TH34 是一种 HDAC6/8/10 抑制剂，IC50值分别为 4.6、1.9 和 7.7 μM。它显示出比 HDAC1/2/3 高的选择性。

TH34 is an HDAC6/8/10 inhibitor (IC50s: 4.6/1.9/7.7 μM). It shows high selectivity over HDAC1/2/3.

TH34 is well-tolerated by non-transformed human skin fibroblasts at concentrations up to 25 μM and modestly impairs colony growth in medulloblastoma cell lines, but specifically induces caspase-dependent programmed cell death in a concentration-dependent manner in several human neuroblastoma cell lines.

HeLa cells, stably transfected with NanoBRET plasmids NanoLuc?-HDAC6 FL Fusion Vector and NanoLuc?-HDAC10 FL Fusion Vector were seeded at 20,000 cells/well in white 96-well plates. Without further incubation, tracer (0.3 μM) and drugs were added in separate steps and plates were placed in a tissue culture incubator for 2 h. For NanoBRET quantification, plates were put at room temperature for 10 min. Nanoglow substrate, diluted in OptiMEM without phenol red, was added and measured within 10 min in an OPTIMA plate reader (460 nm emission for donor and 610LP filter for acceptor). The BRET signal was calculated by the ratio of acceptor signal to donor signal.

2196203-96-8

C15H16N2O2

256.305

DMSO:80 mg/mL (312.13 mM)
H2O:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years