BSJ-4-116
BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly (adenylation) . BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly (ADP-ribose) polymerase inhibitor Olaparib (HY-10162) [1].
Product Specifications
CAS Number
[2519823-34-6]
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
CDK; PROTACs
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; PROTAC
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/bsj-4-116.html
Purity
99.87
Solubility
DMSO : 100 mg/mL (ultrasonic)
Smiles
O=C1C2=C(OCC(NCCCCCCCN3C[C@@H](CCC3)NC4=NC=C(Cl)C(NC5=C(C=CC=C5)S(C(C)C)(=O)=O)=N4)=O)C=CC=C2C(N1C6C(NC(CC6)=O)=O)=O
Molecular Formula
C40H49ClN8O8S
Molecular Weight
837.38
Precautions
H302, H315, H319, H335
References & Citations
[1]Jiang B, et al. Discovery and resistance mechanism of a selective CDK12 degrader. Nat Chem Biol. 2021;17 (6) :675-683.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
CDK12; Cereblon
Available Sizes
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