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Cat. No. M21680
TJ-M2010-5 Structure
Size Price Availability Quantity
5mg USD 86  USD86 In stock
10mg USD 135  USD135 In stock
25mg USD 270  USD270 In stock
50mg USD 420  USD420 In stock
100mg USD 630  USD630 In stock
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Quality Control & Documentation
Biological Activity

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 inhibited MyD88 homodimerization in transfected HEK293 cells in a concentration-dependent manner and suppressed MyD88 signaling in LPS-responsive RAW 264.7 cells in vitro. 

In a 10-week CAC mouse model (n = 30 per group), TJ-M2010-5 treatment statistically significantly reduced AOM/DSS-induced colitis and completely prevented CAC development with less related body mass loss, resulted in 0% mortality of treated mice (compared with 53% mortality of control mice), decreased cell proliferation, and increased apoptosis in colon tissue. TJ-M2010-5 treatment also inhibited production of inflammatory cytokines and chemokines (TNF-α, IL-6,G-CSF, MIP-1β, TGF-β1, IL-11, IL-17A, IL-22 and IL-23) and infiltration of immune cells (macrophages, dendritic cells, neutropihls and CD(+)4 T cells) in colon tissues of mice.

Protocol (for reference only)
Cell Experiment
Cell lines RAW 264.7 cells
Preparation method RAW 264.7 cells were cultured in RPMI medium 1640. After stimulation with 100ng/mL of lipopolysaccharide (LPS) for six hours with 40 µM TJ-M2010-5 or vehicle one hour pretreatment, cells in individual wells were harvested for protein extraction.
Concentrations 40 µM
Incubation time 6 hours
Animal Experiment
Animal models Female BalB/c mice (6–8 weeks old)
Formulation vehicle (ddH2 O)
Dosages 50mg/Kg daily
Administration i.p.
Chemical Information
Molecular Weight 406.54
Formula C23H26N4OS
CAS Number 1357471-57-8
Solubility (25°C) DMSO 90 mg/mL
Storage 4°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Zeyang Li, et al. Front Pharmacol. TJ-M2010-5, a novel CNS drug candidate, attenuates acute cerebral ischemia-reperfusion injury through the MyD88/NF-κB and ERK pathway

[2] Huifang Yang, et al. J Cardiovasc Transl Res. TJ-M2010-5 Attenuates Severe Myocardial Ischemia/Reperfusion Injury in Heart Transplantation by Inhibiting MyD88 Homodimerization In Vivo

[3] Yalong Xie, et al. Chem Biol Interact. TJ-M2010-5, A self-developed MyD88 inhibitor, attenuates liver fibrosis by inhibiting the NF-κB pathway

[4] Wei Zhou, et al. Int Immunopharmacol. Hypothermic oxygenated perfusion combined with TJ-M2010-5 alleviates hepatic ischemia-reperfusion injury in donation after circulatory death

[5] Yan Miao, et al. Am J Transl Res. Inhibition of MyD88 by a novel inhibitor reverses two-thirds of the infarct area in myocardial ischemia and reperfusion injury

[6] Zhimiao Zou, et al. Int Immunopharmacol. TJ-M2010-5, a novel MyD88 inhibitor, corrects R848-induced lupus-like immune disorders of B cells in vitro

[7] Lin Xie, et al. J Natl Cancer Inst. Targeting of MyD88 Homodimerization by Novel Synthetic Inhibitor TJ-M2010-5 in Preventing Colitis-Associated Colorectal Cancer

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