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AB287070

CCT-251921

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MW 410.9 Da, Purity >98%. CCT-251921 is a potent, selective, small-molecule modulator of the mediator complex-associated kinases CDK8 and CDK19 (IC₅₀, CDK8 = 2.3 nM; CDK19 = 2.6 nM).

View Alternative Names

CDC2-related protein kinase 6, CDK11, CDK19_HUMAN, CDK8 like cyclin dependent kinase, CDK8 protein kinase, CDK8_HUMAN, Cell Division Kinase 8, Cell division cycle 2 like 6 (CDK8 like), Cell division cycle 2-like protein kinase 6, Cell division protein kinase 19, Cell division protein kinase 8, Cyclin dependent kinase (CDC2 like) 11, Cyclin dependent kinase 19 variant 2, Cyclin-dependent kinase 11, Cyclin-dependent kinase 19, Cyclin-dependent kinase 8, Death-preventing kinase, K35, KIAA1028, Mediator complex subunit cdk8, Mediator of RNA polymerase II transcription subunit cdk8, Protein kinase K35, bA346C16.3

Key facts

CAS number

1607837-31-9

Purity

>98%

Form

Solid

form

Molecular weight

410.9 Da

Molecular formula

C<sub>2</sub><sub>1</sub>H<sub>2</sub><sub>3</sub>ClN<sub>6</sub>O

PubChem

74222277

Nature

Synthetic

Solubility

>25 mg/ml in DMSO

Biochemical name

8-[2-Azanyl-3-Chloranyl-5-(1-Methylindazol-5-Yl)pyridin-4-Yl]-2,8-Diazaspiro[4.5]decan-1-One

Biological description

CCT-251921 is a potent, selective, small-molecule modulator of the mediator complex-associated kinases CDK8 and CDK19 (IC₅₀, CDK8 = 2.3 nM; CDK19 = 2.6 nM).

Canonical smiles

CN1C2=C(C=C(C=C2)C3=CN=C(C(=C3N4CCC5(CCNC5=O)CC4)Cl)N)C=N1

InChi

InChI=1S/C21H23ClN6O/c1-27-16-3-2-13(10-14(16)11-26-27)15-12-25-19(23)17(22)18(15)28-8-5-21(6-9-28)4-7-24-20(21)29/h2-3,10-12H,4-9H2,1H3,(H2,23,25)(H,24,29)

InChiKey

VPJXPDLMACOGIZ-UHFFFAOYSA-N

IUPAC Name

8-[2-amino-3-chloro-5-(1-methylindazol-5-yl)pyridin-4-yl]-2,8-diazaspiro[4.5]decan-1-one

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Product details

This product is manufactured by BioVision, an Abcam company and was previously called B2502 CCT-251921. B2502-1 is the same size as the 1 mg size of ab287070.
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Properties and storage information

Shipped at conditions
Blue Ice
Appropriate short-term storage conditions
-20°C
Appropriate long-term storage conditions
-20°C
Storage information
Store in the dark
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Cdk8 also known as Cyclin-dependent kinase 8 or CDC2L6 is a member of the cyclin-dependent kinase family. It has a molecular mass of approximately 50 kDa. Cdk8 primarily functions as a kinase regulating various stages of transcription by phosphorylating components of the transcriptional machinery. It is ubiquitously expressed in multiple tissues indicating its broad range of functions within the cellular environment.
Biological function summary

The activity of Cdk8 integrates into critical processes involving cellular growth and gene expression. Cdk8 forms a part of the Mediator complex alongside cyclin C MED12 and MED13 regulating transcriptional initiation. This kinase plays a role in the modulation of RNA polymerase II activity with its regulation affecting diverse gene expression patterns within the cell.

Pathways

Cdk8 participates significantly in Wnt/β-catenin and MAPK signaling pathways. Its involvement in the Wnt pathway affects cellular proliferation and differentiation with implications for development and tumorigenesis. Related proteins within these pathways include β-catenin and MAPK which interact closely with the regulatory functions governed by Cdk8 to ensure proper signaling transduction.

Cdk8 has strong associations with cancer and developmental disorders. Dysregulation of Cdk8 activity is often observed in colorectal cancer making it a potential target for cancer therapy. In developmental disorders Cdk8's interaction with proteins in the Mediator complex links it to congenital malformations. This highlights its importance in both tumorigenesis and normal developmental processes.
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Product protocols

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