BSJ-03-123

SKU: orb1301826

Description

BSJ-03-123 is a selective small-molecule degrader targeting CDK6. It is a valuable chemical probe for studying CDK6-dependent mechanisms in cancer research and has demonstrated utility in both cellular and in vivo models of hematological malignancies.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2361493-16-3
• MW: 937.01
• Purity: 99.38% (May vary between batches)
• Formula: C₄₇H₅₆N₁₀O₁₁
• SMILES: O=C1N(C=2C(C(C)=C1C(C)=O)=CN=C(NC3=CC=C(C=N3)N4CCN(CCOCCOCCOCCNC(COC5=C6C(C(=O)N(C6=O)C7C(=O)NC(=O)CC7)=CC=C5)=O)CC4)N2)C8CCCC8
• Target: PROTACs,CDK
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (4.27 mM);H2O:Insoluble;DMSO:115 mg/mL (122.73 mM)

Bioactivity

• In Vitro:
  BSJ-03-123 induced rapid, dose-dependent ternary complex formation with CDK6 and CRBN, but not with CDK4 and CRBN. Ternary complex formation was prevented by blocking binding sites on CDK6 or CRBN via pretreatment with palbo or lenalidomide.
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• Cell Research:
  4x10^6 MV4-11 CRBN-/- cells were treated for 3 h with 20 μM palbociclib, BSJ-03-123 or vehicle. 1x10^6 cells were spun down at 500 x g for 5 min, and the supernatant removed. Pellets were incubated at 46, 49, 52 or 55°C for 3 min followed by 3 min incubation at room temperature. 30 μl of lysis buffer (20 mM Tris-HCl pH 8.0, 120 mM NaCl, 0.5% NP-40, protease inhibitors) were added and cells lysed by 3 rounds of snap freezing and thawing. Denatured proteins were removed by 20 min centrifugation at 14.000 x g at 4°C and supernatants analyzed by Western Blotting.
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Storage & Handling

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

Alternative Names

BSJ03123, BSJ-03-123, BSJ 03 123, CDK6, CDK, Cyclin dependent kinase, inhibit, Inhibitor, PROTACs

Compound Identifiers

PubChem CID

137628658