BSJ-4-116

For research use only.

Catalog No.S9859

BSJ-4-116 Chemical Structure

CAS No. 2519823-34-6

BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.

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Biological Activity

Description BSJ-4-116 is a specific degrader of cyclin-dependent kinase 12 (CDK12). BSJ-4-116 exhibits potent antiproliferative effects.
Targets
CDK12 [1]
()
In vitro

BSJ-4-116 selectively degrads CDK12 as assessed through quantitative proteomics. BSJ-4-116 downregulates the expression of DDR genes and exhibits antiproliferative activity in cancer cells. BSJ-4-116 also substantially suppresses the phosphorylation of Pol II Ser2 and Thr4.[1]

Protocol

Cell Research:

[1]

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  • Cell lines: Jurkat cells
  • Concentrations: 50 nM
  • Incubation Time: 8 h
  • Method:

    For poly(A) 3'-end sequencing, Jurkat cells are exposed to DMSO or THZ531 (250 nM) or to BSJ-4-116 or BSJ-4-116-NC (50 nM) for 8 h. RNA extraction is performed with TRIzol following the manufacturer's instructions. Total RNA is treated with DNase I. Sequencing libraries are prepared with the RNA-sequencing library kit following the manufacturer's instructions. All samples are sequenced on a HiSeq 2500 sequencer.


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (119.42 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 837.38
Formula

C40H49ClN8O8S

CAS No. 2519823-34-6
Storage powder
in solvent
Synonyms N/A

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CDK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID