For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I037337 |
| CAS Number | 1357471-57-8 |
| Synonyms | 3-(4-benzylpiperazin-1-yl)-N-(4-phenyl-1,3-thiazol-2-yl)propanamide |
| Molecular Formula | C23H26N4OS |
| Purity | ≥95% |
| InChI | InChI=1S/C23H26N4OS/c28-22(25-23-24-21(18-29-23)20-9-5-2-6-10-20)11-12-26-13-15-27(16-14-26)17-19-7-3-1-4-8-19/h1-10,18H,11-17H2,(H,24,25,28) |
| InChIKey | DTIQJBUDKQVBLT-UHFFFAOYSA-N |
| SMILES | C1CN(CCN1CCC(=O)NC2=NC(=CS2)C3=CC=CC=C3)CC4=CC=CC=C4 |
| Reference | [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. [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. |
