1. NF-κB
  2. IKK
  3. HOIPIN-1

HOIPIN-1 (Synonyms: JTP-0819958)

Cat. No.: HY-122881
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HOIPIN-1 (JTP-0819958) is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM. HOIPIN-1 suppress LUBAC-mediated NF-kB activation in vitro.

For research use only. We do not sell to patients.

HOIPIN-1 Chemical Structure

HOIPIN-1 Chemical Structure

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Description

HOIPIN-1 (JTP-0819958) is a selective linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM[1]. HOIPIN-1 suppress LUBAC-mediated NF-kB activation in vitro[2].

IC50 & Target[1]

IKK-α

 

IKK-β

 

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[1].
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[1].
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[1].
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[1].
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[2].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

304.27

Formula

C₁₇H₁₃NaO₄

SMILES

O=C(O[Na])C1=CC=CC=C1/C=C/C(C2=CC=CC=C2OC)=O.[(E)]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

HOIPIN-1JTP-0819958HOIPIN1HOIPIN 1JTP0819958JTP 0819958IKKIκB kinaseI kappa B kinaseLUBACNF-kBubiquitinInhibitorinhibitorinhibit

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HOIPIN-1
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