531057 ETV1 Inhibitor, BRD32048 - Calbiochem

531057
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Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₆H₂₂N₆O

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      Glass bottle 25 mg
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      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

      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 +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesPop, M.S., et al. 2014. Mol. Cancer Ther. 13, 1492.