2. Signaling Pathways
  3. NF-κB
  4. IKK
  5. IKKε Isoform

IKKε

IKKε (IKBKE) is a non-canonical IκB kinase that functions as a central regulator of innate immune signaling by coordinating antiviral and inflammatory responses through the activation of interferon regulatory factors and downstream type I interferon pathways[1][2]. Mechanistically, IKKε operates within the TBK1-IKKε-IRF3/IRF7 signaling axis, where it contributes to nucleic acid sensing pathways and promotes transcriptional programs required for host defense and immune adaptation[1][3]. Beyond antiviral signaling, IKKε also regulates metabolic and inflammatory processes, supporting its emerging role in obesity, diabetes, and related metabolic disorders[4]. In disease-relevant experimental models, genetic or pharmacological disruption of IKKε activity alters inflammatory homeostasis, and combined impairment of IKKε and TBK1 induces systemic inflammation, myeloid cell expansion, and intestinal pathology in mice, demonstrating an essential role in maintaining tissue integrity and controlling RIPK1-associated inflammatory responses[5]. Compared with the closely related kinase TBK1, IKKε exhibits both overlapping and distinct biological functions; notably, IKKε can compensate for loss of TBK1 kinase activity in vivo, while specific C-terminal regions required for downstream signaling and type I interferon activation are functionally important in IKKε but not in TBK1[5][6]. Therefore, the distinction between IKKε and TBK1 is highly relevant for mechanistic studies of innate immunity and inflammation. For experimental applications, small-molecule inhibitors targeting IKKε or the TBK1/IKKε kinase network have been developed and are widely used to investigate inflammatory, metabolic, autoimmune, and cancer-associated signaling pathways, supporting the evaluation of IKKε as a therapeutic target and research tool[4][7][8].

IKKε Related Products (11):

Cat. No. Product Name Effect Purity
  • HY-10514
    BX795
    		Inhibitor 99.84%
    BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKε, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
  • HY-B0713
    Amlexanox
    		Inhibitor 99.70%
    Amlexanox (AA673; Amoxanox; CHX3673) is a specific inhibitor of IKKε and TBK1, and inhibits the IKKε and TBK1 activity determined by MBP phosphorylation with an IC50 of approximately 1-2 μM.
  • HY-13018
    MRT67307
    		Inhibitor 99.56%
    MRT67307 is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 also blocks autophagy in cells.
  • HY-133117
    BAY-985
    		Inhibitor 99.69%
    BAY-985, a chemical probe, is a highly potent, orally active and selective ATP-competitive dual inhibitor of TBK1 and IKKε with IC50s of 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε, respectively. Antitumor efficacy.
  • HY-12453
    TBK1/IKKε-IN-2
    		Inhibitor 98.62%
    TBK1/IKKε-IN-2 is a dual TBK1 and IKKε inhibitor.
  • HY-181271
    IKKε-IN-1
    		Inhibitor
    IKKε-IN-1 is a IKKε inhibitor. IKKε-IN-1 reduces cell viability, inhibits colony formation and cell migration. IKKε-IN-1 induces autophagy (Autophagy) in cancer cells. IKKε-IN-1 can be used in the research of cancers including colorectal cancer, hepatocellular carcinoma, bladder cancer, breast cancer, lung cancer, and cervical cancer.
  • HY-124652
    TBK1/IKKε-IN-4
    		Inhibitor 99.42%
    TBK1/IKKε-IN-4 is a 6-aminopyrazolopyrimidine derivative and a potent, selective TBK1 and IKKε inhibitor with IC50 values of 13 nM and 59 nM, respectively. TBK1/IKKε-IN-4 shows 100- to 1000-fold less activity against other protein kinases including PDK1, PI3K family members and mTOR.
  • HY-14682
    GSK319347A
    		Inhibitor 99.25%
    GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
  • HY-135366
    HPN-01
    		Inhibitor 98.61%
    HPN-01 is a potent and selective IKK inhibitor, with pIC50 values of 6.4, 7.0 and <4.8 for IKK-α, IKK-β and IKK-ε, respectively. HPN-01 displays greater 50-fold selectivity over a panel of more than 50 other kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2.
  • HY-13018A
    MRT67307 hydrochloride
    		Inhibitor
    MRT67307 hydrochloride is a dual inhibitor of the IKKε and TBK-1 with IC50s of 160 and 19 nM, respectively. MRT67307 hydrochloride also inhibits ULK1 and ULK2 with IC50s of 45 and 38 nM, respectively. MRT67307 hydrochloride also blocks autophagy in cells.
  • HY-U00457
    TBK1/IKKε-IN-1
    		Inhibitor
    TBK1/IKKε-IN-1 is a dual TBK1 and IKKε inhibitor extracted from patent US20160376283 A1, Compound 274 in Example 60, has IC50s of <100 nM.