Art. -Nr.: HY-123942

Diprovocim

14 Cited Publications

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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.

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Reinheit: 98.82%
CAS. Nr.: 2170867-89-5
Formel: C₅₆H₅₆N₆O₆
Molecular Weight:909.08

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Diprovocim Chemical Structure

CAS. Nr.: 2170867-89-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (14)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]^[2]

TLR1

TLR2

p38 MAPK

NF-κB

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen :

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

Alle p38 MAPK Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
THP-1	EC₅₀	110 pM Compound: Diprovocim	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	[PMID: 30852386]

In Vitro

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.

Western Blot Analysis^[2]

Cell Line:

THP-1 cells and mouse peritoneal macrophages
Concentration:

5 nM in THP-1 and 500 nM in mouse peritoneal macrophages
Incubation Time:

15, 30, 60, 120 mins
Result:

Induced phosphorylation of IKKα, IKKβ, p38, JNK, and ERK, as well as degradation of IκBα.

In Vivo

Diprovocim (10 mg/kg) uses as an adjuvant and mixed with ovalbumin (OVA; 100 μg) by i.m. induces similar levels of serum OVA-specific IgG after 14 days^[2].
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.

Animal Model:

WT or Tlr2^−/− C57BL/6J mice^[2]
Dosage:

10 mg/kg
Administration:

IM
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

CAS. Nr. 2170867-89-5
Appearance Solid
Molecular Weight 909.08
Formel C₅₆H₅₆N₆O₆
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (14)

All Bio/Physico-chemical AssayIHCRT-PCRCell Proliferation/Viability Assay

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Journal Impact Factor

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.
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.
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

Association of IL-9 Cytokines with Hepatic Injury in Echinococcus granulosus Infection. [Abstract]

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
Aquac Rep

2025 Sep 15.
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
SSRN

2025 Jun 2.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.1000 mL

5.5001 mL

11.0001 mL

5 mM

0.2200 mL

1.1000 mL

2.2000 mL

10 mM

0.1100 mL

0.5500 mL

1.1000 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 2.5 mg/mL (2.75 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

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.

Protocol 1

Add each solvent one by one: 50% PEG300 50% Saline

Solubility: 2 mg/mL (2.20 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
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

14 Cited Publications

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Diprovocim

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Publications Citing Use of MedChemExpress (MCE) Diprovocim

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen

Alle TNF Receptor Isoform-spezifische Produkte anzeigen

Alle p38 MAPK Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (14)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Diprovocim Related Classifications

HY-123942 Related Classifications