Bromosporine 是一种有效的BET抑制剂，对 PCAF 的IC50为 2.1 μM。Bromosporine 能阻滞癌细胞的细胞周期，诱导细胞凋亡 (apoptosis)。Bromosporine 与 5-FU (HY-90006) 联合使用时，在移植瘤小鼠模型中表现出良好的抗肿瘤活性。在HIV-1潜伏期模型中，Bromosporine 可增加CDK9T-loop 磷酸化，从而保护 HIV-1 复制免受潜伏期的影响。Bromosporine 可用于大肠癌、急性髓系白血病 (AML) 和艾滋病 (AIDS) 的研究。
| 生物活性 | Bromosporine is a potentBETinhibitor with anIC50value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induceapoptosisincancercells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with5-FU(HY-90006). Bromosporine can increaseCDK9T-loop phosphorylation inHIV-1latency models, resulting the protection of reactivateHIV-1replication from latency. Bromosporine can be used to research colorectalcancer, acute myeloid leukemia (AML) and AIDS[1][2][3][4]. |
| IC50& Target | IC50: 2.1 μM (PCAF)[2]
Apoptosis, BET, CDK9, HIV-1[1][3][4] |
体外研究
(In Vitro) | Bromosporine (0-1000 nM; 72 h) synergistically inhibits cell growth in CRC cells with5-FU(HY-90006)[1].
Bromosporine (various concentration; 48 h) causes a distinct increase in the cells arrested at G1 phase when combined with5-FU[1].
Bromosporine (various concentration; 48 h) decreases the expressions of PARP, caspase 3, and 9[1].
Bromosporine (0.1, 0.5 and 1 μM; 6-10 days) inhibits AML cells in a dose-dependent manner[3].
Bromosporine (2.5 μM; 72 h) activates HIV-1 replication in vitro in latent HIV-1 J-Lat clone C11 cells[4].
Bromosporine (1-50 μM; 48 h) does not induce marked toxicity in primary CD4+ T cells[4].
Cell Proliferation Assay[1] | Cell Line: | HCT116 and HT29 | | Concentration: | 0, 30, 60, 120, 240, 480 and 1000 nM | | Incubation Time: | 72 h | | Result: | Synergistically inhibited cell growth in CRC cells with5-FU(HY-90006) (0-16 μg/mL) and exhibited a dose-dependent manner. |
Cell Cycle Analysis[1] | Cell Line: | HCT116 and HT29 | | Concentration: | Various concentration | | Incubation Time: | 48 h | | Result: | Caused a distinct increase in the cells arrested at G1 phase when combined with5-FU(HY-90006). |
Western Blot Analysis[1] | Cell Line: | HCT116 and HT29 | | Concentration: | Various concentration | | Incubation Time: | 48 h | | Result: | Elevated the level of apoptosis in both cell lines through cleavage of PARP, caspase 3, and 9. |
Cell Proliferation Assay[3] | Cell Line: | MV4;11, KASUMI-1, OCI-AML3 and K562 | | Concentration: | 0.1, 0.5 and 1 μM | | Incubation Time: | 6-10 days | | Result: | Inhibited these AML cells in a dose-dependent manner. |
Cell Cytotoxicity Assay[4] | Cell Line: | PBMCs | | Concentration: | 1 μM, 2.5 μM, 5 μM, 10 μM, 25 μM and 50 μM | | Incubation Time: | 48 h | | Result: | Did not induce marked toxicity in primary CD4+ T cells with CC50over 10 μM. |
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体内研究
(In Vivo) | Bromosporine (100 mg/kg; i.p.; daily for 10 days) shows better antitumor activity than individual when co-treated with5-FU(HY-90006)[1].
| Animal Model: | Female BALB/c nude mice (5-6 weeks; injected with 1 × 106 cells/100 μL of HT116 cells)[1] | | Dosage: | 100 mg/kg | | Administration: | i.p.; daily for 10 days | | Result: | Exhibited better antitumor activity than individual Bromosporine or5-FU(HY-90006) when co-treated with the two agent. |
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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 : ≥ 51.7 mg/mL(127.83 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.4726 mL | 12.3628 mL | 24.7255 mL | | 5 mM | 0.4945 mL | 2.4726 mL | 4.9451 mL | | 10 mM | 0.2473 mL | 1.2363 mL | 2.4726 mL |
*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。 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；
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%corn oil Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.18 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。
*以上所有助溶剂都可在本网站选购。 |
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