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HOIPIN-8
- Parent CAS: 2519537-69-8
- Soluble in DMSO
- MF: C23H15F2N4NaO3
- MW: 456.38
Description
HOIPIN-8 is a potent inhibitor of the linear ubiquitin chain assembly complex (LUBAC) with an IC50 value of 11 nM. HOIPIN-8 suppresses LUBAC-mediated activation of NF-κB signaling without inducing cytotoxicity, making it a valuable chemical probe for investigating linear ubiquitination pathways.
LUBAC, consisting of HOIP (RNF31), HOIL-1L, and SHARPIN, is the only E3 ubiquitin ligase complex capable of generating linear (M1-linked) ubiquitin chains. Linear ubiquitination plays a critical role in regulating NF-κB activation, inflammation, innate immunity, cell survival, and immune homeostasis. HOIPIN-8 is widely used for mechanistic studies of LUBAC and HOIP (RNF31) function and provides a powerful tool for investigating ubiquitin signaling and inflammatory pathways.
Key Features
- Potent LUBAC inhibitor
- IC50: 11 nM
- Suppresses NF-κB signaling
- Non-cytotoxic under experimental conditions
- Useful tool for HOIP (RNF31) and ubiquitin biology research
Applications
- LUBAC and linear ubiquitination research
- NF-κB signaling studies
- Inflammation and innate immunity investigations
- Ubiquitin biology and signal transduction research
- HOIP (RNF31) target validation studies
Related Products
HOIPIN-11a (Axon 3064) is an advanced HOIP/LUBAC inhibitor that is frequently preferred for in vivo studies. While HOIPIN-8 is widely used for in vitro mechanistic investigations of LUBAC and RNF31 function, HOIPIN-11a offers an excellent alternative for studies requiring in vivo activity.
More Information
| Parent CAS No. | 2519537-69-8 |
|---|---|
| Chemical Name | Sodium (E)-2-(3-(2,6-difluoro-4-(1H-pyrazol-4-yl)phenyl)-3-oxoprop-1-enyl)-4-(1-methyl-1H-pyrazol-4-yl)benzoate |
| SMILES | C1C=C(C(=O)[O-])C(/C=C/C(=O)C2C(F)=CC(C3=CNN=C3)=CC=2F)=CC=1C1C=NN(C)C=1.[Na+] |
| MFCD | N.A. |
| InChi | InChI=1S/C23H16F2N4O3.Na/c1-29-12-17(11-28-29)13-2-4-18(23(31)32)14(6-13)3-5-21(30)22-19(24)7-15(8-20(22)25)16-9-26-27-10-16;/h2-12H,1H3,(H,26,27)(H,31,32);/q;+1/p-1/b5-3+; |
| InChiKey | DLJPWYFLGYVMKV-WGCWOXMQSA-M |
| CID | 146018039 |
| Short Description | LUBAC inhibitor |
References
- K 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.
- Z Zhang et al. RNF31 inhibition sensitizes tumors to bystander killing by innate and adaptive immune cells. Cell Rep Med. 2022 Jun 21;3(6):100655.
- List of publications using HOIPIN-8 (Axon 2972) purchased from Axon Medchem
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