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

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.

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HOIPIN-8 Chemical Structure

HOIPIN-8 Chemical Structure

CAS No. : 2519537-70-1

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1 mg USD 140 In-stock
5 mg USD 350 In-stock
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Based on 1 publication(s) in Google Scholar

HOIPIN-8 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE HOIPIN-8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

HOIPIN-8 Related Antibodies

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
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°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 : 100 mg/mL (219.12 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 2.1912 mL 10.9558 mL 21.9116 mL
5 mM 0.4382 mL 2.1912 mL 4.3823 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.

  • Molarity Calculator

  • Dilution Calculator

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: 1.25 mg/mL (2.74 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 1.25 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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

Purity: 99.89%

COA (248 KB) HNMR (584 KB) LCMS (95 KB)

Handling Instructions (2659 KB)
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 2.1912 mL 10.9558 mL 21.9116 mL 54.7789 mL
5 mM 0.4382 mL 2.1912 mL 4.3823 mL 10.9558 mL
10 mM 0.2191 mL 1.0956 mL 2.1912 mL 5.4779 mL
15 mM 0.1461 mL 0.7304 mL 1.4608 mL 3.6519 mL
20 mM 0.1096 mL 0.5478 mL 1.0956 mL 2.7389 mL
25 mM 0.0876 mL 0.4382 mL 0.8765 mL 2.1912 mL
30 mM 0.0730 mL 0.3652 mL 0.7304 mL 1.8260 mL
40 mM 0.0548 mL 0.2739 mL 0.5478 mL 1.3695 mL
50 mM 0.0438 mL 0.2191 mL 0.4382 mL 1.0956 mL
60 mM 0.0365 mL 0.1826 mL 0.3652 mL 0.9130 mL
80 mM 0.0274 mL 0.1369 mL 0.2739 mL 0.6847 mL
100 mM 0.0219 mL 0.1096 mL 0.2191 mL 0.5478 mL
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HOIPIN-8 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-82519537-70-1HOIPIN8HOIPIN 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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