CAS NO: | 849234-64-6 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
生物活性 | 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 Ki of 0.2 and 1.5 nM, respectively. BRD-6929 can be used for mood-related behavioral model research[3]. | ||||||||||||||||
IC50& Target[1][3] |
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体外研究 (In Vitro) | 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 (Ki) and kinetics (half-life ‘T1/2′ in minutes) for HDAC 1, 2 and 3 incubated with BRD-6929 (10 μM), the Kivalues are<0.2 nM, 1.5nM, and 270 nM for HDAC 1, 2 and 3, respectively. The T1/2values 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]. | ||||||||||||||||
体内研究 (In Vivo) | BRD-6929 (intraperitoneal injection; 45 mg/kg; single dose) exhibits a Cmax, T1/2and AUC values of 17.7 μM, 7.2 hours, and 25.6 μM/L*hr, respectively in plasma. It shows a Cmax, T1/2and 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]. | ||||||||||||||||
分子量 | 351.42 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C19H17N3O2S | ||||||||||||||||
CAS 号 | 849234-64-6 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 5 mg/mL(14.23 mM;Need ultrasonic) 配制储备液
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