[CAS NO. 1357471-57-8] TJ-M2010-5
PRODUCTS SPECIFICATIONS [1357471-57-8]
DESCRIPTION [1357471-57-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 406.54 |
| Molecular Formula | C23H26N4OS |
| SMILES | O=C(NC1=NC(C2=CC=CC=C2)=CS1)CCN3CCN(CC4=CC=CC=C4)CC3 |
1 Publications Citing Use of MCE
Summary
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]
.
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]
.
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). |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL ( 245.98 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 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 |
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1.
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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
References
- [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.