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Chemical Structure| 2519823-34-6 Chemical Structure| 2519823-34-6

Structure of BSJ-4-116
CAS No.: 2519823-34-6

Chemical Structure| 2519823-34-6

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BSJ-4-116 is a CDK12-specific degrader with IC50 value of 6nM. Degradation of CDK12 by BSJ-4-116 resulted in premature cleavage and poly(adenylation) of DDR genes.

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Product Details of BSJ-4-116

CAS No. :2519823-34-6
Formula : C40H49ClN8O8S
M.W : 837.38
SMILES Code : O=C(NCCCCCCCN1C[C@H](NC2=NC=C(Cl)C(NC3=CC=CC=C3S(=O)(C(C)C)=O)=N2)CCC1)COC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O
MDL No. :MFCD34186973
InChI Key :YJOJMGTVKMABKQ-FIQOPJFZSA-N
Pubchem ID :155235839

Safety of BSJ-4-116

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P280-P301+P312-P302+P352-P305+P351+P338

Related Pathways of BSJ-4-116

Hedgehog

Isoform Comparison

Biological Activity

Description
BSJ-4-116 is a PROTAC comprising ligands for Cereblon and CDK. It serves as a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes by inducing premature termination of transcription, primarily through increased poly(adenylation). It demonstrates robust antiproliferative effects, both alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib[1].

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.19mL

0.24mL

0.12mL

5.97mL

1.19mL

0.60mL

11.94mL

2.39mL

1.19mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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