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HomeProduct name listBRD32048

BRD32048

BRD32048 Structural

What is BRD32048?

Description

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. The ETV1 transcription factor is phosphorylated downstream of MAPK signaling and is acetylated at lysines 33 and 116 by the histone acetyltransferase p300. 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. At 20-100 μM, BRD32048 can dose-dependently prevent invasion of ETV1-reliant cancer cells in in vitro models.

Definition

ChEBI: N2-(4-methoxyphenyl)-6-(1-piperidinylmethyl)-1,3,5-triazine-2,4-diamine is a member of methoxybenzenes and a substituted aniline.

Properties of BRD32048

Boiling point: 545.3±60.0 °C(Predicted)
Density  1.268±0.06 g/cm3(Predicted)
solubility  DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml; Ethanol: 2 mg/ml
form  A crystalline solid
pka 7.87±0.10(Predicted)
color  White to off-white

Safety information for BRD32048

Computed Descriptors for BRD32048

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