2. NF-κB
  3. IKK
  4. HOIPIN-1

HOIPIN-1  (Synonyms: JTP-0819958)

Cat. No.: HY-122881 Purity: 97.28%
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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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Based on 1 publication(s) in Google Scholar

HOIPIN-1 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE HOIPIN-1

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IKK-α IKK-β IKK IKKε TBK1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

HOIPIN-1 Related Antibodies
Molecular Weight

304.28

Formula

C17H13NaO4
Appearance

Solid

Color

White to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 5 mg/mL (16.43 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2864 mL 16.4322 mL 32.8645 mL
5 mM 0.6573 mL 3.2864 mL 6.5729 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 0.5 mg/mL (1.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 0.5 mg/mL (1.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2864 mL 16.4322 mL 32.8645 mL 82.1612 mL
5 mM 0.6573 mL 3.2864 mL 6.5729 mL 16.4322 mL
10 mM 0.3286 mL 1.6432 mL 3.2864 mL 8.2161 mL
15 mM 0.2191 mL 1.0955 mL 2.1910 mL 5.4774 mL
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HOIPIN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

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

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