Cat. No.: HY-139397

TJ-M2010-5

34 Cited Publications

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Based on 34 publication(s) in Google Scholar

TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI).

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.94%
CAS No.: 1357471-57-8
Formule: C₂₃H₂₆N₄OS
Masse moléculaire:406.54

Stockage:

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)

TJ-M2010-5 Chemical Structure

CAS No.: 1357471-57-8

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

Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (34)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

TJ-M2010-5 is a MyD88 inhibitor that binds to the TIR domain of MyD88 to interfere with its homodimerization, and the TLR/MyD88 signal pathway^[1]^[2]. TJ-M2010-5 can be used for the research of myocardial ischemia/reperfusion injury (MIRI)^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
Peritoneal macrophage	IC₅₀	10.25 μM Compound: 6; TJ-M2010-5	Antiinflammatory activity in ICR mouse primary peritoneal macrophages assessed as inhibition of LPS-induced IL-6 production preincubated for 2 hrs followed by LPS stimulation and measured after 22 hrs by ELISA Antiinflammatory activity in ICR mouse primary peritoneal macrophages assessed as inhibition of LPS-induced IL-6 production preincubated for 2 hrs followed by LPS stimulation and measured after 22 hrs by ELISA	[PMID: 30342423]
Peritoneal macrophage	IC₅₀	11.88 μM Compound: 6; TJ-M2010-5	Antiinflammatory activity in ICR mouse primary peritoneal macrophages assessed as inhibition of LPS-induced TNFalpha production preincubated for 2 hrs followed by LPS stimulation and measured after 22 hrs by ELISA Antiinflammatory activity in ICR mouse primary peritoneal macrophages assessed as inhibition of LPS-induced TNFalpha production preincubated for 2 hrs followed by LPS stimulation and measured after 22 hrs by ELISA	[PMID: 30342423]

In Vitro

TJ-M2010-5 (40 μM) inhibits MyD88 homodimerization in transfected HEK293 cells in a concentration-dependent manner and suppresses MyD88 signaling in LPS (100 ng/mL)-responsive RAW 264.7 cells in vitro^[1].
? TJ-M2010-5 (5-30 μM) prevents B cell proliferation and induces B cells apoptosis after stimulation with R848 (500 ng/mL)^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[3]

Cell Line:

Purified B cells
Concentration:

0 μM, 5 μM, 10 μM, 20 μM and 30 μM
Incubation Time:

48 hours
Result:

Inhibited the viability of B cells with or without the stimulation of CD40L.

In Vivo

TJ-M2010-5 treatment statistically significantly reduces AOM/DSS-induced colitis and completely prevented CAC development with less related body mass loss, results in 0% mortality of treated mice, decreases cell proliferation, and increased apoptosis in colon tissue in a 10-week CAC mouse model^[1].
? TJ-M2010-5 statistically significantly decreases TNF-α, IL-6, G-CSF, MIP-1β, IL-11, IL-17A, IL-22, and IL-23 serum concentrations in mice at both two and seven weeks postinduction, as well as TGF-β1 serum levels at seven weeks postinduction^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Female BalB/c mice (6–8 weeks old) ^[1]
Dosage:

50 mg/kg
Administration:

Treated i.p. daily beginning two days before the first dextran sodium sulfate (DSS) administration throughout a 10-week observation period.
Result:

Significantly prevented inflammation/CAC-related body weight loss and mortality (0% vs 53% in the control group).

Chemical Information

CAS No. 1357471-57-8
Appearance Solid
Masse moléculaire 406.54
Formule C₂₃H₂₆N₄OS
Color White to light yellow
SMILES

O=C(NC1=NC(C2=CC=CC=C2)=CS1)CCN3CCN(CC4=CC=CC=C4)CC3
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, protect from light, stored under nitrogen

* In solvent : -80°C, 2 years; -20°C, 1 year (protect from light, stored under nitrogen)

Publications (34)

All ELISAIn Vivo Efficacy StudyWBIFRT-PCR

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Journal Impact Factor

Immunity

A TLR4-dependent fibroblast-monocyte axis in tumor-draining lymph nodes contributes to metastasis in triple-negative breast cancer. [Abstract]

2025 Sep 15:S1074-7613(25)00378-4. PMID: 40957419
Adv Funct Mater

2025 Aug 3.

TJ-M2010-5 purchased from MedChemExpress. Usage Cited in: Adv Funct Mater. 2025 Aug 3.

