CYP1B1-IN-12 

CYP1B1-IN-12 is a selective cytochrome P450 1B1 (CYP1B1) inhibitor with an IC₅₀ of 6.05 nM. CYP1B1-IN-12 demonstrates remarkable selectivity, exceeding 1600-fold and 16,000-fold over CYP1A1 and CYP1A2, respectively. CYP1B1-IN-12 can enhance Paclitaxel (HY-B0015)-mediated apoptosis and restore Paclitaxel sensitivity in A549/Taxol-resistant cells. CYP1B1-IN-12 can inhibit the epithelial-mesenchymal transition process and reduce cells migration and invasion. CYP1B1-IN-12 can be used for the research of cancer, such as non-small cell lung cancer (NSCLC)^[1].

CYP1B1-IN-12 (Compound B14) (10 μM) 对包括 CYP2B6 和 CYP2C8 在内的 7 种主要 CYP 酶的抑制率低于 50%，表明其药物相互作用潜力较低^[1]。
Compound B14 (0-20 μM, 48 h) 在 HUVEC 和 BEAS-2B 细胞中的 IC₅₀ 值大于 20 μM^[1]。
CYP1B1-IN-12 (2-8 μM, 48 h) 与 Paclitaxel (HY-B0015) 联合使用时，可剂量依赖性地抑制 A549/Tax 细胞的增殖^[1]。
CYP1B1-IN-12 (2-8 μM, 14 days) 与 Paclitaxel 联合使用时，可减少 A549/Tax 细胞的集落数量^[1]。
CYP1B1-IN-12 (8 μM, 48 h) 与 Paclitaxel 联合使用时，可增加 A549/Tax 细胞中总凋亡细胞的比例^[1]。
CYP1B1-IN-12 (1-4 μM, 24 h) 可抑制 A549/Tax 细胞的迁移和侵袭^[1]。
CYP1B1-IN-12 (1-4 μM, 48 h) 可上调 A549/Tax 细胞中 E-钙粘蛋白的水平，并下调 N-钙粘蛋白和波形蛋白的水平^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

431.25

C₁₇H₁₀IN₃OS

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Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Li C, et al. Discovery of novel selective CYP1B1 inhibitors: Design, synthesis and biological evaluation. Bioorg Chem. 2025 Sep;164:108838.  [Content Brief]