An inhibitor of ETV1 transcriptional activity that binds to ETV1 (KD = 17.1 µM in vitro)

BRD32048 – 1 mg

Brand:
Cayman
CAS:
433694-46-3
Storage:
-20
UN-No:
Non-Hazardous - /

ETS variant 1 (ETV1) is a transcription factor oncogene implicated in several cancers where it has been altered by chromosomal translocation, gene amplification, or lineage dysregulation.{26964} The ETV1 transcription factor is phosphorylated downstream of MAPK signaling and is acetylated at lysines 33 and 116 by the histone acetyltransferase p300.{26964} Both of these events increase the protein half-life of ETV1 and enhance its transcriptional activity. BRD32048 is a substituted [1,3,5]triazine derivative that inhibits ETV1 transcriptional activity by binding to ETV1 (KD = 17.1 µM in vitro), which reduces p300-dependent acetylation and stability of ETV1 and, thereby, promotes its degradation.{26612} At 20-100 µM, BRD32048 can dose-dependently prevent invasion of ETV1-reliant cancer cells in in vitro models.{26612}  

 

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Description

An inhibitor of ETV1 transcriptional activity that binds to ETV1 (KD = 17.1 µM in vitro), which reduces p300-dependent acetylation and stability of ETV1 and, thereby, promotes its degradation; dose-dependently prevents invasion of ETV1-reliant cancer cells in vitro

Formal name: N2-(4-methoxyphenyl)-6-(1-piperidinylmethyl)-1,3,5-triazine-2,4-diamine

Synonyms: 

Molecular weight: 314.4

CAS: 433694-46-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Transcription Factors

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