TH1020
Based on 13 publication(s) in Google Scholar
TH1020 is a potent and selective toll-like receptor 5 (TLR5)/flagellin complex antagonist with an IC50 of 0.85 μM. TH1020 inhbits flagellin-induced TLR5 signaling. TH1020 is inactive against TLR2, TLR3, TLR4, TLR7 and TLR8.
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 1841460-82-9
- Formula: C23H15N7S2
- Molecular Weight:453.54
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) TH1020
More- Cancer Cell. 2024 Nov 11;42(11):1882-1897.e7. [Abstract]
- Gut. 2023 Nov;72(11):2112-2122. [Abstract]
- Exploration. 2025 Dec 18;5(6):20240396. [Abstract]
- Hepatology. 2025 Nov 7. [Abstract]
- Trends Biotechnol. 2025 Oct 30:S0167-7799(25)00401-9. [Abstract]
- Biomed Pharmacother. 2025 Sep 17:192:118569. [Abstract]
- Cell Rep. 2024 Sep 25:114785. [Abstract]
- Sci Rep. 2023 Oct 28;13(1):18490. [Abstract]
- PLoS Negl Trop Dis. 2023 Jan 27;17(1):e0011085. [Abstract]
- bioRxiv. 2025 Jun 15:2025.06.10.658497. [Abstract]
- Research Square Preprint. 2024 Dec 02.
- Patent. US20240366693A1.
- Research Square Preprint. 2023Dec 8.
Biological Activity
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TLR5 |
TH1020 inhibits the downstream signaling transduction mediated by the formation of the TLR5/Flagellin complex. TH1020 is suggested to compete with flagellin and disrupt its association with TLR5. TH1020 almost completely abolishes the TLR5-mediated TNF-α secretion at 0.37 μM[1].
The IL-17C secretion is almost completely abolished by TH1020 (0.5 μM) in bacterial strain C83901 infected IPEC-J2 cells[2].
Blocking TLR5 with TH1020 (0.5 μM) dramatically inhibits porcine beta-defensin (pBD)-2, claudin-1 and -2 mRNA expression in C83091 infected IPEC-J2 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1841460-82-9
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Appearance Solid
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Molecular Weight 453.54
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Formula C23H15N7S2
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Color Light yellow to yellow
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SMILES
C12=NC=NC(SC3=NN=C(N3CC4=CC=CC=C4)C5=CC=NC=C5)=C1SC6=NC=CC=C62
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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 2 years -20°C 1 year
Publications (13)
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Journal Impact Factor
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Most Recent
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Cancer Cell
Overcoming tyrosine kinase inhibitor resistance in lung cancer brain metastasis with CTLA4 blockade. [Abstract]2024 Nov 11;42(11):1882-1897.e7. PMID: 39423817 -
Gut
Roseburia intestinalis generated butyrate boosts anti-PD-1 efficacy in colorectal cancer by activating cytotoxic CD8+ T cells. [Abstract]2023 Nov;72(11):2112-2122. PMID: 37491158 -
Exploration
A Bioorthogonal and Programmable Bacterial Delivery System for Spatiotemporally Targeted Therapy of Solid Tumors. [Abstract]2025 Dec 18;5(6):20240396. PMID: 41476656 -
Hepatology
GPC3-based circular RNA vaccine suppresses hepatocellular carcinoma progression by activating adaptive immune responses. [Abstract]2025 Nov 7. PMID: 41201153 -
Trends Biotechnol
2025 Oct 30:S0167-7799(25)00401-9. PMID: 41173725 -
Biomed Pharmacother
Baicalin attenuates acetaminophen-induced acute liver injury through inhibiting TLR2-dependent neutrophil extracellular trap formation. [Abstract]2025 Sep 17:192:118569. PMID: 40967078 -
Cell Rep
Tyzzerella nexilis strains enriched in mobile genetic elements are involved in progressive multiple sclerosis. [Abstract]2024 Sep 25:114785. PMID: 39341204 -
Sci Rep
Hypersensitivity of myelinated A-fibers via toll-like receptor 5 promotes mechanical allodynia in tenascin-X-deficient mice associated with Ehlers-Danlos syndrome. [Abstract]2023 Oct 28;13(1):18490. PMID: 37898719 -
PLoS Negl Trop Dis
Toll-like receptor 2 mediates Acanthamoeba-induced allergic airway inflammatory response in mice. [Abstract]2023 Jan 27;17(1):e0011085. PMID: 36706056 -
bioRxiv
Ovarian Cancer Drives TLR5-Dependent Expansion of Myeloid Progenitors Through Systemic Dissemination of Ligands. [Abstract]2025 Jun 15:2025.06.10.658497. PMID: 40661568 -
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Solvent & Solubility
DMSO : 5 mg/mL (11.02 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)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.5 mg/mL (1.10 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.5 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 (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (279 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Lei Yan, et al. Pyrimidine Triazole Thioether Derivatives as Toll-Like Receptor 5 (TLR5)/Flagellin Complex Inhibitors. ChemMedChem. 2016 Apr 19;11(8):822-6. [Content Brief]
[2]. Yu Luo, et al. Toll-like Receptor 5-mediated IL-17C Expression in Intestinal Epithelial Cells Enhances Epithelial Host Defense Against F4 + ETEC Infection. Vet Res. 2019 Jun 20;50(1):48. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2049 mL | 11.0244 mL | 22.0488 mL | 55.1219 mL |
| 5 mM | 0.4410 mL | 2.2049 mL | 4.4098 mL | 11.0244 mL | |
| 10 mM | 0.2205 mL | 1.1024 mL | 2.2049 mL | 5.5122 mL |
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