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BSJ-4-116

Cat. No. 7528 Submit a Review Datasheet / COA / SDS
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Description: Selective CDK12 PROTAC® Degrader
Chemical Name: N-[7-[(3R)-3-[[5-Chloro-4-[[2-[(1-methylethyl)sulfonyl]phenyl]amino]-2-pyrimidinyl]amino]-1-piperidinyl]heptyl]-2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for BSJ-4-116

BSJ-4-116 is a selective CDK12 PROTAC® Degrader. BSJ-4-116 selectively degrades CDK12 over a panel of other kinases and exhibits no degradation of CDK13 or cyclin K. The compound inhibits growth of T-ALL cells and sensitizes them to PARP inhibitor Olaparib (Cat. No. 7579).

PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.

Licensing Information

Sold under license from Dana-Farber Cancer Institute

Technical Data for BSJ-4-116

M. Wt 837.39
Formula C40H49ClN8O8S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2519823-34-6
PubChem ID 155235839
InChI Key YJOJMGTVKMABKQ-FIQOPJFZSA-N
Smiles CC(S(=O)(C1=C(C=CC=C1)NC2=NC(N[C@@H]3CCCN(C3)CCCCCCCNC(COC4=C5C(N(C(C5=CC=C4)=O)C6CCC(NC6=O)=O)=O)=O)=NC=C2Cl)=O)C

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 BSJ-4-116

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 83.74 100

Preparing Stock Solutions for BSJ-4-116

The following data is based on the product molecular weight 837.39. 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
1 mM 1.19 mL 5.97 mL 11.94 mL
5 mM 0.24 mL 1.19 mL 2.39 mL
10 mM 0.12 mL 0.6 mL 1.19 mL
50 mM 0.02 mL 0.12 mL 0.24 mL

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References for BSJ-4-116

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

Jiang et al (2021) Discovery and resistance mechanism of a selective CDK12 degrader. Nat.Chem.Biol. 17 675 PMID: 33753926

If you know of a relevant reference for BSJ-4-116, please let us know.

View Related Products by Target

Keywords: BSJ-4-116, BSJ-4-116 supplier, Selective, CDK12, Degraders, degrades, TPD, targeted, protein, degradation, PROTACs, Transcriptional, CDKs, Cyclin, Dependent, Kinase, (CDK), 7528, Tocris Bioscience

Citations for BSJ-4-116

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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