| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C25H28N8 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1, acting with an IC50 of 0.9 μM[1]. It is supplied as a light yellow to yellow solid (C25H28N8, MW 440.54) at 98.42% purity.
Physical & Chemical Properties
| CAS Number | 1875036-75-1 |
|---|---|
| Molecular Formula | C25H28N8 |
| Molecular Weight | 440.54 g/mol |
| Purity | 98.42% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | NCC1=CC=CC(CNC2=C(C3=NC=N2)N=CN=C3N4CCN(CC5=CC=CC=C5)CC4)=C1 |
| Signaling Pathway | Metabolic Enzyme/Protease |
| Solubility | In Vitro: DMSO: 83.33 mg/mL (189.15 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target
IC50: 0.9 μM (HUWE1)[1]
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 83.33 mg/mL (189.15 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (4.72 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 2.08 mg/mL (4.72 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In HeLa cells, BI8626 abolishes MCL1 ubiquitination by ectopically expressed HUWE1[1]. Colony formation by Ls174T cells is suppressed by BI8626 (estimated IC50 value of 0.7 μM), while BI8622 treatment (1-4 days) slows the passage of Ls174T cells through all phases of the cell cycle, most strongly in G1[1]. In U2OS cells, BI8626 (0-50 μM; 0-6 hours) slows MCL1 degradation after UV irradiation, to the same extent as HUWE1 depletion[1].
Cell Cycle Analysis[1]
| Cell Line | Ls174T cells |
|---|---|
| Concentration | 0 μM, 5 μM,10 μM, 15 μM, 20 μM |
| Incubation Time | 0-4 days |
| Result | Retarded passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1. |
Western Blot Analysis[1]
| Cell Line | U2OS cells |
|---|---|
| Concentration | 0 μM, 20 μM, 50 μM |
| Incubation Time | 0 hour,1 hour,2 hours,4 hours,6 hours |
| Result | Retarded the degradation of MCL1 in response to UV irradiation in HeLa cells by inhibiting HUWE1 in U2OS cells. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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HECT, UBA and WWE domain containing 1 represses cholesterol efflux during CD4+ T cell activation in Sjögren's syndrome. Front Pharmacol 2023 Jun 26:14:1191692. PMID: 37435494
Rapid proteasomal degradation of the stress response protein REDD2 is mediated by the E3 ligase HUWE1. Biochem Biophys Res Commun 2025 Sep 1:777:152270. PMID: 40609208