IκK/IκB

AKCI is an AURKC-IκBα interaction inhibitor with an IC50 value of 24.9 μM. It effectively induces G2/M cell cycle arrest in MDA-MB-231 cells by modulating the p53/p21/CDC2/cyclin B1 signaling pathway, while also inhibiting cell migration and invasion. Additionally, AKCI reduces colony formation and tumor growth, making it a valuable tool for investigating breast cancer mechanisms.

FIKK9.1-IN-1 is a selective inhibitor of the protein kinase FIKK9.1, targeting its ATP-binding residues. This compound demonstrates significant biological activity as an antimalarial agent, exhibiting an IC50 value of 2.68 μg/mL. By disrupting the life cycle of malaria parasites, FIKK9.1-IN-1 facilitates their elimination, making it a valuable tool for research focused on malaria intervention strategies.

GSK2181306A is a pan-FIKK inhibitor that exhibits an EC50 value of 0.16 μM for the inhibition of parasite growth. This compound is valuable for research focused on Plasmodium infections, enabling exploration of FIKK pathways in parasitic disease mechanisms and potential therapeutic interventions.

PI3K/PIKK-IN-2 is a potent inhibitor of the phosphoinositide 3-kinase (PI3K) and phosphoinositide-dependent kinase (PIKK) pathways. This compound demonstrates significant biological activity by modulating signaling pathways involved in cell growth, metabolism, and survival. PI3K/PIKK-IN-2 is suitable for use in research applications focused on targeted therapies, including the development of antibody-drug conjugates (ADCs).

BAY-985 is a selective ATP-competitive dual inhibitor targeting TBK1 and IKKε, demonstrating high potency with IC50 values of 2 nM for TBK1 under low ATP conditions and 30 nM under high ATP conditions, and 2 nM for IKKε. This inhibitor exhibits significant antitumor activity, making it a valuable tool for research applications focused on cancer therapy and the modulation of inflammatory pathways. Its oral bioavailability further enhances its utility in preclinical studies.

BAY32-5915 is a selective inhibitor of IKKα, exhibiting an IC50 value of 60 nM. This compound effectively prevents the activation of NF-κB without interfering with Doxorubicin-induced pathways. It is valuable for research in inflammation and cancer, providing insights into NF-κB signaling modulation.

NF-κB-IN-1 is a selective inhibitor of the IκB kinase (IKK) and functions primarily through the inhibition of NF-κB signaling. This compound effectively blocks the activation of NF-κB, demonstrating potent anti-cancer activity by reducing cell viability in lung cancer cells. Additionally, NF-κB-IN-1 significantly diminishes the clonogenic potential of A549 cells, making it a valuable tool for research on cancer therapeutics targeting NF-κB pathways.

6-Chloro-7-deazaguanine serves as a negative control for IκB kinase (IKK), specifically lacking the essential 5-cyano group that defines its activity. As an inactive analog, it provides a useful reference for studying the IKKβ and IKKα pathways, which are crucial components of the canonical and non-canonical NF-κB signaling pathways. Researchers can utilize this compound to delineate the role of IKK in various cellular processes and disease models, particularly in inflammation and immune responses.

SU1261 is a potent inhibitor of IKK, displaying Ki values of 10 nM for IKKα and 680 nM for IKKβ. This compound effectively inhibits non-canonical NF-κB signaling pathways, making it a valuable tool for studying the role of IKK in various cellular processes. Its application in research, particularly in osteosarcoma cell models such as U2OS, can provide insights into inflammatory responses and oncogenic signaling mechanisms.

SR12343 is an IKK/NF-κB inhibitor that acts as a mimetic of the NF-κB essential modulator (NEMO)-binding domain. It effectively disrupts the interaction between IKKβ and NEMO, leading to inhibition of TNF-α- and LPS-induced NF-κB activation, with an IC50 of 37.02 μM for TNF-α-mediated pathways. SR12343 has been shown to reduce LPS-induced acute pulmonary inflammation in murine models, making it valuable for research into inflammatory and degenerative diseases.

