BRD-6929 是 I 类组蛋白去乙酰化酶 HDAC1 和 HDAC2 的脑渗透性选择性抑制剂 (IC₅₀= 1 和 8 nM)。BRD-6929 对 HDAC1 和 HDAC2 有高亲和力 (K_i = 0.2 和 1.5 nM)。BRD-6929 可用于情绪相关行为的研究。

BRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylase HDAC1 and HDAC2 inhibitor with IC 50 of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity to HDAC1 and HDAC2 with K i  of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research.

Solid

HDAC1 1 nM (IC50) HDAC2 8 nM (IC50

In vitro IC50 for HDAC1-9 by BRD-6929 using recombinant human HDAC enzymes and HDAC class-specific substrates. BRD-6929 and substrate are incubated for 180 min (HDAC1-3) to control for HDAC1-3 inhibition, BRD-6929 is against HDAC1, HDAC2, HDAC3 and HDAC4-9 with IC50s of 0.001 μM, 0.008 μM, 0.458 μM and >30 μM, respectively.
In vitro binding affinity (Ki) and kinetics (half-life ‘T1/2′ in minutes) for HDAC 1, 2 and 3 incubated with BRD-6929 (10 μM), the Ki values are <0.2 nM, 1.5nM, and 270 nM for HDAC 1, 2 and 3, respectively. The T1/2 values are >2400 mins, >4800 mins, and 1200 mins for HDAC 1, 2 and 3, respectively.
BRD-6929 (1 and 10 uM) does not cause an increase or decrease in overall cell number in brain region specific primary cultures. Additionally, BRD-6929 (10 uM

BRD-6929 (intraperitoneal injection; 45 mg/kg; single dose) exhibits a C max , T 1/2 and AUC values of 17.7 μM, 7.2 hours, and 25.6 μM/L*hr, respectively in plasma. It shows a C max , T 1/2 and AUC values of 0.83 μM, 6.4 hours, and 3.9 μM/L*hr, respectively in brain.
BRD-6929 (intraperitoneal injection; 45 mg/kg; 10 days) acts as a deacetylase inhibitor in mouse brain. It significantly increases acetylation in each brain region by 1.5- to 2.0-fold compared to vehicle. The western blotting reveals that BRD-6929 significantly increases acetylation of histone H2B (tetra-acetylated), H3K9 and H4K12 in cortex, ventral striatum and hippocampus after the 10th daily treatment in adult male C57BL/6J mice.
has not independently confirmed the accuracy of these methods.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；In solvent -80°C 6 months

[1]. Li-Huei Tsai, et al. Inhibition of hdac2 to promote memory. patent/US20120101147
[2]. Schroeder FA, et al. A selective HDAC 1/2 inhibitor modulates chromatin and gene expression in brain and altersmouse behavior in two mood-related tests. PLoS One. 2013 Aug 14;8(8):e71323.
[3]. Huang L, et al. Elimination of HIV-1 Latently Infected Cells by Gnidimacrin

In Vitro: DMSO : 5 mg/mL (14.23 mM; Need ultrasonic)配制储备液