CDK8-IN-11 是一种有效的、选择性的CDK8抑制剂，IC50值为 46 nM。CDK8-IN-11 可抑制 WNT/β-catenin 信号通路。CDK8-IN-11 可用于结肠癌的研究。
| 生物活性 | CDK8-IN-11 is a potent and selectiveCDK8inhibitor with anIC50value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of coloncancer[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | CDK8-IN-11 (compound 29, 200 nM) shows inhibitory effects against CDK8 by 73.6%[1].
CDK8-IN-11 (0-50 μM, 48 h) inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells[1].
CDK8-IN-11 (0-4 μM, 48 h) inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM, 24 h) suppresses canonical WNT/β-catenin signaling pathways and deregulates β-catenin-mediated transcription in HCT-116 cells[1].
CDK8-IN-11 (0.5-2 μM, 48 h) increases the number of cells in the G1 phase in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM) reversesSorafenib(HY-10201) resistance of HCT-116 cells[1].
Cell Proliferation Assay[1] | Cell Line: | HCT-116, HHT-29, SW480, CT-26, GES-1 cells | | Concentration: | 0.08, 0.4, 2, 10, and 50 μM | | Incubation Time: | 48 h | | Result: | Inhibited cell proliferation with IC50values of 1.2, 0.7, 2.4, 5.5, 62.7 nM respectively. |
Western Blot Analysis[1] | Cell Line: | HCT-116 cell | | Concentration: | 0, 1, 2, 4 μM | | Incubation Time: | 48 h | | Result: | Inhibited the phosphorylation of STAT1 at Ser727 without affecting the JAK-regulated phosphorylation at Tyr701. |
Cell Cycle Analysis[1] | Cell Line: | HCT-116 cell | | Concentration: | 0.5-2 μM | | Incubation Time: | 48 h | | Result: | Increased the number of cells in the G1 phase with an obvious decreased percentage of cells in the G2/M and S phase in HCT-116 cells. |
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体内研究
(In Vivo) | CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice[1].
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days[1].
CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10–6cm/s[1].
| Animal Model: | CT-26 xenograft mice[1] | | Dosage: | 10 and 40 mg/kg | | Administration: | Oral adminstration (p.o.) | | Result: | Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor. |
| Animal Model: | Rats (pharmacokinetic assay)[1] | | Dosage: | 10 mg/kg (p.o.), 2 mg/kg (i.v.) | | Administration: | Oral adminstration (p.o.) or intravenous injection (i.v.) | | Result: | Pharmacokinetic profile of CDK8-IN-11 (compound 29).
| dose (mg/kg) | T1/2(h) | Tmax(h) | Cmax(ng/mL) | F (%) | |
| 10 (p.o.) | 1.1 | 0.8 | 453 | 31.7 | |
| 2 (i.v.) | 0.5 | | 318 | |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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