TBK1/IKKε-IN-4 is a selective inhibitor of TBK1 and IKKε, characterized by its 6-aminopyrazolopyrimidine structure. With IC50 values of 13 nM and 59 nM for TBK1 and IKKε, respectively, this compound demonstrates significant potency. It exhibits minimal activity against other protein kinases, including PDK1, PI3K family members, and mTOR, making it an efficient tool for investigating TBK1/IKKε-related pathways in various biological contexts. This inhibitor is useful for studies in inflammation, immune response, and neurodegenerative diseases.

BOT-64 is a selective IκB kinase β (IKKβ) inhibitor with an IC50 value of 1 µM. This compound effectively inhibits lipopolysaccharide-induced activation of nuclear factor-κB (NF-κB) and the subsequent transcription of NF-κB-regulated inflammatory genes. BOT-64 is valuable for research into inflammatory pathways and NF-κB signaling, providing insights into potential therapeutic strategies for inflammatory diseases.

IKK2-IN-4 is a selective inhibitor of IKK-2, exhibiting a potent IC50 value of 25 nM. This compound effectively inhibits LPS-induced TNFα production in peripheral blood mononuclear cells (PBMCs), making it a valuable tool for studying inflammatory responses. Research applications include investigations into signaling pathways involved in inflammation and potential therapeutic strategies for immune-related disorders.

HPN-01 is a potent and selective inhibitor of IκB kinase (IKK), demonstrating pIC50 values of 6.4, 7.0, and <4.8 for IKK-α, IKK-β, and IKK-ε, respectively. This compound exhibits significant selectivity, showing more than 50-fold preference over a diverse panel of over 50 kinases, including ALK5, CDK-2, EGFR, ErbB2, GSK3β, PLK1, Src, and VEGFR-2. HPN-01 is a valuable tool for research applications focused on inflammatory pathways, cancer cell signaling, and the study of immune responses.

IKKβ-IN-4 is a selective inhibitor of IkappaB kinase-β (IKKβ), with an IC50 value of 1.9 μM. IKKβ plays a crucial role in the NF-κB signaling pathway, which is implicated in various diseases, including inflammation and cancer. This compound is utilized in research to study the modulation of NF-κB activity and its potential therapeutic applications in related disease models.

MLN120B dihydrochloride is a potent inhibitor of IKKβ, exhibiting competitive ATP binding with an IC50 of 60 nM. This compound effectively inhibits the growth of multiple myeloma cells both in vitro and in vivo, making it a valuable tool for cancer research. Additionally, MLN120B can be utilized in studies focused on rheumatoid arthritis, contributing to the understanding of inflammatory pathways and potential therapeutic interventions.

IKK2-IN-3 is a selective inhibitor of IKK2, demonstrating a potent inhibitory effect with an IC50 value of 0.075 μM. This compound effectively disrupts the NF-κB signaling pathway, impacting various cellular processes such as inflammation and immune response. IKK2-IN-3 is suitable for research applications involving the modulation of IKK2 activity in disease models and studying the role of NF-κB in cellular signaling.

LY2409881 is a selective inhibitor of IκB kinase β (IKK2), demonstrating potent inhibition with an IC50 of 30 nM. This compound is primarily used in research for its ability to modulate the NF-κB signaling pathway, making it relevant for studying inflammation, cancer, and autoimmune diseases. Researchers utilize LY2409881 to explore its therapeutic potential in various disease models and to investigate the role of IKK2 in cellular processes.

IKK-IN-4 is a selective inhibitor of IkappaB kinase 2 (IKKβ), exhibiting an IC50 of 45 nM for IKKβ and 650 nM for IKKα. This compound is instrumental in research focusing on the NF-κB signaling pathway and its regulation, providing insights into inflammation, cancer, and other diseases linked to IKK activity. IKK-IN-4 serves as a valuable tool for studying IKKβ-mediated signaling mechanisms and potential therapeutic interventions.

SR8185 is a potent dual inhibitor of TBK1 and IKKi, exhibiting IC50 values of 3 nM and less than 10 nM, respectively. This compound demonstrates significant antiproliferative effects across a wide range of human cancer cell lines. SR8185 is ideal for exploring cancer-related pathways and therapeutic strategies in cancer research.

