50=875 pM) and by mouse peritoneal macrophages (EC50=1.3 nM) and bone marrow-derived dendritic cells (BMDC) (EC50=6.7 nM). In addition to TNF, Diprovocim induced IL-6 production by mouse BMDC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:THP-1 cells and mouse peritoneal macrophages
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Concentration:5 nM in THP-1 and 500 nM in mouse peritoneal macrophages
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Incubation Time:15, 30, 60, 120 mins
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Result:Induced phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα.
Diprovocim (10 mg/kg; i.m.) mixed with ovalbumin (OVA; 100 μg) before inoculation with B16-OVA cells immunizes significantly slows tumor growth rate but failed to prolong survival relative to OVA alone after 7 days[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:WT or Tlr2−/− C57BL/6J mice[2]
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Dosage:10 mg/kg
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Administration:IM
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Result:Induced similar levels of serum OVA-specific IgG, which were highly elevated compared with levels induced by immunization with OVA plus vehicle by i.m. with 100 μg OVA mixed with this drug.
Chemical Information
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CAS No. 2170867-89-5
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Appearance Solid
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Molecular Weight 909.08
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Formula C56H56N6O6
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Color White to off-white
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SMILES
O=C(N1C[C@@H](C(N[C@@H]2[C@@H](C3=CC=CC=C3)C2)=O)[C@H](C(N[C@@H]4[C@@H](C5=CC=CC=C5)C4)=O)C1)C6=CC=C(C(N7C[C@@H](C(N[C@@H]8[C@@H](C9=CC=CC=C9)C8)=O)[C@H](C(N[C@@H]%10[C@@H](C%11=CC=CC=C%11)C%10)=O)C7)=O)C=C6
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (14)
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Journal Impact Factor
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Most Recent
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J Adv Res
Lactobacillus johnsonii-derived extracellular vesicles carrying GAPDH protect against ulcerative colitis through modulating macrophage polarization. [Abstract]2025 Jun 16:S2090-1232(25)00444-8. PMID: 40533059 -
J Adv Res
Extracellular vesicles derived from Lactobacillus johnsonii promote gut barrier homeostasis by enhancing M2 macrophage polarization. [Abstract]2025 Mar:69:545-563. PMID: 38508446
Diprovocim purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Mar:69:545-563. [Abstract]
Diprovocim (500 nM, 12 h) co-incubated with LjEVs also obviously reduced the gene abundance of Arg1, IL-4/10, and CD206 in J774A.1 cells.
Diprovocim purchased from MedChemExpress. Usage Cited in: J Adv Res. 2025 Mar:69:545-563. [Abstract]
Diprovocim (500 nM, 12 h) and LjEVs co-pretreated pretreated J774A.1 cells significantly increased IL-1β and TNF-α mRNA expression and decreased ZO-1 and Occludin mRNA expression in MODE-K cells.
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J Neuroinflammation
Esketamine alleviates COPD-depression comorbidity in rats via MAPK/NF-κB inhibition and gut-lung-brain axis modulation. [Abstract]2026 Jan 22;23(1):68. PMID: 41572340
Diprovocim purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2026 Jan 22;23(1):68. [Abstract]
Representative hippocampal sections showing HE staining, TUNEL assay, and IBA-1 immunofluorescence, with quantification of pathological scores, apoptotic index (TUNEL-positive cells), and microglial activation (IBA-1-positive cells and mean fluorescence intensity) (n = 3). Con, control; CY, comorbid model; CYK, CY rats treated with Esketamine; CYKD, CY rats treated with Esketamine and Diprovocim (intraperitoneally at 1 mg/kg every 3 days for 14 days).
Diprovocim purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2026 Jan 22;23(1):68. [Abstract]
Immunohistochemistry corroborated these findings: CY rats exhibited stronger and more widespread staining for p-p38, p-JNK, and p-p65, reductions were evident in CYK rats, and Diprovocim (intraperitoneally at 1 mg/kg every 3 days for 14 days) again reinstated the heightened expression pattern.
