| Bioactivity | AKR1C3-IN-9 is a selective inhibitor of Aldo-keto Reductase 1C3 (AKR1C3) with an IC50 value of 8.92 nM. AKR1C3-IN-9 significantly reverses the Doxorubicin (HY-15142A) (DOX) resistance in a resistant breast cancer cell line[1]. | |||||||||
| Target | IC50: 8.92 nM (AKR1C3) | |||||||||
| Invitro | AKR1C3-IN-9 (compound 24) (10-100 μM; 72 h and 96 h) 对 3 种乳腺癌细胞系 (MDA-MB-231、MCF-7) 均有较弱的抗增殖作用，抑制范围为 100 μM[1]。AKR1C3-IN-9 (10 μM, 25 μM, 50 μM; 72 h) 与 10-50 μM DOX 协同抑制 MCF-7 细胞增殖[1]。AKR1C3-IN-9 (10 μM; 8 d) 与 50 μM DOX 协同抑制 MCF-7/DOX 细胞系的增殖、克隆生存，从而恢复对 DOX 的敏感性[1]。 | |||||||||
| Name | AKR1C3-IN-9 | |||||||||
| Formula | C20H20N2O4 | |||||||||
| Molar Mass | 352.38 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
|
|||||||||
| Reference | [1]. Liu Y, et al. Development of highly potent and specific AKR1C3 inhibitors to restore the chemosensitivity of drug-resistant breast cancer. Eur J Med Chem. 2022 Dec 13;247:115013. |