| SKU | Size | Availability | Price | Qty |
|---|---|---|---|---|
| T654500-1ml | 1ml | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $473.90 |
| Specifications & Purity | 10mM in DMSO |
|---|---|
| Storage Temp | Store at -80°C |
| Shipped In | Dry ice |
| Product Description | T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC 50 s of 2.7 μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ , IL-1β, IL-6 and TNF-α, respectively In Vitro T6167923 (0-500 μM; 20 h) inhibits the pro-inflammatory cytokine response of staphylococcal enterotoxin B (SEB) in peripheral blood mono nuclear cells. T6167923 (10-500 μM; 2 h) inhibits secreted alkaline phosphatase response (SEAP) expression in HEK 293T cells. T6167923 (100 μM; 16 h) binds to TIR protein and reduced the inhibitory effect on MyD88-signaling. T6167923 (1-500 μM; 13 h) inhibits full-length MyD88 homodimeric formation. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Peripheral blood mono nuclear cells Concentration: 0-500 μM Incubation Time: 20 hours Result: Dose-dependently attenuated the response of SEB to TNF-α, INF-γ, IL-6, and IL-1β with IC 50 s of 2.66, 2.7, 2.66 and 2.9 μM in peripheral blood mono nuclear cells. Cell Viability AssayCell Line: HEK 293T cell line Concentration: 10-500 μM Incubation Time: 2 hours Result: Dose-dependently inhibited lipo-polysaccharide (LPS) induced MyD88-mediated NF-kB driven SEAP expression in HEK 293T cells with IC 50 s in the range of 40–50 μM. Cell Viability AssayCell Line: HEK 293T cell line Concentration: 100 μM Incubation Time: 16 hours Result: Specifically targeted MyD88 and dose-denpendently with TIR protein to reduced the inhibitory effect of MyD88-signaling. Western Blot AnalysisCell Line: HEK 293-I3A cells with MyD88 knockout Concentration: 1-500 μM Incubation Time: 13 hours Result: Dose-dependently inhibited TIR domain-mediated dimerization of full-length MyD88 and the recombinant TIR domain protein. In Vivo T6167923 (0.17 and 1 mg; i.p. once) survives the mice from intoxication with SEB and LPS injection. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 16-20 week-old BALB/c mice with LPS potentiation modelDosage: 0.17 and 1 mg Administration: Intraperitoneal injection; 0.17 and 1 mg once Result: Dose-dependently showed a therapeutic efficacy against SEB intoxication. IC50& Target:IC50: 2.7 μM (IFN-γ), 2.9 μM (IL-1β), 2.66 μM (IL-6), 2.66 μM (TNF-α) |
| Canonical SMILES | BrC1=CC(S(=O)(N2CCN(C(N[C@H](C3=CC=CS3)C)=O)CC2)=O)=CC=C1 |
|---|---|
| Molecular Weight | 458.39 |
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