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531057 ETV1 Inhibitor, BRD32048 - Calbiochem

Cell-permeable, reversibly binds to ETV1 (KD = 17.1 µM) and reduces its transcriptional activity, independent of its binding to DNA.

ETV1 Inhibitor, BRD32048 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: N-(4-Methoxyphenyl)-6-(1-piperidinylmethyl)-1,3,5-triazine-2,4-diamine, ER81 Inhibitor, ETV1-mediated Transcription Inhibitor, Transcription Inhibitor ETV1 Inhibitor

Primary Target: ETS family transcription factor ETV1
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₆H₂₂N₆O

Products

Catalogue NumberPackaging Qty/Pack
5310570001 Glass bottle 25 mg
Description
OverviewA cell-permeable triazine compound that directly and reversibly binds to ETS family transcription factor ETV1 (KD = 17.1 µM) and reduces its transcriptional activity, independent of its binding to DNA. Selectively inhibits p300-dependent ETV1 acetylation at K33 and K116 and thereby promotes its degradation (~50 µM). Inhibits the invasion capacity of ETV1-dependent cell lines and primary melanocytes expressing NRASG12D, but not in primary melanocytes expressing NRAS. Does not affect PC3 cell line that is not dependent on ETV1 for invasion. Also it has no effect on the invasion of cancer cells expressing mutated ETV1 (K33R/K116R).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number531057
Brand Family Calbiochem®
SynonymsN-(4-Methoxyphenyl)-6-(1-piperidinylmethyl)-1,3,5-triazine-2,4-diamine, ER81 Inhibitor, ETV1-mediated Transcription Inhibitor, Transcription Inhibitor ETV1 Inhibitor
References
ReferencesPop, M.S., et al. 2014. Mol. Cancer Ther. 13, 1492.
Product Information
FormOff-white powder
Hill FormulaC₁₆H₂₂N₆O
Chemical formulaC₁₆H₂₂N₆O
ReversibleY
Quality LevelMQ100
Applications
Biological Information
Primary TargetETS family transcription factor ETV1
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
5310570001 04055977242539

Documentation

ETV1 Inhibitor, BRD32048 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

References

Reference overview
Pop, M.S., et al. 2014. Mol. Cancer Ther. 13, 1492.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision29-August-2014 JSW
SynonymsN-(4-Methoxyphenyl)-6-(1-piperidinylmethyl)-1,3,5-triazine-2,4-diamine, ER81 Inhibitor, ETV1-mediated Transcription Inhibitor, Transcription Inhibitor ETV1 Inhibitor
DescriptionA cell-permeable triazine compound that targets the ETS family transcription factor ETV1, but not TBX21, RELA, RUNX1, RFWD2, or P/CAF, via affinity interaction (KD = kd/ka = 5.853 x 10-2 s-1/4.128 x 103 M-1s-1= 14.2 µM) and selectively suppresses ETV1-, but not MITF-, dependent reporter transcription activity in 501mel melanoma cells (2.57-fold vs 4-fold of mock level in 24 h, respectively, with or without 10 µM BRD32048) without affecting ETV1 DNA-binding activity. Shown to inhibit ETV1-dependent invasion by downregulating p300-, but not P/CAF-, mediated ETV1 lysine acetylation (K-Ac) in LNCaP & 501mel cultures (50 µM for 16 h) that are known to harbor ETV1 chromosomal rearrangement (translocation) and amplification, respectively, resulting in enhanced ETV1 degradation, while ETV1 K-Ac is not detectable in PC3 (lacking ETV1 rearrangement) & SK-MEL-28 (wild-type ETV1) cells and no invasion inhibition by BRD32048 treatment is seen in these cultures. Likewise, BRD32048 is demonstrated to inhibit invasion of NRASG12D-expressing primary melanocytes (pmel) only when infected to express ETV1, and no inhibition is seen in the non-infected or MYC-infected cells.
FormOff-white powder
Intert gas (Yes/No) Packaged under inert gas
Chemical formulaC₁₆H₂₂N₆O
Purity≥95% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesPop, M.S., et al. 2014. Mol. Cancer Ther. 13, 1492.