| Bioactivity | THK01 is a potent ROCK2 inhibitor with IC50 values of 5.7 and 923 nM for ROCK2 and ROCK1, respectively. THK01 inhibits breast cancer metastasis through the ROCK2-STAT3 signaling pathway. THK01 can be used in research of breast cancer[1]. |
| Invitro | THK01 (1.25-10 μM; 48 h) 以剂量依赖的方式抑制 MDA-MB-231 细胞的迁移和侵袭能力[1]。THK01 (5 μM; 24 h; MDA-MB-231 细胞) 通过 STAT 信号通路抑制乳腺癌转移[1]。THK01 (1.25-10 μM; 24 h; MDA-MB-231 细胞) 以剂量依赖性方式下调 STAT3Y705 的磷酸化水平，同时略微上调 STAT3S727 的水平[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | THK01 (15 mg/kg; i.v.; 雌性 BALB/c 裸鼠) 在体内抑制乳腺癌细胞转移[1]。 Animal Model: |
| Name | THK01 |
| CAS | 2226941-26-8 |
| Formula | C20H13N3O2 |
| Molar Mass | 327.34 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Wang J, et, al. Discovery of unglycosylated indolocarbazoles as ROCK2 isoform-selective inhibitors for the treatment of breast cancer metastasis. Eur J Med Chem. 2023 Mar 15;250:115181. |