BSJ-4-116

SKU: orb1298355

Description

BSJ-4-116 is a potent and selective CDK12-targeting PROTAC degrader with 6 nM IC50. It disrupts DNA damage response gene transcription via premature termination and increased polyadenylation, applicable for oncology research in both cellular and animal models to study transcription-dependent vulnerabilities.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2519823-34-6
• MW: 837.38
• Purity: 99.09% (May vary between batches)
• Formula: C₄₀H₄₉ClN₈O₈S
• SMILES: O=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
• Target: CDK,PROTACs
• Solubility: DMSO:250 mg/mL (298.55 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (5.97 mM)

Bioactivity

• Target 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Cereblon, CDK12, CDK, degrader, Cyclin dependent kinase, C1039F, cancer, BSJ4116, BSJ-4-116, BSJ 4 116, antiproliferative, Kelly, mutation, inhibit, Inhibitor, PROTACs

Compound Identifiers

PubChem CID

155235839