2. Cell Cycle/DNA Damage
  3. CDK
  4. CDK8-IN-15

CDK8-IN-15 (Compound 46) 是一种强有效的 CDK8 抑制剂，IC50 值为 57 nM。它能增强 CDK8 的热稳定性并同时抑制 NF-κB ，也能选择性抑制 CDK 家族 和 酪氨酸。此外，也能对体外 TNF-α 导致的牛皮癣起积极作用并增强 Foxp3 和 IL-10 的表达来减弱炎症反应，有望用于牛皮癣疾病的研究。

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CDK8-IN-15 Chemical Structure

CDK8-IN-15 Chemical Structure

CAS No. : 2988020-03-5

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CDK8-IN-15 相关抗体

Top Publications Citing Use of Products

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CDK8-IN-15 (Compound 46) is a potent CDK8 inhibitors with an IC50 value of 57 nM. It can enhance the thermal stability of CDK8 along with inhibition against NF-κB and have favourable selectivity across the CDK family and tyrosine kinase. Additionally, it also demostrates a positive effect in vitro psoriasis model induced by TNF-α and alleviats the inflammatory response enhancing the expression of Foxp3 and IL-10, which is promising for research of psoriasis diseases[1].
IC50 & Target[1]

CDK8

57 nM (IC50)

体外研究
(In Vitro)

CDK8-IN-15 抗 CDK8 活性最高，IC50 值为 57.3 nM，并且对 HaCat 细胞模型中 TNF-α -诱导的牛皮癣病有正向作用，IC50 值为 4.6 μM[1]。
CDK8-IN-15 (5 μM, 4 h) 抑制 CDK8 酶活性，并且增强 HEK293T-CDK8 细胞内源性和外源性 CDK8 的热稳定性[1]。
CDK8-IN-15 (0,1,2,4 μM, 75h) 在处理 HEK293 细胞后，显著降低 CXCL1，CXCL2，IL-8 的水平[1]。

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

CDK8-IN-15 相关抗体:

Cell Viability Assay[1]

Cell Line: HaCat cells
Concentration: 0, 1 μM, 2 μM, 4 μM
Incubation Time: 75 h
Result: Down-regulated the levels of IL-8 and IL-6 in a dose-dependent manner with values of 0, 1 μM, 2 μM, 4 μM .

Western Blot Analysis[1]

Cell Line: HEK293T-CDK8 cells
Concentration: 5 μM
Incubation Time: 4 h
Result: Enhanced the thermal stability of endogenous and exogenous CDK8.

Western Blot Analysis[1]

Cell Line: HEK 293 cells
Concentration: 1 μM
Incubation Time: 0, 1, 2, 4, 8, 12 h.
Result: Had a great NF-κB transcriptional activity inhibitory effect with an IC50 value of 1 μM.
体内研究
(In Vivo)

CDK8-IN-15 (2 MG/KG, i.v. and 10 mg/kg, p.o.) 在大鼠中具有 Caco-2 高通透性，对 5 种细胞色素 p450 同工酶无明显抑制作用[1]。
CDK8-IN-15 在ICE鼠中不引起明显的组织损伤 [1]。
CDK8-IN-15 (5/10/20 MG/KG, p.o.) 在IMQ诱导的牛皮癣模型小鼠中可能通过靶向 CDK8 增强 IL-10 的生成和 Foxp3 的表达，从而缓解牛皮癣[1]。

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

Animal Model: Rats[1]
Dosage: 2 mg/kg, iv and 10 mg/kg, po
Administration: iv and po, a single administration
Result: Showed high Caco-2 permeability in rats
Animal Model: Imiquimod-induced psoriasis model of mice[1]
Dosage: 5, 10, 20 mg/kg
Administration: 5 % imiquimod cream and 5, 10, 20 mg/kg daily, p.o.
Result: Alleviated the symptoms of imiquimod-induced psoriasis and increase the productions of TNF-α and IL-6 in imiquimod-induced psoriasis model of mice
Animal Model: ICR mice[1].
Dosage: 1000 mg/kg
Administration: i.g., a single administration
Result: Didn’t cause a significant tissue damage on ICR mice
分子量

352.39

Formula

C19H20N4O3
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-15 相关分类

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  • 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-152988020-03-5CDKCyclin dependent kinaseHaCat cellsTNF-α-induced psoriasis model of miceinflammatory responseICR micethermal stabilitypsoriasis diseasesInhibitorinhibitorinhibit

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