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JH-XI-10-02

Cat. No. 7304 Submit a Review Datasheet / COA / SDS
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Description: CDK8 Degrader (PROTAC®)
Chemical Name: 15-[[2-(2,6-Dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]-N-[(3β,5α,17β)-17-(7-isoquinolinyl)androstan-3-yl]-N-methyl-4,7,10,13-tetraoxapentadecanamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for JH-XI-10-02

JH-XI-10-02 is a CDK8 Degrader (PROTAC®) comprising the cereblon binding ligand Pomalidomide (Cat. No. 6302) joined by a linker to a CDK8 inhibitor. JH-XI-10-02 (1 μM) induces significant proteasome-dependent degradation of CDK8 in Jurkat cells after 24 h, with no significant effect on CDK19 levels.

CDK8 antibody validated for Western Blot also available: Catalog # NBP2-92972.

Licensing Information

Sold under license from Dana-Farber Cancer Institute.

Technical Data for JH-XI-10-02

M. Wt 920.16
Formula C53H69N5O9
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2209085-22-1
PubChem ID 145708490
InChI Key JECHBTRAPARMGI-GFTKVEOVSA-N
Smiles [H][C@@]12CC[C@@H]([C@]1(CC[C@]3([C@]2(CC[C@]4(C[C@@H](N(C(CCOCCOCCOCCOCCNC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O)C)CC[C@]34C)[H])[H])[H])C)C8=CC9=C(C=C8)C=CN=C9

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for JH-XI-10-02

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.01 50

Preparing Stock Solutions for JH-XI-10-02

The following data is based on the product molecular weight 920.16. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 2.17 mL 10.87 mL 21.74 mL
2.5 mM 0.43 mL 2.17 mL 4.35 mL
5 mM 0.22 mL 1.09 mL 2.17 mL
25 mM 0.04 mL 0.22 mL 0.43 mL

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References for JH-XI-10-02

References are publications that support the biological activity of the product.

Hatcher et al (2018) Development of highly potent and selective steroidal inhibitors and degraders of CDK8. ACS Med.Chem.Lett. 9 540 PMID: 29937979

If you know of a relevant reference for JH-XI-10-02, please let us know.

View Related Products by Target

Keywords: JH-XI-10-02, JH-XI-10-02 supplier, CDK8, degraders, protacs, cyclin-dependent, kinases, targeted, protein, degradation, TPD, degrades, Transcriptional, CDKs, Cyclin, Dependent, Kinase, (CDK), Degraders, 7304, Tocris Bioscience

Citations for JH-XI-10-02

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Literature in this Area

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia