Catalog No.
Product Name
Application
Product Information
Citations
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PDK-1 inhibitor
BX-795 is a potent PDK1 inhibitor that blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induced apoptosis.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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IKK inhibitor
BMS 345541 is a cell-permeable and highly selective IKB kinase (IKK) inhibitor that binds at allosteric site of the enzyme and blocks NF-kB-dependent transcription in mice.- Lizhi Liu, .et al. , Cell Rep, 2024, Mar 26;43(3):113886 PMID: 38430516
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IκB/IKK inhibitor
Bardoxolone methyl is an orally-available first-in-class synthetic triterpenoid. It is an inducer of the Nrf2 pathway, which can suppress oxidative stress and inflammation.- May Barakat, .et al. , Sci Rep, 2024, Oct 24;14(1):25258 PMID: 39448644
- Nakamura S, .et al. , Invest Ophthalmol Vis Sci, 2019, 60: 1943-1952 PMID: 31050722
- Hisamichi M, .et al. , Hypertens Res, 2018, Jan;41(1):8-17 PMID: 28978980
- Takahiko Imai, .et al. , Neurobiol Dis, 2016, May;89:136-46 PMID: 26850917
- Takagi T, .et al. , Free Radic Biol Med, 2014, 72:124-33 PMID: 24746614
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IκB/IKK inhibitor
Bardoxolone methyl, previously known as RTA 402, is the lead molecule in Reata's portfolio of Antioxidant Inflammation Modulators (AIMs).- Rothan HA, .et al. , Antiviral Res, 2019, Aug 14;171:104590 PMID: 31421166
- Turpaev K, .et al. , Eur J Pharmacol, 2016, Aug 5;784:69-80 PMID: 27178899
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IKKβ kinase inhibitor
Bay 65-1942 is an ATP-competitive inhibitor that selectively targets IKKβ kinase activity. -
IKKβ inhibitor
Bay 65-1942 is an ATP-competitive inhibitor that selectively targets IKKβ kinase activity. -
IKK Inhibitor
IKK-2 inhibitor VIII is a potent and selective IKK-2 inhibitor with IC50 of 8.5 nM. -
IKK Inhibitor
GSK319347A (CAY10576) is a potent, selective, inhibitor of IKK-epsilon kinase with IC50 of 40 nM; inactive at IKK-alpha and IKK-beta.
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IKK-2 inhibitor
TPCA-1 is a potent and selective inhibitor of human IκB kinase-2 (IKK-2) with IC50 = 17.9 nM for IKK-2 compared to 400nm for IKK-1. -
IκB/IKK inhibitor
Bay 11-7821 is an irreversible inhibitor of TNF-α-stimulated IκBα phosphorylation.- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Ali Nasrollahzadeh, .et al. , Rep Biochem Mol Biol, 2022, Jan;10(4):602-613 PMID: 35291620
- Ali Nasrollahzadeh, .et al. , Life Sci, 2020, Jul 6;257:118060 PMID: 32645343
- Momeny M, .et al. , Int J Biochem Cell Biol, 2018, Jun;99:1-9 PMID: 29567488
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IκB/IKK inhibitor
BAY 11-7085 is an irreversible inhibitor of TNFα-induced IκBα phosphorylation with IC50 of 10 μM- Byungki Jang, .et al. , Int J Mol Sci, 2017, Nov; 18(11): 2258 PMID: 29077055
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IKK2/IKK1 inhibitor
BMS-345541 is a highly selective inhibitor of the catalytic subunits of IKK-2 and IKK-1 with IC50 of 0.3 μM and 4 μM -
IKK Inhibitor
IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK-2, IKK complex and IKK-1 with IC50 of 40 nM, 70 nM and 200 nM, respectively.- Rulina AV, .et al. , Cell Death Dis, 2016, Dec 1;7(12):e2505 PMID: 27906189
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IKK Inhibitor
IMD 0354 is an inhibitor of IκB kinase-β (IKKβ) that blocks NF-κB nuclear translocation.- Anton Lennikov, .et al. , Angiogenesis, 2018, 21(2): 267-285 PMID: 29332242
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IKK Inhibitor II
Wedelolactone, a compound originally extracted from Eclipta alba, has been shown to inhibit caspase-11, which is a key regulator of proinflammatory cytokine IL-1β maturation and pathological apoptosis.- Shigetoshi Yokoyama, .et al. , eLife, 2018, 7: e37854 PMID: 30526845
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IKK Inhibitor?€?
