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HOIPIN-1

CAS No. :

MCE 站：HOIPIN-1

产品活性：HOIPIN-1 (JTP-0819958) 是一种选择性线性泛素链组装复合物 (LUBAC) 抑制剂，IC₅₀ 值 >2.8 μM。HOIPIN-1 抑制 LUBAC 介导的 NF-kB 激活。

研究领域：NF-κB

作用靶点：IKK

In Vitro: In?the HTRF-based LUBAC-mediated ubiquitination assay with Petit-LUBAC. HOIPIN-1 (0.9-120 μM) exhibits an increased inhibitory activity with a a longer preincubation time in the reaction buffer. The IC₅₀ values are 26 μM, 26 μM, 26 μM, and 3.926 μM, at 1h, 3h, 6h and 24 h, respectively.
The coexpression of the LUBAC subunits in HEK293T cells increases the intracellular amounts of linear polyubiquitin, HOIPIN-1 (1-30 μM) dose dependently suppressed the production of intracellular linear polyubiquitin in LUBAC-expressing HEK293T cells.
HOIPIN-1 (30-100 μM; 30-60 mins) inhibits IL-1β-induced NF-κB activation and decreases the phosphorylation of IKKα/β, p105, and p65 in hela cells.
HOIPIN-1 (10-100 μM) inhibits the expression of NF-κB target genes such as?ICAM1?and?TNF-α in IL-1β-induced hela cells in a dose-dependent manner.
The linear ubiquitin chain assembly complex (LUBAC), composed of the HOIL-1L, HOIP, and SHARPIN subunits. HOIPIN-1 exhibits IC₅₀ values of 4.4 μM, 3.5 μM and 3.7 μM for inhibition of linear polyubiquitination activity by the HOIL-1L/HOIP complex, the HOIL-1L/HOIP/SHARPIN complex and the HOIP/SHARPIN complex, respectively.
HOIPIN-1 (1-100 μM; 72 hours) shows no apparent cytotoxicity based on ATP content, it exhibits cytotoxicity in A549 cells with an IC₅₀>100 μM in A549 cells.

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