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HOIPIN-1

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Catalog No. T78557Cas No. 2470242-33-0
Alias JTP0819958

HOIPIN-1 (JTP0819958) is a selective and potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) (IC50 >2.8 μM).HOIPIN-1 inhibits LUBAC-mediated NF-kB activation.

HOIPIN-1

HOIPIN-1

🥰Excellent
Purity: 98.83%
Catalog No. T78557Alias JTP0819958Cas No. 2470242-33-0
HOIPIN-1 (JTP0819958) is a selective and potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) (IC50 >2.8 μM).HOIPIN-1 inhibits LUBAC-mediated NF-kB activation.
Pack SizePriceAvailabilityQuantity
1 mg$195In Stock
5 mg$465In Stock
10 mg$679In Stock
25 mg$1,070In Stock
50 mg$1,430In Stock
100 mg$1,930In Stock
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Purity:98.83%
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Product Introduction

Bioactivity
Description
HOIPIN-1 (JTP0819958) is a selective and potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) (IC50 >2.8 μM).HOIPIN-1 inhibits LUBAC-mediated NF-kB activation.
Targets&IC50
HOIL-1L/HOIP:4.4 μM, HOIP/SHARPIN:3.7 μM, A549 cells:100 μM, LUBAC:26 μM, HOIL-1L/HOIP/SHARPIN:3.5 μM
In vitro
In the HTRF-based analysis of LUBAC-mediated ubiquitination using Petit-LUBAC, the preincubation time of HOIPIN-1 (0.9-120 μM) in the reaction buffer correlates with increased inhibitory activity. The IC50 values at 1 h, 3 h, 6 h, and 24 h are 26 μM, 26 μM, 26 μM, and 3.926 μM, respectively[1].
Co-expression of LUBAC subunits in HEK293T cells increases the level of intracellular linear polyubiquitin chains. HOIPIN-1 (1-30 μM) dose-dependently inhibits the production of intracellular linear polyubiquitin chains in HEK293T cells expressing LUBAC[1].
In HeLa cells, HOIPIN-1 (30-100 μM; 30-60 minutes) inhibits IL-1β-induced NF-κB activation and reduces the phosphorylation of IKKα/β, p105, and p65. Furthermore, at doses of 10-100 μM, HOIPIN-1 dose-dependently inhibits the expression of NF-κB target genes such as ICAM1 and TNF-α induced by IL-1β in HeLa cells[1].
The linear ubiquitin chain assembly complex (LUBAC) consists of HOIL-1L, HOIP, and SHARPIN subunits. HOIPIN-1 inhibits the linear polyubiquitination activity of the HOIL-1L/HOIP complex, HOIL-1L/HOIP/SHARPIN complex, and HOIP/SHARPIN complex with IC50 values of 4.4 μM, 3.5 μM, and 3.7 μM, respectively[2].
In A549 cells, HOIPIN-1 (1-100 μM; 72 hours) shows no apparent cytotoxicity based on ATP content. However, it exhibits cytotoxicity in A549 cells with an IC50 > 100 μM[2].
AliasJTP0819958
Chemical Properties
Molecular Weight304.27
FormulaC17H13NaO4
Cas No.2470242-33-0
SmilesO=C(C1=C(C=CC(C2=C(OC)C=CC=C2)=O)C=CC=C1)[O-].[Na+]
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 3.33 mg/mL (10.96 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM3.2866 mL16.4328 mL32.8655 mL164.3277 mL
5 mM0.6573 mL3.2866 mL6.5731 mL32.8655 mL
10 mM0.3287 mL1.6433 mL3.2866 mL16.4328 mL

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