CDK8-IN-15

CAS: 2988020-03-5 F: C19H20N4O3 W: 352.39

CDK8-IN-15 (Compound 46) is a potent CDK8 inhibitors with an IC50 value of 57 nM. It can enhance the thermal stability o

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Bioactivity	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].
Invitro	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. 0 --> CDK8-IN-15 相关抗体: Cell Viability Assay[1] Cell Line:
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:
CAS	2988020-03-5
Formula	C19H20N4O3
Molar Mass	352.39
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Yan YY, et al.The discovery of a novel pyrrolo[2,3-b]pyridine as a selective CDK8 inhibitor offers a new approach against psoriasis[J]. 2024 May 6;175, 0753-3322.

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