BRD73954 |
| Katalog-Nr.GC12484 |
BRD73954 ist ein potenter HDAC-Inhibitor und hemmt selektiv sowohl HDAC6 als auch HDAC8 mit IC50-Werten von 0,0036, 0,12, 9, 12, 23 μM fÜr HDAC6, HDAC8, HDAC2, HDAC1 bzw. HDAC3. BRD73954 senkt die HDAC6-Spiegel, die mit der Hochregulierung von Ac-Tubulin verbunden sind.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1440209-96-0
Sample solution is provided at 25 µL, 10mM.
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BRD73954 is a potent and selective inhibitor of HDAC with IC50 values of 36 and 120 nM for HDAC6 and HDAC8, respectively [1].
Histone deacetylases (HADCs) are a series of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone and make the histones to wrap the DNA more tightly, which prevent transcription [1].
BRD73954 is a potent and selective HDAC inhibitor with IC50 values of 36 and 120 nM for HDAC6 and HDAC8, respectively. Also, BRD73954 inhibited HDAC1, HDAC2, HDAC3, HDAC4, HDAC5, HDAC7 and HDAC9 with IC50 values of 12, 9.0, 23, >33, >33, 13 and >33 μM, respectively. In HeLa cells, BRD73954 significantly increased α-tubulin acetylation, which was a substrate for HDAC6, while there was no change in the acetylation state of histone H3, which was a substrate for HDACs 1, 2 and 3 [1].
Reference:
[1]. Olson DE, Wagner FF, Kaya T, et al. Discovery of the first histone deacetylase 6/8 dual inhibitors. J Med Chem, 2013, 56(11): 4816-4820.
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