IKKβ-IN-1 is a selective inhibitor of IkappaB kinase beta (IKK-β), exhibiting an IC50 of 0.20 μM. This compound effectively reduces the production of pro-inflammatory cytokines such as PGE2 and TNF-α in mouse macrophage cells. Additionally, IKKβ-IN-1 has demonstrated protective effects against mortality in mice subjected to septic shock, highlighting its potential for research in inflammation and immune response.

TBK1/IKKε-IN-6 is a selective inhibitor of TBK1 and IKKε, exhibiting IC50 values below 100 nM for both targets. This compound plays a significant role in modulating inflammatory signaling pathways by inhibiting the activation of these kinases. It is particularly useful in research focused on autoimmune diseases, cancer, and viral infections, enabling the exploration of therapeutic strategies targeting the TBK1/IKKε pathway.

(E/Z)-HOIPIN-1 is a selective inhibitor of the linear ubiquitin chain assembly complex (LUBAC), targeting the IκB kinase (IKK) pathway. With an IC50 value greater than 2.8 μM, this compound effectively inhibits LUBAC-mediated NF-κB activation. Its potential applications include studies of inflammatory responses, cancer biology, and the modulation of immune signaling pathways.

SAR113945 is a highly potent inhibitor of IKK-β, exhibiting an IC50 value of 0.4 nM. This compound is primarily utilized in research focusing on inflammatory pathways and oncogenic processes. Its efficacy makes it a valuable tool for investigating the role of IKK-β in various disease states, particularly in understanding mechanisms underlying inflammation and cancer progression.

MLN-0415 is an inhibitor of IKKβ, a key regulator in the NF-κB signaling pathway. This compound exhibits significant anti-inflammatory activity and is instrumental in researching conditions such as arthritis and other inflammatory diseases. MLN-0415 facilitates the exploration of therapeutic strategies targeting the modulation of inflammatory responses.

(Rac)-PF-184 is a selective inhibitor of the inhibitor of κB kinase 2 (IKK-2) with an IC50 value of 37 nM. This compound exhibits significant anti-inflammatory properties, making it a valuable tool for research into inflammatory signaling pathways. It is suitable for studies investigating the role of IKK-2 in various biological processes and disease models.

1-Dehydro-[10]-gingerdione functions as a selective inhibitor of IKKβ by targeting its activation loop, leading to the disruption of IKKβ-mediated phosphorylation of IκBα in macrophages stimulated with various agonists. This compound effectively inhibits LPS-induced NF-κB transcriptional activity. 1-Dehydro-[10]-gingerdione holds promise for research into NF-κB-related inflammation and autoimmune disorders.

IKK-IN-3 is a potent and selective inhibitor of IkappaB kinase 2 (IKK2, also known as IKKβ), exhibiting IC50 values of 19 nM for IKK2 and 400 nM for IKK1 (IKKα). This compound is valuable in research focused on the regulation of the NF-kB signaling pathway, which plays a critical role in inflammation, immune responses, and cancer progression. IKK-IN-3 can be utilized to investigate the therapeutic potential of IKK2 inhibition in various disease models.

GTCpFE is a selective inhibitor of IKKα/β, functioning within the NF-κB signaling pathway. This compound exhibits significant anti-inflammatory properties by preventing the nuclear translocation of the p65 subunit of NF-κB. Additionally, GTCpFE demonstrates targeted anti-cancer stem-like cell activity by impairing mammosphere formation and reducing the CD44+ CD24- immunophenotype associated with aggressive breast cancer. Its dual mechanism positions GTCpFE as a promising agent for both inflammation and cancer research.

TBK1/IKKε-IN-1 is a potent dual inhibitor of TBK1 and IKKε, demonstrating IC50 values of less than 100 nM. This compound is valuable for research applications involving the modulation of inflammatory pathways and immune responses. Its inhibition of these kinases provides a tool for studying their roles in various biological processes and disease states, particularly those related to cancer and neuroinflammation.