BAY-850
A chemical probe for ATAD2A
This probe is available from Sigma
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overview
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properties
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references
overview
Probe | | Negative control |
| | |
BAY-850 | | BAY-460 |
ATAD2 and ATAD2B are epigenetic regulators known to function as co-factors for oncogenic transcription factors. ATAD2 overexpression correlates with poor outcomes in several cancers. The bromodomain module of ATAD2 has been shown to be essential for its association with acetylated chromatin and presumable function.
BAY-850 is a chemical probe for the ATAD2A bromodomain which displaces acetylated H4 peptide from the ATAD2 bromodomain with an IC50 value of 20 nM (HTRF). MST and BROMOscan measurements indicate a Kd of 84.9 nM and 120 nM, respectively. BAY-850 displays exquisite selectivity over all other bromodomains (no hits in BROMOscan at 10 µM) and displaces full-length ATAD2 from chromatin in live cells at a concentration of 1 µM as determined by FRAP. To avoid potential unspecific off-target effects concentrations of ≥ 5 µM are not recommended.
BAY-460 is a companion control compound with strongly reduced potency against ATAD2 (HTRF IC50 = 16 µM, no activity in BROMOscan at 10 µM test concentration).
Properties
ATAD2H4AcK5/8/12/16 IC50 (HTRF) | 0.02 μM |
LLElogD | 2.6 |
ATAD2 TSA ΔT(100μM) | 13.9°C |
BRD4 BD1 IC50 (HRTF) | >20 μM |
BRD4BD2 IC50 (HTRF) | >20 μM |
DiscoverX BromoScan | ATAD2A @ 10 μM |
DiscoverX ATAD2A KD | 0.12 μM |
MST KD | 0.08 μM |
Sw pH 6.5 [mg/L] | >500* |
log D (pH 7.5) | 2.9 |
*HCl salt
properties
Probe | | Negative control |
| | |
BAY-850 | | BAY-460 |
references
Fernández-Montalván, A., Berger, M., Kuropka, B., Koo, S., Badock, V., & Weiske, J. et al. (2017). Isoform-Selective ATAD2 Chemical Probe with Novel Chemical Structure and Unusual Mode of Action. ACS Chemical Biology. http://dx.doi.org/10.1021/acschembio.7b00708