BSJ-4-116

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

BSJ-4-116 Chemical Structure

BSJ-4-116 Chemical Structure

CAS: 2519823-34-6

Purity & Quality Control

Batch: S985901 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.93%
99.93

BSJ-4-116 Related Products

Signaling Pathway

Choose Selective CDK Inhibitors

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
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]

Cell Research 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.

Chemical Information & Solubility

Molecular Weight 837.38 Formula

C40H49ClN8O8S

CAS No. 2519823-34-6 SDF --
Smiles CC(C)[S](=O)(=O)C1=C(NC2=NC(=NC=C2Cl)NC3CCCN(CCCCCCCNC(=O)COC4=C5C(=O)N(C6CCC(=O)NC6=O)C(=O)C5=CC=C4)C3)C=CC=C1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (119.42 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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