TBK1/IKKε-IN-5

Research use only, not for human use.

TBK1/IKKε-IN-5 is a dual TBK1 and IKKε inhibitor(IC50 of 1 nM and 5.6 nM respectively).

TBK1/IKKε-IN-5 is a dual TBK1 and IKKε inhibitor(IC50 of 1 nM and 5.6 nM respectively).

TBK1/IKKε-IN-5 (0.001-10 μM; 24 or 96 h) promotess secretion of IL-2 and IFN-γ in purified CD4+ and CD8+ T cells and IL-2 in Jurkat human T-cell leukemia cells.TBK1/IKKε-IN-5 effectively blocks immune suppressive cytokine elaboration by CT26 cell line spheroids, without cytotoxic effects. Cell Viability Assay Cell Line:CD4+ and CD8+ T cells, Jurkat T cell leukemia cells Concentration:0.001-10 μM Incubation Time:24 h (for IL-2); 96 h(for IFN-γ)Result:Enhanced secretion of IL-2 and IFN-γ.

TBK1/IKKε-IN-5 (40 mg/kg; p.o.; single daily for 26 days) shows good antitumor activity and prolongs survival, as well as induces immunologic memory of CT26 cells in mice when combines with anti-PD-L1. Animal Model:Female Balb/c mice (11 to 12-week-old; bearing CT26 tumors).Dosage:40 mg/kg Administration:Oral gavage; single daily for 26 days (combine with anti-PD-L1).Result:Exhibited greater tumor control and longer survival when combined with anti-PD-L1 than used alone of both agents.Induced immunologic memory of CT26 cells in mice when combined with anti-PD-L1.

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Immunology/Inflammation

IκB kinase (IKK)

TBK1| IKK?

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1893397-65-3

513.59

C28H31N7O3

>98% (HPLC)

DMSO:7.81 mg/mL (15.21 mM; Need ultrasonic)

N#Cc1cc(ccc1OC1CCOCC1)-c1ncnc(Nc2ccc(cc2)N2CCN(CC2)C2COC2)n1

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(-20℃)

With Ice Pack

≥ 2 years