2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK8-IN-9

CDK8-IN-9 (compound 22) 是一种有效的 II 型 CDK8 抑制剂, 其IC50 值为 48.6 nM。CDK8-IN-9 可以抑制肿瘤生长，用于结直肠癌研究。

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CDK8-IN-9

CDK8-IN-9 Chemical Structure

CAS No. : 2850253-95-9

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CDK8-IN-9 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK8-IN-9 (compound 22) is a potent type II CDK8 inhibitor with an IC50 value of 48.6 nM. CDK8-IN-9 can inhibit tumor growth and is used in colorectal cancer studies[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CT26 GI50
4 μM
Compound: 22
Antiproliferative activity against mouse CT26 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against mouse CT26 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
[PMID: 36068975]
GES1 GI50
61.5 μM
Compound: 22
Cytotoxicity against human GES1 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Cytotoxicity against human GES1 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
[PMID: 36068975]
HCT-116 GI50
4.9 μM
Compound: 22
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
[PMID: 36068975]
HT-29 GI50
4.3 μM
Compound: 22
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
[PMID: 36068975]
SW480 GI50
2.1 μM
Compound: 22
Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
Antiproliferative activity against human SW480 cells assessed as cell growth inhibition measured after 48 hrs by MTT assay
[PMID: 36068975]
体外研究
(In Vitro)

CDK8-IN-9 (compound 22) (0-100 μM, 48 h) can significantly inhibit cell proliferation and target CDK8 to inhibit the activation of the WNT/β-catenin pathway, thereby suppressing β-catenin-mediated transcriptional activity of TCF/ LEF[1].
CDK8-IN-9 (compound 22) (0.5,1 and 2 μM, 24 h) induces G2/M and S-phase cell cycle arrest, thereby inhibiting cell proliferation rather than inducing apoptosis[1].

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

CDK8-IN-9 相关抗体:

Cell Viability Assay[1]

Cell Line: HCT-116, HT-29, SW-480, CT-26 and GES-1 cells
Concentration: 0-100 μM
Incubation Time: 48 hours
Result: Inhibited HCT-116, HT-29, SW-480, CT-26 and GES-1 cells with the GI50 values of 4.9, 4.3, 2.1, 4.0 and 61.5 μM, respectively.

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 1, and 2 μM
Incubation Time: 24 hours
Result: Arrested cells in G2/M phase by 17%, 20.26% and 34.45% at concentrations of 0.5, 1, and 2 μM, respectively.
Showed a decrease in the G0/G1 phase and a slight increase in the S phase.
体内研究
(In Vivo)

CDK8-IN-9 (compound 22) (p.o., 20, 40 and 80 mg/kg, daily, 3 weeks) significantly reduces in tumor volume and inhibits weight loss in mice at the concentration of 80 mg/kg in Balb/c mice infected with CT-26 murine colon cancer cells[1].

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

Animal Model: Sprague−Dawley rats[1]
Dosage: 10 mg/kg or 5 mg/kg
Administration: p.o. for 10 mg/kg and i.v. for 5 mg/kg
Result: The pharmacokinetic parameters of CDK8-IN-9 (compound 22)
Parameters t1/2 (h) Tmax (h) MRT (h) Cmax (μg/L) AUC0-∞ (μg/L·h) CL (L/h/kg) F (%)
10 mg/kg (po) 1.21 0.75 2.022 497.56 783.66 9.23 39.8
5 mg/kg (iv) 1.63 - 1.756 706.29 983.09 11.32 -
分子量

423.43

Formula

C24H20F3N3O
CAS 号
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.
纯度 & 产品资料
参考文献

CDK8-IN-9 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CDK8-IN-92850253-95-9CDKCyclin dependent kinaseCDK8tumorcolorectal cancerInhibitorinhibitorinhibit

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