Bay 65-1942 (R form) is an ATP-competitive inhibitor that selectively targets IKKβ kinase. -
IKK2 inhibitor
LY2409881 is a potent and selective IKK2 inhibitor with IC50 of 30 nM, >10-fold selectivity over IKK1 and other common kinases. -
IKK-ε inhibitor
IKK epsilon-IN-1 is a potent IKKε inhibitor; inhibit the in-situ IKK ε-mediated phosphorylation of IRF3 with an IC50 value of less than about 100 nM. -
dual TBK1 and IKKε inhibitor
TBK1/IKKε-IN-5 is a dual TBK1 and IKKε inhibitor, with IC50 values of 1 nM and 5.6 nM for TBK1 and IKKε, respectively. -
PTP1B/IKK-βinhibitor and dual PPARα and PPARβ agonist
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ. -
IKK2/IKK complex/IKK1 inhibitor
IKK 16 hydrochloride is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. -
anti-infective agent
Tizoxanide is the active metabolite of Nitazoxanide, which is a thiazolide anti-infective compound against anaerobic bacteria, protozoa, and a range of viruses. Tizoxanide has anti-HIV-1 activities. -
TBK1 Degrader
PROTAC TBK1 Degrader-2 is a targeted protein degrader designed to selectively degrade the serine/threonine kinase TANK-binding kinase 1 (TBK1) with a DC50 of 15 nM and Kd of 4.6 nM, exhibiting a maximum efficiency of 96%. Additionally, this compound also influences IkB kinase IKKε, demonstrating an IC50 of 8.7 nM, and displays a low selectivity over TBK1 with an IC50 of 1.3 nM. This reagent is suitable for investigating TBK1-related signaling pathways and potential therapeutic applications in various diseases. -
PROTAC IKKβ/NR4A1 Degrader
PROTAC IKKβ/NR4A1 degrader-1 is a novel dual-PROTAC degrader designed to selectively target and degrade IKKβ and NR4A1, utilizing the E3 ligase cereblon. This compound effectively increases the levels of caspase 3 and cleaved caspase 3 proteins, indicating a potential to induce apoptosis without affecting the necroptosis marker RIP kinase. It is a valuable tool for investigating the mechanisms underlying Acute Myeloid Leukemia (AML) and offers insights into therapeutic strategies targeting these pathways. -
Bacterial Inhibitor; IKKβ Inhibitor
Abietic acid is a diterpene compound that acts as an IKKβ inhibitor, showcasing significant antibacterial properties alongside anti-inflammatory and anti-proliferative effects. It exhibits remarkable activity in ameliorating liver injury, enhancing cell migration, and promoting angiogenesis through ERK and p38 upregulation. Abietic acid has demonstrated efficacy in reducing non-small-cell lung cancer (NSCLC) cell proliferation and shows potential for addressing conditions such as psoriasis and sepsis-induced lung injury by modulating inflammatory pathways. Its diverse biological activities make it a valuable reagent for research in cancer, liver diseases, and inflammatory disorders. -
IKK/STAT3 Dual Inhibitor
ACHP is a selective IκB kinase (IKK) and STAT3 dual inhibitor, demonstrating potent inhibitory activity with IC50 values of 8.5 nM and 250 nM for IKKβ and IKKα, respectively. It effectively disrupts the STAT3 signaling pathway, leading to cancer cell cycle arrest and apoptosis. Additionally, ACHP exhibits significant anti-inflammatory properties in preclinical models, such as the mouse ear edema model. This compound is a valuable tool for research in anti-inflammatory and anti-cancer studies, including applications in multiple myeloma and leukemia. -
ACE/IKK-β/PKC Inhibitor
