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BI8622 is a ubiquitin ligase HUWE1-specific antagonist that restores the level of RP2 mutants in retinal cell lines and inhibits the activation of NLRP3, NLRC4, and AIM2 inflammatory vesicles in cells.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $116 | 6-8 weeks | 6-8 weeks | |
| 5 mg | $297 | 6-8 weeks | 6-8 weeks | |
| 25 mg | $987 | 6-8 weeks | 6-8 weeks | |
| 50 mg | $1,360 | 6-8 weeks | 6-8 weeks | |
| 100 mg | $1,860 | 6-8 weeks | 6-8 weeks | |
| 1 mL x 10 mM (in DMSO) | $365 | 6-8 weeks | 6-8 weeks |
| Description | BI8622 is a ubiquitin ligase HUWE1-specific antagonist that restores the level of RP2 mutants in retinal cell lines and inhibits the activation of NLRP3, NLRC4, and AIM2 inflammatory vesicles in cells. |
| Targets&IC50 | HUWE1:3.1 μM, Ls174T cells:8.4 μM, MCL1:6.8 μM |
| In vitro | BI8622 is a specific inhibitor of HUWE1 ubiquitin ligase with an IC50 of 3.1 μM.It inhibited ubiquitination of MCL1 in HeLa cells by ectopic expression of HUWE1, with an IC50 value of 6.8 μM.In addition, BI8622 inhibited clonogenic formation of Ls174T cells with an estimated IC50 of 8.4 μM. BI8622 (10 μM, 1-4 days treatment) delayed the progression of Ls174T cells at all stages of the cell cycle, with the most pronounced inhibitory effect in the G1 phase.BI8622 (0-50 μM, 16 hours treatment) prevented the degradation of MCL1 in HeLa cells under UV irradiation by inhibiting HUWE1. It also inhibited MYC-dependent transcriptional activation in colorectal cancer cells. [1] |
| Synonyms | BI 8622 |
| Molecular Weight | 426.51 |
| Formula | C25H26N6O |
| Cas No. | 1875036-74-0 |
| Smiles | N#CC1(C=2C=CC=CC2)CCN(C=3N=CN=C(C(=O)NC4=CC=C(C=C4)CN)C3C)CC1 |
| Relative Density. | 1.29 g/cm3 (Predicted) |
| Storage | keep away from direct sunlight,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (234.46 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (9.38 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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