- Cat. No.
- A19119
INH14
INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively.
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- Cat. No.
- A19438
GSK8612
GSK8612 is a highly selective and potent Tank-binding Kinase-1 (TBK1) inhibitor, with a pIC50 of 6.8 for recombinant TBK1.
In stock View Details -
- Cat. No.
- A20815
Ertiprotafib
Synonyms: PTP 112
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.
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- Cat. No.
- A21221
IKK-IN-1
IKK-IN-1 is an inhibitor of IKK extracted from patent WO2002024679A1, compound example 18-13.
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- Cat. No.
- A21588
IKK 16 hydrochloride
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.
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- Cat. No.
- A21972
BMS-066
BMS-066 is an IKKβ/Tyk2 pseudokinase inhibitor, with IC50s of 9 nM and 72 nM, respectively.
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- Cat. No.
- A22702
GS143
Synonyms: GS 143,GS-143
GS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation.
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- Cat. No.
- A27052
Abietic acid
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.
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- Cat. No.
- A30218
Plantainoside D
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.
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- Cat. No.
- A31801
ACHP
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.
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- Cat. No.
- A33350
EC-70124
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.
Out of stock
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- Cat. No.
- A36578
ITA-5
ITA-5 is a potent inhibitor of TBK1, derived from itaconic acid. It effectively reduces the phosphorylation of TBK1, IRF3, and STAT1, significantly inhibiting the secretion of IFN-β. This compound is valuable for investigations into autoimmune diseases and the modulation of excessive inflammation.
Out of stock
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- Cat. No.
- A39070
IKKβ-IN-7
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.
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- Cat. No.
- A39520
MRT67307 hydrochloride
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.
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- Cat. No.
- A39645
MRT67307 dihydrochloride
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.
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- Cat. No.
- A39655
IKKε-IN-1
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.
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- Cat. No.
- A41088
PI3K/PIKK-IN-1
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.
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- Cat. No.
- A52337
GSK2181306A
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.
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- Cat. No.
- A52603
FIKK9.1-IN-1
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.
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- Cat. No.
- A53910
AKCI
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.
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- Cat. No.
- A54064
TASIN-30
TASIN-30 is a selective inhibitor of the enoyl-CoA hydratase/3-hydroxyacyl-CoA dehydratase, targeting cholesterol biosynthesis by blocking the production of 7-dehydrocholesterol (7-DHC). With an EC50 of 0.097 μM, TASIN-30 effectively depletes downstream sterols, disrupts lipid raft integrity in tumor cells, and inhibits cell proliferation. This compound induces ferroptosis and apoptosis through reduced 7-DHC levels and enhanced phospholipid peroxidation. It demonstrates significant tumor suppression activity in nude mice models of osteosarcoma, making TASIN-30 a valuable tool for cancer research, particularly in osteosarcoma and colorectal cancer studies.
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- Cat. No.
- A71081
DSP-0390
DSP-0390 is an orally bioavailable inhibitor of Emopamil-binding protein (EBP). By targeting EBP, DSP-0390 disrupts the cholesterol de novo synthesis pathway in tumor cells, resulting in significant anti-tumor effects, particularly in an orthotopic xenograft model of glioblastoma (GBM). This compound is valuable for research focused on recurrent high-grade gliomas and their underlying mechanisms.
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- Cat. No.
- A79454
BAY-985
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.
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- Cat. No.
- A79455
TBK1-IN-1
TBK1-IN-1 is a selective inhibitor of TANK binding kinase 1 (TBK1) with an IC50 of 22.4 nM. This compound effectively inhibits the expression of downstream target genes such as cxcl10 and ifnβ, demonstrating its potential in modulating inflammatory responses. TBK1-IN-1 is also recognized for its anticancer activity, making it a valuable tool for research in cancer biology and inflammation-related studies.
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