BRD-6929 is a potent, selective brain-penetrant inhibitor of class I histone deacetylaseHDAC1andHDAC2inhibitor withIC₅₀of 1 nM and 8 nM, respectively. BRD-6929 shows high-affinity toHDAC1andHDAC2with K_i of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research^[3].

In vitro IC₅₀for 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^[1].
In vitro binding affinity (K_i) and kinetics (half-life ‘T_1/2′ in minutes) for HDAC 1, 2 and 3 incubated with BRD-6929 (10 μM), the K_ivalues are<0.2 nM, 1.5nM, and 270 nM for HDAC 1, 2 and 3, respectively. The T_1/2values are >2400 mins, >4800 mins, and 1200 mins for HDAC 1, 2 and 3, respectively^[1].
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) causes an increase in H4K12 acetylation in brain region specific primary cultures (striatum)^[1].
BRD-6929 (1-10 uM; 6 hours) causes a significant increase in H2B acetylation in primary neuronal cell cultures. BRD-6929 (1-20 uM; 24 hours) induces a dose-dependent acetylation of H4K12ac with an EC₅₀of 7.2 μM in cultured neurons^[1].
BRD-6929 potentiates the efficacy of gnidimacrin (a PKC Agonist) against latent HIV-1^[3].

BRD-6929 (intraperitoneal injection; 45 mg/kg; single dose) exhibits a C_max, T_1/2and AUC values of 17.7 μM, 7.2 hours, and 25.6 μM/L*hr, respectively in plasma. It shows a C_max, T_1/2and AUC values of 0.83 μM, 6.4 hours, and 3.9 μM/L*hr, respectively in brain^[1].
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^[1].

351.42

Solid

C₁₉H₁₇N₃O₂S

849234-64-6

Room temperature in continental US; may vary elsewhere.

DMSO : 5 mg/mL(14.23 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 2.08 mg/mL (5.92 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (5.92 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明