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BRD 9757

Names

[ CAS No. ]:
1423058-85-8

[ Name ]:
BRD 9757

Biological Activity

[Description]:

BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC50 of 30 nM. BRD9757 shows excellent selectivity toward HDAC6 versus the class I (>20-fold) and class II (>400-fold) HDACs[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC
Signaling Pathways >> Epigenetics >> HDAC

[Target]

HDAC6:0.03 μM (IC50)

HDAC1:0.638 μM (IC50)

HDAC2:1.79 μM (IC50)

HDAC3:0.694 μM (IC50)

HDAC4:21.80 μM (IC50)

HDAC5:18.32 μM (IC50)

HDAC7:12.61 μM (IC50)

HDAC8:1.09 μM (IC50)

HDAC9:>33.33 μM (IC50)


[In Vitro]

BRD9757（化合物 14）对抗 HDAC1、HDAC2、HDAC3、HDAC4、HDAC5、HDAC7、HDAC8 和 HDAC9，IC50 值分别为 0.638 μM、1.79 μM、0.694 μM、21.80 μM、18.32 μM、12.61 μM、1.09 μM 和 >33.33 μM[1]。 BRD9757（化合物 14；10-30 μM；24 小时）选择性地增加 Ac-tubulin 的水平，而不增加组蛋白乙酰化[1]。 Western Blot Analysis[1] Cell Line: HeLa cells Concentration: 10 μM and 30 μM Incubation Time: for 24 h Result: Increased the level of Ac-tubulin.

[References]

[1]. Florence F Wagner, et al. Potent and selective inhibition of histone deacetylase 6 (HDAC6) does not require a surface-binding motif. J Med Chem. 2013 Feb 28;56(4):1772-6.  

Chemical & Physical Properties

[ Molecular Formula ]:
C6H9NO2

[ Molecular Weight ]:
127.14100

[ Exact Mass ]:
127.06300

[ PSA ]:
49.33000

[ LogP ]:
0.99300

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H319-H412

[ Precautionary Statements ]:
P273-P305 + P351 + P338

[ RIDADR ]:
NONH for all modes of transport

Related Compounds