| 货号 | 13574-25mg |
| 描述 | The aldo-keto reductase (AKR) enzymes constitute a family of related NADPH-dependent oxidoreductases. The 1C subfamily (AKR1C) includes four human hydroxysteroid dehydrogenases, with AKR1C1 being a 20α-HSD and the other three being 3α-HSDs. AKR1C1 metabolizes progesterone to an inactive progestin, 20α-hydroxy progesterone.1 In addition, AKR1C1 actions have been implicated in cancer and in the processing of neuroactive steroids involved in brain function.2,3,4,5 3-bromo-5-phenyl Salicylic acid selectively inhibits AKR1C1 (Ki = 4 nM) over AKR1C2 (Ki = 87 nM), AKR1C3 (Ki = 4.2 μM), and AKR1C4 (Ki = 18.2 μM).6 Moreover, it potently inhibits the metabolism of progesterone by bovine aortic endothelial cells overexpressing AKR1C1 (IC50 = 460 nM).6 |
| 别名 | NSC 109116; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Zhang, Y.,Dufort, I.,Rheault, P., et al. Characterization of a human 20α-hydroxysteroid dehydrogenase. Journal of Molecular Endocrinology 25, 221-228 (2000). 2.Lewis, M.J.,Wiebe, J.P. and Heathcote, J.G. Expression of progesterone metabolizing enzyme genes (AKR1C1, AKR1C2, AKR1C3, SRD5A1, SRD5A2) is altered in human breast carcinoma. BMC Cancer 4(27), (2004). 3.Wang, H.W.,Lin, C.P.,Chiu, J.H., et al. Reversal of inflammation-associated dihydrodiol dehydrogenases (AKR1C1 and AKR1C2) overexpression and drug resistance in nonsmall cell lung cancer cells by wogonin and chrysin. International Journal of Cancer 120, 2019-2027 (2007). 4.Belelli, D.,Herd, M.B.,Mitchell, E.A., et al. Neuroactive steroids and inhibitory neurotransmission: Mechanisms of action and physiological relevance. Neuroscience 138, 821-829 (2006). 5.Usami, N.,Yamamoto, T.,Shintani, S., et al. Substrate specificity of human 3(20)α-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. Biological and Pharmaceutical Bullentin 25(4), 441-445 (2002). 6.El-Kabbani, O.,Scammells, P.J.,Gosling, J., et al. Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20α-hydroxysteroid dehydrogenase (AKR1C1). Journal of Medicinal Chemistry 52, 3259-3264 (2009). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 293.1 |
| 分子式 | C13H9BrO3 |
| CAS号 | 4906-68-7 |
| 稳定性 | ≥ 2 years |
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