2226941-26-8
2226941-26-8 structure
- Name: THK01
- Chemical Name: THK01
- CAS Number: 2226941-26-8
- Molecular Formula: C20H13N3O2
- Molecular Weight: 327.34
- Catalog: Signaling Pathways Cell Cycle/DNA Damage ROCK
- Create Date: 2023-05-31 13:02:13
- Modify Date: 2024-01-31 08:39:38
-
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].
| Name | THK01 |
|---|
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
ROCK2:5.7 nM (IC50) ROCK1:923 nM (IC50) |
| In Vitro | 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: MDA-MB-231 cells Concentration: 5 μM Incubation Time: 24 hours Result: Down-regulated the phosphorylation levels (p-STAT) of STAT1, STAT2, and STAT3, up-regulated of p-STAT5A and STAT6. Western Blot Analysis[1] Cell Line: MDA-MB-231 cells Concentration: 1.25, 2.5, 5, 10 μM Incubation Time: 24 hours Result: Reduced the level of p-STAT3Y705 and increased the expression of p-STAT3S727 in MDA-MB-231 cells. |
| 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: Female BALB/c nude mice with MDAMB-231-Luc-mcherry xenografts (6 weeks old, weight about 20 g)[1] Dosage: 15 mg/kg Administration: Intravenous injection; once a day for 43 days Result: Reduced the pulmonary metastasis of MDA-MB-231 in vivo with negligible toxicity. |
| References |
| Molecular Formula | C20H13N3O2 |
|---|---|
| Molecular Weight | 327.34 |