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BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC 50 of 3.1 μM
In Vitro
BI8622 induces HUWE1 ectopically expresses to abolish ubiquitination of MCL1 with an IC 50 value of 6.8 μM in HeLa cells. BI8622 suppresses colony formation of Ls174T cells with estimated IC 50 value of 8.4 μM. BI8622 (10 μM; 1-4 days) treatment retards passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1. BI8622 (0-50 μM; 16 hours) retards the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells. BI8622 inhibits MYC-dependent transactivation in colorectal cancer cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Cycle AnalysisCell 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 AnalysisCell Line: HeLa cells Concentration: 0 μM, 10 μM, 20 μM Incubation Time: 16 hours Result: Retarded the degradation of MCL1 in response to UV irradiation by inhibiting HUWE1 in HeLa cells.
Form:Solid
IC50& Target:IC50: 3.1 μM (HUWE1)
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Visualizza scheda tecnica →Attributi di qualità completi e criteri di accettazione per questa qualità.
Visualizza scheda delle specifiche →Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Benzenoids |
| Classe | Benzene and substituted derivatives |
| Subclass | Anilides |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Aromatic anilides |
| Alternative Parents | Phenylpiperidines Pyrimidinecarboxylic acids and derivatives Dialkylarylamines Aminopyrimidines and derivatives Imidolactams Heteroaromatic compounds Amino acids and derivatives Nitriles Carboxylic acid amides Azacyclic compounds Organopnictogen compounds Organooxygen compounds Organic oxides Monoalkylamines Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteromonocyclic compounds |
| Substituents | Aromatic anilide - Phenylpiperidine - Pyrimidine-6-carboxylic acid or derivatives - Dialkylarylamine - Tertiary aliphatic/aromatic amine - Aminopyrimidine - Imidolactam - Pyrimidine - Piperidine - Heteroaromatic compound - Tertiary amine - Carboxamide group - Amino acid or derivatives - Azacycle - Organoheterocyclic compound - Nitrile - Carbonitrile - Carboxylic acid derivative - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Primary aliphatic amine - Amine - Aromatic heteromonocyclic compound |
| Descrizione | This compound belongs to the class of organic compounds known as aromatic anilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with an aromatic group. They have the general structure RNC(=O)R', where R= benzene, and R = aryl group. |
| External Descriptors | Not available |
| Solubilità | DMSO : 125 mg/mL (293.08 mM; Need ultrasonic) |
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