Plantainoside D is a phenylethanoid glycoside that functions primarily as an inhibitor of IKK-β, with additional inhibitory effects on angiotensin-converting enzyme (ACE) and protein kinase C (PKC). It exhibits significant biological activities, including the reduction of glutamate release in the rat cerebral cortex, alleviating cell apoptosis through the inhibition of reactive oxygen species (ROS) and NF-κB activation. Additionally, Plantainoside D has been shown to improve outcomes in acute lung injury induced by sepsis via modulation of the Sirt3/NLRP3 signaling pathway. This compound is applicable in studies of neuroprotection, antioxidant activity, anti-inflammatory responses, and antihypertensive effects. -
IKKβ/JAK2 Inhibitor
EC-70124 is an orally active multikinase inhibitor that targets IKKβ and JAK2. By blocking IkB phosphorylation and the activation of STAT3 (Tyr705), EC-70124 inhibits NF-κB nuclear translocation and impedes STAT3 transcriptional activity. This compound has demonstrated the ability to reduce tumor growth and diminish cancer stem cell populations in prostate cancer cells and xenograft models, making it a valuable tool for research in prostate cancer. -
IKKε/TBK-1 Inhibitor
MRT67307 hydrochloride is a selective inhibitor of IKKε and TBK-1, exhibiting IC50 values of 160 nM and 19 nM, respectively. Additionally, it inhibits ULK1 and ULK2 with IC50s of 45 nM and 38 nM, respectively. This compound is employed in research to study autophagy regulation and related cellular processes. It is particularly useful in investigations of inflammatory signaling pathways and cancer biology. -
IKKε/TBK-1 Inhibitor
MRT67307 dihydrochloride is a potent inhibitor of IKKε and TBK-1, demonstrating IC50 values of 160 nM and 19 nM, respectively. Additionally, this compound inhibits ULK1 and ULK2 with IC50s of 45 nM and 38 nM, respectively. MRT67307 dihydrochloride plays a significant role in blocking autophagy in cellular environments, making it a valuable tool for studies involving inflammation and autophagic processes. -
IKKε Inhibitor
IKKε-IN-1 is a selective inhibitor of IKKε, a key enzyme involved in the NF-κB signaling pathway. This compound effectively reduces cell viability, inhibits colony formation, and diminishes cell migration in various cancer cell lines. Additionally, IKKε-IN-1 induces autophagy, illustrating its potential as a research tool in the study of multiple cancer types, including colorectal, hepatocellular, bladder, breast, lung, and cervical cancers. -
IKKβ Inhibitor
IKKβ-IN-7 is a selective inhibitor of IKKβ, exhibiting an IC50 value of 9.44 μM. This compound induces DNA damage, S-phase cell cycle arrest, and apoptosis, while also promoting reactive oxygen species accumulation and loss of mitochondrial membrane potential. By inhibiting the phosphorylation of p65 and IκBα, IKKβ-IN-7 effectively restricts p65 nuclear translocation and modulates NF-κB-regulated gene expression. This agent demonstrates significant antitumor activity in xenograft models, particularly in colorectal cancer, while exhibiting low cytotoxicity in normal cells. IKKβ-IN-7 serves as a valuable tool for research in the field of colorectal cancer. -
PI3K/PIKK Inhibitor
PI3K/PIKK-IN-1 is a potent inhibitor of phosphoinositide 3-kinases (PI3K) and PI3-kinase-related kinases (PIKK). This compound is utilized in the development of antibody-drug conjugates (ADCs), making it valuable for therapeutic applications. It is particularly relevant in the research of various cancers, including breast cancer, multiple myeloma, Burkitt lymphoma, diffuse large B-cell lymphoma, and non-small cell lung cancer, aiding in the exploration of targeted cancer therapies.
