CDK8-IN-11 hydrochloride 是一种有效的、选择性的
CDK8抑制剂，
IC50值为 46 nM。CDK8-IN-11 hydrochloride 可抑制 WNT/β-catenin 信号通路。CDK8-IN-11 hydrochloride 可用于结肠癌的研究。
| 生物活性 |
CDK8-IN-11 hydrochloride is a potent and selectiveCDK8inhibitor with anIC50value of 46 nM. CDK8-IN-11 hydrochloride inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 hydrochloride can be used in the research of coloncancer[1].
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体外研究
(In Vitro) |
CDK8-IN-11 (compound 29, 200 nM) hydrochloride shows inhibitory effects against CDK8 by 73.6%[1].
CDK8-IN-11 (0-50 μM, 48 h) hydrochloride inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells[1].
CDK8-IN-11 (0-4 μM, 48 h) hydrochloride inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM, 24 h) hydrochloride 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) hydrochloride increases the number of cells in the G1 phase in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM) hydrochloride 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.) hydrochloride inhibits tumor growth in CT-26 xenograft mice[1].
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) hydrochloride shows no obvious abnormal behavior within 7 days[1].
CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) hydrochloride 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: |
Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor. |
| 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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| 分子量 |
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| Formula |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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