Gene expression of IFN-β and TNF-α in RAW 264.7 cells incubated with 100 µg/mL M-BSA@PSiNPs or 100 µg/mL M-BSA for 6 h in the presence of 40 µM TJ-M2010-5 (TJ-M) or 20 µM TFA, respectively.
Nat Commun

Inflammatory disease progression shapes nanoparticle biomolecular corona-mediated immune activation profiles. [Abstract]

2025 Jan 22;16(1):924. PMID: 39843415

TJ-M2010-5 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Jan 22;16(1):924. [Abstract]

TJ-M2010-5 (5 μM; 48 h). TNFɑ secretions from macrophages treated with PLGA NP coronas in the presence or absence of TJ-m2010-5, a MyD88 inhibitor at 30 µM.
Natl Sci Rev

Combining cisplatin and a STING agonist into one molecule for metalloimmunotherapy of cancer. [Abstract]

2024 Jan 17;11(1):nwae020. PMID: 38332843
Trends Biotechnol

Synthetic M13 phage engagers expand CAR-T cell antigen recognition to overcome tumor heterogeneity. [Abstract]

2026 Mar 28:S0167-7799(26)00047-8. PMID: 41904099
Environ Sci Technol

Poly- and Perfluoroalkyl Substances Induce Immunotoxicity via the TLR Pathway in Zebrafish: Links to Carbon Chain Length. [Abstract]

2023 Apr 18;57(15):6139-6149. PMID: 37017313
EBioMedicine

Preclinical characterisation of the protective capacity of an anti-nucleoprotein hRSV monoclonal antibody. [Abstract]

2026 Jan:123:106104. PMID: 41483686
Angiogenesis

G3BP1 maintains endothelial barrier integrity through dual mechanisms: direct stabilization of junction protein mRNAs and suppression of the inflammatory MYD88-ARNO-ARF6 pathway. [Abstract]

2025 Aug 25;28(4):46. PMID: 40855241

TJ-M2010-5 purchased from MedChemExpress. Usage Cited in: Angiogenesis. 2025 Aug 25;28(4):46. [Abstract]

TJ-M2010-5 (TJM; 50 mg/kg; ip). Gross lung morphology and EBD extravasation in G3bp1^fl/fl and G3bp1^CKO mice after LPS challenge (10 mg/kg) for 6 h with or without TJM pre-treatment for seven days (50 mg/kg).

TJ-M2010-5 purchased from MedChemExpress. Usage Cited in: Angiogenesis. 2025 Aug 25;28(4):46. [Abstract]

TJ-M2010-5 (TJM; 50 mg/kg; ip). Western blots of relative VE-cadherin and p120 protein levels normalized to β-actin in lung tissues from G3bp1^fl/fl and G3bp1^CKO mice treated with LPS and either vehicle or TJM.

TJ-M2010-5 purchased from MedChemExpress. Usage Cited in: Angiogenesis. 2025 Aug 25;28(4):46. [Abstract]

TJ-M2010-5 (TJM; 50 mg/kg; ip). Immunofluorescence staining of p120 (green) and CD31 (red) in lung sections.
Proc Natl Acad Sci U S A

MyD88 knockdown by RNAi prevents bacterial stimulation of tubeworm metamorphosis. [Abstract]

2025 Jun 10;122(23):e2505805122. PMID: 40455987
Int J Biol Macromol

Mechanistic insights into the hepatic metabolism of lentinan: A TLR2-ROS-lysosome axis. [Abstract]

2026 Feb:347:150597. PMID: 41643971
Biochem Pharmacol

CHD1 regulates the inflammatory response in macrophages and functions as a pharmacological target during sepsis. [Abstract]

2026 Aug;250(Pt 1):118006. PMID: 42034314
Biomacromolecules

Antioxidant Hydrogel-Based Transdermal Drug Delivery Patch for Reactive Oxygen Species- and MyD88-Targeted Management of Atopic Dermatitis. [Abstract]

2025 Dec 11. PMID: 41378693
Int J Mol Sci

Human α-Defensin 51-9 and Human β-Defensin 2 Improve Metabolic Parameters and Gut Barrier Function in Mice Fed a Western-Style Diet. [Abstract]

2023 Sep 9;24(18):13878. PMID: 37762180
Int Immunopharmacol

A tyrosine catabolic intermediate 4-hydroxyphenylpyruate attenuates murine endotoxic shock by blocking NLRP3 inflammasome activation. [Abstract]

2022 Oct:111:109098. PMID: 35944460
Inflammation

TXM-CB13 Improves the Intestinal Mucosal Barrier and Alleviates Colitis by Inhibiting the ROS/TXNIP/TRX/NLRP3 and TLR4/MyD88/NF-κB/NLRP3 Pathways. [Abstract]

2025 Mar 14. PMID: 40085192
Sci Rep

Enhancement of melanoma aggressiveness via p38-MAPK, HIF-1α pathways, and metabolic reprogramming induced by Candida albicans. [Abstract]

2025 Nov 17;15(1):40227. PMID: 41249785
PLoS Pathog

Suppressing neutrophil itaconate production attenuates Mycoplasma pneumoniae pneumonia. [Abstract]

2024 Nov 5;20(11):e1012614. PMID: 39499730
Toxics

TLR/MyD88-Mediated Inflammation Induced in Porcine Intestinal Epithelial Cells by Ochratoxin A Affects Intestinal Barrier Function. [Abstract]

2023 May 6;11(5):437. PMID: 37235251
iScience

Protective effect of Zymosan-A against radiation-induced premature ovarian insufficiency in a murine model. [Abstract]

2026 Feb 14;29(4):115027. PMID: 41858627
iScience

PTEN acts as a crucial inflammatory checkpoint controlling TLR9/IL-6 axis in B cells. [Abstract]

