[CAS NO. 1893397-65-3] TBK1/IKKε-IN-1(compound 1)
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PRODUCTS SPECIFICATIONS [1893397-65-3]
Store
Catalog
SLK-S8922
Brand
Selleck
CAS
1893397-65-3
DESCRIPTION [1893397-65-3]
Overview
| MDL | MFCD32067990 |
|---|---|
| Molecular Weight | 513.59 |
| Molecular Formula | C28H31N7O3 |
| SMILES | N#CC1=C(OC2CCOCC2)C=CC(C3=NC=NC(NC4=CC=C(N5CCN(CC5)C6COC6)C=C4)=N3)=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9471 mL | 9.7354 mL | 19.4708 mL |
| 5 mM | 0.3894 mL | 1.9471 mL | 3.8942 mL |
| 10 mM | - | - | - |
| 50 mM | - | - | - |
Description
TBK1/IKKε-IN-1 (compound 1) is a dual inhibitor of and with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo.
In vitro
TBK1/IKKε-IN-1(compound 1) effectively blocks immune suppressive cytokine elaboration by CT26 cell line spheroids, without cytotoxic effects, and enhances secretion of IL-2 and IFN-γ from purified CD4+ and CD8+ T cells from healthy human donors and IL-2 from Jurkat human T-cell leukemia cells. Ex vivo addition of TBK1/IKKε-IN-1(compound 1) to PD-1 blockade enhances killing of CT26 MDOTS, associated with decreased levels of CCL4, CCL3, and IL-1β and induction of cytokines involved in activated innate immune responses.
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