BMS453 (BMS-189453) 是一种合成类维生素 A，是一种RARβ激动剂和RARα/RARγ拮抗剂。BMS453 主要通过诱导活性 TGFβ 来抑制乳腺细胞生长。
| 生物活性 | BMS453 (BMS-189453), a synthetic retinoid, is aRARβagonist and aRARα/RARγantagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ[1][2]. |
体外研究
(In Vitro) | BMS453 (1 μM; 11 hours; 184 and HMEC cells) treatment inhibits the proliferation of normal breast cell growth without significantly inducing apoptosis[2].
BMS453 (1 μM; 5 days; 184 and HMEC cells) treatment inhibits normal breast cell proliferation by causing G1 arrest[2].
BMS453 (1 μM; 24-72 hours; 184 cells) treatment induces Rb hypophosphorylation and decrease CDK2 kinase activity. BMS453 increases total p21 protein levels and CDK2-bound p21 protein, but does not change CDK4-bound p21[2].
BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ[2].
Cell Proliferation Assay[2] | Cell Line: | Normal human mammary epithelial cells (184 and HMEC) | | Concentration: | 1 μM | | Incubation Time: | 11 hours | | Result: | Inhibited3H-thymidine uptake in normal breast cells (184 and HMEC) by 40 %. |
Cell Cycle Analysis[2] | Cell Line: | Normal human mammary epithelial cells (184 and HMEC) | | Concentration: | 1 μM | | Incubation Time: | 5 days | | Result: | Increased the proportion of cells in G0/G1 phase and decreased the proportion of cells in S phase. |
Western Blot Analysis[2] | Cell Line: | 184 cells | | Concentration: | 1 μM | | Incubation Time: | 24 hours, 48 hours, 72 hours | | Result: | Induced Rb hypophosphorylation and decrease CDK2 kinase activity. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | -20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| 溶解性数据 | In Vitro: DMSO : 16.67 mg/mL(43.81 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.6283 mL | 13.1413 mL | 26.2826 mL | | 5 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL | | 10 mM | 0.2628 mL | 1.3141 mL | 2.6283 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 (stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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