HOIPIN-1 (Synonyms: JTP-0819958) |
Catalog No.GC62161
One-Click Copy Product Info
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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.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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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[1]. HOIPIN-1 suppress LUBAC-mediated NF-kB activation in vitro[2].
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].
[1]. Ken Katsuya, et al. High-Throughput Screening for Linear Ubiquitin Chain Assembly Complex (LUBAC) Selective Inhibitors Using Homogenous Time-Resolved Fluorescence (HTRF)-Based Assay System. SLAS Discov. 2018 Dec;23(10):1018-1029
[2]. Ken Katsuya, et al. Small-molecule inhibitors of linear ubiquitin chain assembly complex (LUBAC), HOIPINs, suppress NF-κB signaling. Biochem Biophys Res Commun. 2019 Feb 12;509(3):700-706.
| Cas No. | SDF | ||
| Synonyms | JTP-0819958 | ||
| Formula | C17H13NaO4 | M.Wt | 304.27 |
| Solubility | DMSO : 5 mg/mL (16.43 mM; Need ultrasonic) | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2866 mL | 16.4328 mL | 32.8655 mL |
| 5 mM | 657.3 μL | 3.2866 mL | 6.5731 mL |
| 10 mM | 328.7 μL | 1.6433 mL | 3.2866 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >97.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)