BRD3308 是一种高选择性的HDAC3抑制剂，IC50为 54 nM。BRD3308 对HDAC3的选择性是 HDAC1 (IC50为 1.26 μM) 或 HDAC2 (IC50为 1.34 μM) 的 23 倍。BRD3308 抑制由炎性细胞因子或糖脂毒性应激诱导的胰腺 β 细胞凋亡，并增加功能性胰岛素释放。BRD3308 还可激活HIV-1转录并破坏HIV-1潜伏期。
| 生物活性 | BRD3308 is a highly selectiveHDAC3inhibitor with anIC50of 54 nM. BRD3308 is 23-fold selectivity forHDAC3overHDAC1(IC50of 1.26 μM) orHDAC2(IC50of 1.34 μM). BRD3308 suppresses pancreatic β-cellapoptosisinduced by inflammatory cytokines or glucolipotoxic stress, and increases functionalinsulinrelease. BRD3308 activatesHIV-1transcription and disruptsHIV-1latency[1][2][3]. |
| IC50& Target[1][3] | HDAC3 54 nM (IC50) | HDAC3 29 nM (Ki) | HDAC1 1260 nM (IC50) | HDAC1 5100 nM (Ki) | HDAC2 1340 nM (IC50) | HDAC2 6300 nM (Ki) | HIV-1 |
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体外研究
(In Vitro) | BRD3308 (5-30 μM; 6-24 hours) treatment increases HIV-1 expression in the 2D10 cell line[1].
BRD3308 (15 μM; overnight) is able to induce outgrowth of HIV-1 from latently infected cells ex vivo in resting CD4+ T cells[1].
BRD3308 inhibits HDAC1, HDAC2 and HDAC3 with Kivalues of 5.1 μM, 6.3 μM and 29 nM, respectively[3].
RT-PCR[1] | Cell Line: | 2D10 cells | | Concentration: | 5 μM, 10 μM, 15 μM, or 30 μM | | Incubation Time: | 6 hours, 12 hours, 18 hours, or 24 hours | | Result: | An increase in HIV-1 expression was observed. |
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体内研究
(In Vivo) | BRD3308 (5 mg/kg; intraperitoneal injection; every second day; male Zucker Diabetic Fatty rats) treatment reduces hyperglycaemia and increases insulin secretion in a rat model of type 2 diabetes. At the end of the hyperglycaemic clamp, circulating insulin levels are significantly higher in BRD3308-treated rats. Pancreatic insulin staining and contents are also significantly higher. BRD3308 preserves the functional β-cell mass against glucolipotoxicity in vivo[2].
| Animal Model: | Male Zucker Diabetic Fatty (Obese) rats (6-week-old)[2] | | Dosage: | 5 mg/kg | | Administration: | Intraperitoneal injection; every second day | | Result: | Reduced hyperglycaemia and increased insulin secretion in a rat model of type 2 diabetes. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(870.20 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.4808 mL | 17.4040 mL | 34.8080 mL | | 5 mM | 0.6962 mL | 3.4808 mL | 6.9616 mL | | 10 mM | 0.3481 mL | 1.7404 mL | 3.4808 mL |
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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。 In Vivo: 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；
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