Product Information
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.

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Categories

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Other Inhibitors of Biological Interest