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IκK/IκB

IκK/IκB inhibitors act on the IκB kinase (IKK) complex, which frees nuclear factor kappa B (NF-κB) from IκB. In 1997 a cytokine-responsive IKK was purified, and the complex was shown to contain two catalytic subunits, IKKα and IKKβ. The kinases phosphorylate IκBα, which marks this inhibitor for degradation and frees NF-κB dimers to enter the nucleus. BMS-345541 HCl, described in 2003, binds an allosteric site on IKK and blocks NF-κB-dependent transcription. IKK-16 inhibits IKKβ and the IKK complex, while IMD 0354 and Bay 65-1942 HCl act mainly on IKKβ. BAY 11-7085 is used to block IκBα phosphorylation in cells. BX-795 targets the related TANK-binding kinase 1 (TBK1) and IKKε along with 3-phosphoinositide-dependent protein kinase 1 (PDK1).

Cat. No.

A24827

CAS No.

2052306-13-3

PROTAC TBK1 degrader-2

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.

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$275.00

5 mg

$850.00

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Cat. No.

A25211

CAS No.

2826215-20-5

PROTAC IKKβ/NR4A1 degrader-1

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.

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