Diprovocim purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2026 Jan 22;23(1):68. [Abstract]
In grouped assays, CSE decreased viability, Esketamine restored it, Diprovocim (500 nM, final 2 h) further suppressed it, and combined treatment diminished the protective effect of esketamine.
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Food Chem X
'Fengtang' plum seed waste: Phytochemicals and anti-inflammatory effects in vivo and in vitro. [Abstract]2026 Mar 26:35:103793. PMID: 41953656 -
J Med Chem
From Functional Group and Metabolite Analysis to Rational Design: Discovery of BXY-14 as a Highly Potent TLR2 Agonist with Enhanced Vaccine Adjuvants and Cancer Immunotherapy. [Abstract]2026 Mar 12;69(5):6158-6178. PMID: 41764631 -
J Med Chem
The Development of a Highly Potent and Selective Human Toll-like Receptor 2 Agonist: Synthesis and Biological Evaluation of CaLGL-1 and Its Derivatives. [Abstract]2024 Aug 8;67(15):12932-12944. PMID: 38996365 -
Cell Biol Toxicol
Targeting B4GALT3 in BMSCs-EVs for Therapeutic Control of HCC via NF-κB pathway inhibition. [Abstract]2025 Apr 5;41(1):67. PMID: 40186771 -
Biomolecules
2024 Aug 14;14(8):1007. PMID: 39199394 -
Int Immunopharmacol
Research of STEAP3 interaction with Rab7A and RACK1 to modulate the MAPK and JAK/STAT signaling in Osteoarthritis. [Abstract]2023 Oct 9;124(Pt B):111034. PMID: 37820423 -
Neuropharmacology
HIV1 gp120 activates microglia via TLR2-nf-κb signaling to up-regulate inflammatory cytokine expression and induce neuropathic pain. [Abstract]2024 Aug 29:110136. PMID: 39216684 -
Mol Neurobiol
Activation of NR2A-Wnt-TLR2 Signaling Axis in Satellite Glial Cells of the Dorsal Root Ganglion Contributes to Neuropathic Pain Induced by Nerve Injury in Diabetic Mice. [Abstract]2025 Jun;62(6):8013-8037. PMID: 39964585 -
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Biomol Ther (Seoul)
Crebanine Protects HUVECs from LPS-Induced Inflammation and Oxidative Stress by Suppressing NF-κB Pathway. [Abstract]2026 Mar 1;34(2):423-433. PMID: 41755781 -
Solvent & Solubility
DMSO : 33.33 mg/mL (36.66 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 2 mg/mL (2.20 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Matthew D Morin, et al. Diprovocims: A New and Exceptionally Potent Class of Toll-like Receptor Agonists. J Am Chem Soc. 2018 Oct 31;140(43):14440-14454. [Content Brief]
[2]. Ying Wang, et al. Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti-PD-L1 to eliminate melanoma in mice. Proc Natl Acad Sci U S A. 2018 Sep 11;115(37):E8698-E8706. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.1000 mL | 5.5001 mL | 11.0001 mL | 27.5003 mL |
| 5 mM | 0.2200 mL | 1.1000 mL | 2.2000 mL | 5.5001 mL | |
| 10 mM | 0.1100 mL | 0.5500 mL | 1.1000 mL | 2.7500 mL | |
| 15 mM | 0.0733 mL | 0.3667 mL | 0.7333 mL | 1.8334 mL | |
| 20 mM | 0.0550 mL | 0.2750 mL | 0.5500 mL | 1.3750 mL | |
| 25 mM | 0.0440 mL | 0.2200 mL | 0.4400 mL | 1.1000 mL | |
| 30 mM | 0.0367 mL | 0.1833 mL | 0.3667 mL | 0.9167 mL |
Diprovocim Related Classifications
HY-123942 Related Classifications
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