1. Metabolic Enzyme/Protease
  2. E1/E2/E3 Enzyme
  3. HOIPIN-8

HOIPIN-8 

Cat. No.: HY-122882
Handling Instructions

HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC.

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

HOIPIN-8 Chemical Structure

HOIPIN-8 Chemical Structure

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Description

HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC[1].

In Vitro

HOIPIN-8 (0-100 μM; 72 hours) has little cell toxicity on A549 cells, and exhibits an IC50 value of 100 μM[1].
HOIPIN-8 (0-10 μM; 24 hours) has an inhibitory effect over 10-fold enhancement over that of HOIPIN-1 on NF-κB activation, exhibits an IC50 value of 0.42 μM in HEK293T cells[1].
HOIPIN-8 (0-30 μM; NF-κB luciferase reporter is transfected into cells for 18 hours; then with 10 ng/ml TNF-α for 6 h) exhibits a 4-fold enhancements of the potency than HOIPIN-1, the IC50 value is 11.9 μM. It also effectively reduces IL-1β-induced expression of NF-κB target genes, such as ICAM1 and IL-6 as compared to HOIPIN-1[1].

Cell Viability Assay[1]

Cell Line: Human lung carcinoma A549 cells, HEK293T cells 
Concentration: 0 μM; 1 μM; 3 μM; 10 μM; 30 μM; 100 μM
Incubation Time: 72 hours
Result: Did not effect A549 cell viability.

RT-PCR[1]

Cell Line: HEK293T cells 
Concentration: 0 μM; 0.3 μM; 1 μM; 10 μM; 30 μM
Incubation Time: 24 hours
Result: Had an inhibitory effect on the inflammatory cytokine-induced NF-κB activation pathway.
Molecular Weight

456.38

Formula

C₂₃H₁₅F₂N₄NaO₃

SMILES

O=C(O[Na])C1=CC=C(C2=CN(C)N=C2)C=C1/C=C/C(C3=C(F)C=C(C4=CNN=C4)C=C3F)=O

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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-8HOIPIN8HOIPIN 8E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseB cell lymphomaABC-DLBCLinear?ubiquitin?chain assembly complexLUBACHOIPIN derivativeA549cellsHEK293TInhibitorinhibitorinhibit

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HOIPIN-8
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HY-122882
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