An inhibitor of the ETV1 transcription factor oncoprotein
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BRD32048

Item No. 16516

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N2-(4-methoxyphenyl)-6-(1-piperidinylmethyl)-1,3,5-triazine-2,4-diamine
CAS Number
433694-46-3
Molecular Formula
C16H22N6O
Formula Weight
314.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 2 mg/ml
λmax
269 nm
SMILES
COC1=CC=C(C=C1)NC2=NC(CN3CCCCC3)=NC(N)=N2
InChi Code
InChI=1S/C16H22N6O/c1-23-13-7-5-12(6-8-13)18-16-20-14(19-15(17)21-16)11-22-9-3-2-4-10-22/h5-8H,2-4,9-11H2,1H3,(H3,17,18,19,20,21)
InChi Key
PVHJDJWPRZUURH-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Cayman Chemical
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    Product 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.1 The ETV1 transcription factor is phosphorylated downstream of MAPK signaling and is acetylated at lysines 33 and 116 by the histone acetyltransferase p300.1 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.2 At 20-100 µM, BRD32048 can dose-dependently prevent invasion of ETV1-reliant cancer cells in in vitro models.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Oh, S., Shin, S., and Janknecht, R. ETV1, 4 and 5: An oncogenic subfamily of ETS transcription factors. Biochim. Biophys. Acta 1826(1), 1-12 (2012).

    2. Pop, M.S., Stransky, N., Garvie, C.W., et al. A small molecule that binds and inhibits the ETV1 transcription factor oncoprotein. Mol. Cancer Ther. 13(6), 1492-1502 (2014).