2024 Jun 26;27(7):110388. PMID: 39092178
Antiviral Res

Ceragenins exhibit antiviral activity against SARS-CoV-2 by increasing the expression and release of type I interferons upon activation of the host's immune response. [Abstract]

2023 Sep:217:105676. PMID: 37481038
Microb Pathog

Extracellular vesicles derived from Cryptococcus neoformans promoted neutrophil extracellular traps. [Abstract]

2026 Jul:216:108543. PMID: 42103018
Vet Res

MyD88 inhibitor TJ-M2010-5 alleviates spleen impairment and inflammation by inhibiting the PI3K/miR-136-5p/AKT3 pathway in the early infection of Trichinella spiralis. [Abstract]

2025 Feb 4;56(1):28. PMID: 39905552
Npj Viruses

The soluble G protein of respiratory syncytial virus promotes viral dissemination via TLR2-mediated NLRP3 priming and pyroptosis. [Abstract]

2026 Jan 27;4(1):6. PMID: 41593203
Neuroscience

MyD88 Inhibition Attenuates Cerebral Ischemia-reperfusion Injury by Regulating the Inflammatory Response and Reducing Blood-brain Barrier Damage. [Abstract]

2024 Jun 21:549:121-137. PMID: 38754722
Microbes Infect

Suppressive effects of toll-like receptor 2, toll-like receptor 4, and toll-like receptor 7 on protective responses to Mycobacterium bovis BCG from epithelial cells. [Abstract]

2025 Feb;27(2):105428. PMID: 39368609
Vet Microbiol

M1 polarization of chicken macrophage HD11 can be activated by duck Tembusu virus via MyD88-NF-κB-mediated signaling pathway. [Abstract]

2023 Oct:285:109867. PMID: 37639898
Vet Dermatol

Toll-like receptor 2 activation induces C-C motif chemokine ligand 5 production in canine keratinocytes. [Abstract]

2025 Apr;36(2):117-126. PMID: 39973011
bioRxiv

MicroRNA-21 restrains myD88-dependent protective inflammation worsening Staphylococcus aureus skin infection. [Abstract]

2026 Jun 4:2026.06.01.729375. PMID: 42282617
SSRN

2025 Mar 17.
bioRxiv

2025 January 18.
bioRxiv

2024 September 13.
Universidad Del Pais Vasco

2023 Jun 22.
SSRN

2023 Sep 6.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (245.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

2.4598 mL

12.2989 mL

24.5978 mL

5 mM

0.4920 mL

2.4598 mL

4.9196 mL

10 mM

0.2460 mL

1.2299 mL

2.4598 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, 2 years; -20°C, 1 year (protect from light, stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.15 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 20% SBE-β-CD in Saline, and mix evenly.

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (394 KB)
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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)
Instruction de manipulation (2659 KB)

Références

[1]. Lin Xie, et al. Targeting of MyD88 Homodimerization by Novel Synthetic Inhibitor TJ-M2010-5 in Preventing Colitis-Associated Colorectal Cancer. J Natl Cancer Inst. 2015 Dec 28;108(4):djv364. [Content Brief]

[2]. Yan Miao,et al. Inhibition of MyD88 by a novel inhibitor reverses two-thirds of the infarct area in myocardial ischemia and reperfusion injury.Am J Transl Res. 2020 Sep 15;12(9):5151-5169. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4598 mL	12.2989 mL	24.5978 mL	61.4946 mL
	5 mM	0.4920 mL	2.4598 mL	4.9196 mL	12.2989 mL
	10 mM	0.2460 mL	1.2299 mL	2.4598 mL	6.1495 mL
	15 mM	0.1640 mL	0.8199 mL	1.6399 mL	4.0996 mL
	20 mM	0.1230 mL	0.6149 mL	1.2299 mL	3.0747 mL
	25 mM	0.0984 mL	0.4920 mL	0.9839 mL	2.4598 mL
	30 mM	0.0820 mL	0.4100 mL	0.8199 mL	2.0498 mL
	40 mM	0.0615 mL	0.3075 mL	0.6149 mL	1.5374 mL
	50 mM	0.0492 mL	0.2460 mL	0.4920 mL	1.2299 mL
	60 mM	0.0410 mL	0.2050 mL	0.4100 mL	1.0249 mL
	80 mM	0.0307 mL	0.1537 mL	0.3075 mL	0.7687 mL
	100 mM	0.0246 mL	0.1230 mL	0.2460 mL	0.6149 mL

Keywords

TJ-M2010-5

34 Cited Publications

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TJ-M2010-5

Anti-Cardiovascular Disease Compound Library

Anti-Obesity Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Immunology/Inflammation Compound Library

Publications Citing Use of MedChemExpress (MCE) TJ-M2010-5

Activité biologique

Chemical Information

Publications (34)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

TJ-M2010-5

Anti-Cardiovascular Disease Compound Library

Anti-Obesity Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Immunology/Inflammation Compound Library

Publications Citing Use of MedChemExpress (MCE) TJ-M2010-5

Activité biologique

Chemical Information

Publications (34)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

TJ-M2010-5 Related Classifications

HY-139397 Related Classifications