TJ-M2010-5, a MyD88 inhibitor, interacts with the TIR domain of MyD88 to block its homodimerization and disrupt the TLR/MyD88 signaling pathway [1][2]. TJ-M2010-5 is applicable for research into myocardial ischemia/reperfusion injury (MIRI) [2].
体内研究
TJ-M2010-5 treatment significantly reduces AOM/DSS-induced colitis and completely prevents the development of colorectal cancer-associated colitis (CAC) with minimal related body mass loss, resulting in 0% mortality in treated mice. It also reduces cell proliferation and increases apoptosis in colon tissue in a 10-week CAC mouse model [1].
TJ-M2010-5 significantly lowers serum concentrations of TNF-α, IL-6, G-CSF, MIP-1β, IL-11, IL-17A, IL-22, and IL-23 at both two and seven weeks postinduction, and TGF-β1 levels at seven weeks postinduction [1].
体外研究
TJ-M2010-5 (40 μM) concentration-dependently inhibits MyD88 homodimerization in transfected HEK293 cells and reduces MyD88 signaling in LPS (100 ng/mL)-responsive RAW 264.7 cells in vitro[1].
TJ-M2010-5 (5-30 μM) inhibits B cell proliferation and triggers apoptosis in B cells following stimulation with R848 (500 ng/mL) [3].
TJ-M2010-5 细胞实验
Cell Line
Concentration
Treated Time
Description
References
Primary microglia
30 µM
24 hours
TJ-M2010-5 inhibited CORT-induced microglial activation, as indicated by reduced immunofluorescence intensity of CD68 and Iba1.
Brain Behav Immun. 2023 Feb;108:204-220
BV2 cells
30 µM
24 hours
TJ-M2010-5 inhibited CORT-induced neuroinflammatory activation, as indicated by reduced levels of NF-κB p65 phosphorylation and IL-1β protein.
Brain Behav Immun. 2023 Feb;108:204-220
SH-SY5Y cells
0, 1, 5, 10, 20, 30 µM
24 hours
Evaluate the effect of TJ-M2010-5 on SH-SY5Y cell viability, results showed TJ-5 did not affect cell viability at concentrations below 20 μM
Front Pharmacol. 2022 Dec 15;13:1080438
BV-2 cells
0, 1, 5, 10, 20, 30 µM
24 hours
Evaluate the effect of TJ-M2010-5 on BV-2 cell viability, results showed TJ-5 did not affect cell viability at concentrations below 20 μM
Front Pharmacol. 2022 Dec 15;13:1080438
RAW 264.7 cells
40 µM
4 hours
To evaluate the effect of TJ-M2010-5 on cytokine secretion in RAW 264.7 cells. Results showed that TJ-M2010-5 significantly reduced the secretion of GM-CSF, IFN-γ, IL-1β, IL-6, and TGF-β1.
Invest New Drugs. 2022 Jun;40(3):506-518
RAW264.7 cells
10 and 20 µM
6 hours
TJ-M2010-5 significantly inhibited LPS-induced inflammation by down-regulating the expression of IL6, IL1β, and TNFα, reversed macrophage M1 polarisation, decreased the M1/M2 ratio, and inhibited NO production.
Vet Res. 2025 Feb 4;56(1):28
Bone marrow-derived macrophages (BMDMs)
10 and 30 µM
6 hours LPS stimulation followed by 2 hours ATP stimulation
To evaluate the inhibitory effect of TJ-5 on LPS- and ATP-induced pyroptosis in BMDMs. Results showed that TJ-5 effectively inhibited GSDMD cleavage and cell death.
Transplantation. 2023 Feb 1;107(2):392-404
TJ-M2010-5 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6J mice
Chronic social defeat stress (CSDS) model
Intraperitoneal injection
2.5 mg/kg
Twice daily for 2 days
TJ-M2010-5 alleviated CSDS-induced depressive-like behaviors, as evidenced by increased social interaction time and sucrose preference, and reduced immobility time in TST and FST.
Brain Behav Immun. 2023 Feb;108:204-220
BALB/c mice
Early infection model of T. spiralis
Intraperitoneal injection
30 mg/kg/day
Five successive days
TJ-M2010-5 significantly alleviated spleen impairment and reduced inflammation in mice infected with T. spiralis in its early stages by blocking the activation of PI3K/miR-136-5p/AKT3 pathway.
Vet Res. 2025 Feb 4;56(1):28
C57BL/6 mice
Middle cerebral artery occlusion (MCAO) model
Intravenous injection
5, 10, 15 mg/kg
Single dose, lasted for 24 hours
Evaluate the therapeutic effect of TJ-M2010-5 on cerebral ischemia-reperfusion injury, results showed TJ-5 significantly reduced cerebral infarction volume and neuronal loss
Front Pharmacol. 2022 Dec 15;13:1080438
Female BalB/c mice
Colitis-associated colorectal cancer (CAC) model
Intraperitoneal injection
50 mg/kg
Daily for 10 weeks
To evaluate the effect of TJ-M2010-5 on MDSC accumulation and function in the CAC model. Results showed that TJ-M2010-5 significantly reduced the accumulation of CD11b+Gr-1+ MDSCs, decreased the secretion of cytokines (GM-CSF, G-CSF, IL-1β, IL-6, and TGF-β) associated with MDSC accumulation, and reduced the expression of molecules (iNOS, Arg-1, and IDO) associated with the suppressive capacity of MDSCs.
Invest New Drugs. 2022 Jun;40(3):506-518
BALB/c mice
Hepatic ischemia-reperfusion injury (IRI) model
Intraperitoneal injection
50 mg/kg
3 consecutive days, once daily
To evaluate the protective effect of TJ-5 on hepatic IRI. Results showed that TJ-5 significantly improved liver function and reduced hepatocellular injury and inflammation.
Transplantation. 2023 Feb 1;107(2):392-404
C57BL/6J mice
DSS-induced acute colitis model
Intraperitoneal injection
50 mg/kg
Once daily, starting one day before the first DSS administration until the seventh day of DSS challenge.
To investigate the impact of MyD88 inhibition on DSS-induced acute colitis. Results showed that although TJ5 significantly reduced NF-κB activation, it did not significantly alleviate the severity of colitis.
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