| Bioactivity | AKR1C1-IN-1 is a potent and selective inhibitor of human 20α-hydroxysteroid dehydrogenase (AKR1C1), with a Ki value of 4 nM for AKR1C1[1]. | |||||||||
| Target | Ki: 4 nM (AKR1C1), 87 nM (AKR1C2), 4.2 μM (AKR1C3), 18.2 μM (AKR1C4) | |||||||||
| Invitro | AKR1C1-IN-1 potently inhibits the metabolism of progesterone in AKR1C1-overexpressed BAECs, and with an IC50 of 460 nM[1]. | |||||||||
| Name | AKR1C1-IN-1 | |||||||||
| CAS | 4906-68-7 | |||||||||
| Formula | C13H9BrO3 | |||||||||
| Molar Mass | 293.11 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [1]. El-Kabbani O, et al. Structure-guided design, synthesis, and evaluation of salicylic acid-based inhibitors targeting a selectivity pocket in the active site of human 20alpha-hydroxysteroid dehydrogenase (AKR1C1). J Med Chem. 2009 May 28;52(10):3259-64. |