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BSJ-4-116

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Catalog No. T9117Cas No. 2519823-34-6

BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation).

BSJ-4-116

BSJ-4-116

🥰Excellent
Purity: 99.09%
Catalog No. T9117Cas No. 2519823-34-6
BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation).
Pack SizePriceAvailabilityQuantity
1 mg$50In Stock
5 mg$113In Stock
10 mg$189In Stock
25 mg$396In Stock
50 mg$637In Stock
100 mg$953In Stock
1 mL x 10 mM (in DMSO)$173In Stock
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Purity:99.09%
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Product Introduction

Bioactivity
Description
BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. It downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation).
Targets&IC50
CDK12:6 nM
In vitro
BSJ-4-116 (50?nM; 6-24?hours) decreases the level of CDK12 protein, regardless of the mutational status of the cell line.BSJ-4-116 (10-10000 nM; 72 hours) exhibits potent antiproliferative effects in Kelly CDK12C1039F.BSJ-4-116 inhibits the growth of T-ALL cells (Jurkat and MOLT-4 cells) and sensitizes them to PARP inhibition. BSJ-4-116 regulates DDR genes via poly(adenylation). BSJ-4-116 overcomes CDK12C1039F mutation. BSJ-4-116 represents the first example of resistance to a bivalent degrader molecule that is a consequence of an acquired point mutation in the target protein.
Chemical Properties
Molecular Weight837.38
FormulaC40H49ClN8O8S
Cas No.2519823-34-6
SmilesO=C1C=2C(C(=O)N1C3C(=O)NC(=O)CC3)=CC=CC2OCC(NCCCCCCCN4C[C@H](NC=5N=C(NC6=C(S(C(C)C)(=O)=O)C=CC=C6)C(Cl)=CN5)CCC4)=O
Relative Density.1.368 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 250 mg/mL (298.55 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.1942 mL5.9710 mL11.9420 mL59.7100 mL
5 mM0.2388 mL1.1942 mL2.3884 mL11.9420 mL
10 mM0.1194 mL0.5971 mL1.1942 mL5.9710 mL
20 mM0.0597 mL0.2986 mL0.5971 mL2.9855 mL
50 mM0.0239 mL0.1194 mL0.2388 mL1.1942 mL
100 mM0.0119 mL0.0597 mL0.1194 mL0.5971 mL

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