T6167923 B

SKU: orb2901699

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 IC50s 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.

Images & Validation

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Key Properties

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CAS Number	2437475-16-4
MW	458.39
Purity	>98% (HPLC)
Formula	C₁₇H₂₀BrN₃O₃S₂
SMILES	C[C@H](NC(=O)N1CCN(CC1)S(=O)(=O)c1cccc(Br)c1)c1cccs1
Target	MyD88
Solubility	In Vitro: DMSO : 250 mg/mL (545.39 mM; Ultrasonic ) H2O : < 0.1 mg/mL (insoluble)

Bioactivity

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In Vivo

T6167923 (0.17 and 1 mg; i.p. once) survives the mice from intoxication with SEB and LPS injection. Animal model: 16-20 week-old BALB/c mice with LPS potentiation model. Dosage: 0.17 and 1 mg. Administration: Intraperitoneal injection; 0.17 and 1 mg once. Result: Dose-dependently showed a therapeutic efficacy against SEB intoxication.

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 onMyD88-signaling. T6167923 (1-500 μM; 13 h) inhibits full-length MyD88 homodimeric formation. Cell Viability Assay Cell 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 IC50s of 2.66, 2.7, 2.66 and 2.9 μM in peripheral blood mono nuclear cells. Cell Viability Assay Cell 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 IC50s in the range of 40-50 μM. Cell Viability Assay Cell 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 analysis. Cell 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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Gene Symbol

MyD88

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T6167923 B

Description

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Key Properties

Bioactivity

Storage & Handling

Quality Guarantee

Quick Database Links

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Protocol Information

T6167923 B (orb2901699)

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