IκK/IκB

Cat. No.

A41088

CAS No.

3109464-35-6

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.

Cat. No.

A52337

CAS No.

2579173-55-8

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.

Cat. No.

A52603

CAS No.

1448523-50-9

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.

Cat. No.

A53910

CAS No.

669750-88-3

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.

Cat. No.

A54064

CAS No.

1678515-93-9

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.

Cat. No.

A71081

CAS No.

2376765-57-8

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.

Cat. No.

A79454

CAS No.

2409479-29-2

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.

Cat. No.

A79455

CAS No.

3041973-64-9

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.

Cat. No.

A79456

CAS No.

1571-30-8

BAY32-5915

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.

Cat. No.

A79457

CAS No.

1227098-15-8

NF-κB-IN-1

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.

Cat. No.

A79459

CAS No.

84955-31-7

6-Chloro-7-deazaguanine

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.

Cat. No.

A79460

CAS No.

3061890-98-7

SU1261

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.

Cat. No.

A79461

CAS No.

2055101-86-3

SR12343

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.

Cat. No.

A79462

CAS No.

1381930-17-1

TBK1/IKKε-IN-4

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.

Cat. No.

A79463

CAS No.

113760-29-5

BOT-64

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.

Cat. No.

A79464

CAS No.

354811-10-2

IKK2-IN-4

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.

Cat. No.

A79465

CAS No.

928655-63-4

HPN-01

HPN-01 is a potent and selective inhibitor of IκB kinase (IKK), demonstrating pIC50 values of 6.4, 7.0, and

Cat. No.

A79466

CAS No.

4815-35-4

IKKβ-IN-4

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.

Cat. No.

A79467

CAS No.

1782573-78-7

MLN120B dihydrochloride

Synonyms: ML120B dihydrochloride

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.

Cat. No.

A79468

CAS No.

916985-21-2

IKK2-IN-3

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.

Cat. No.

A79469

CAS No.

946518-61-2

LY2409881 (free base)

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.

Cat. No.

A79471

CAS No.

2101925-20-4

(Rac)-BAY-985

(Rac)-BAY-985 is a potent ATP-competitive inhibitor targeting TBK1, demonstrating a remarkable IC50 of 1.5 nM. This compound exhibits significant antitumor efficacy, making it a valuable tool for cancer research. Its selective inhibition of TBK1 provides insights into the role of this kinase in various biological processes and disease mechanisms.

Cat. No.

A79472

CAS No.

615529-94-7

IKK-IN-4

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.

Cat. No.

A79474

CAS No.

1356225-62-1

SR8185

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.

Cat. No.

A79475

CAS No.

2410423-31-1

IKKβ-IN-1

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.