1. PROTAC
    Cell Cycle/DNA Damage
  2. PROTAC
    CDK
  3. BSJ-04-132

BSJ-04-132 

目录号: HY-136252
产品使用指南

BSJ-04-132 是一种有效的,选择性的基于 Ribociclib (HY-15777) 的 CDK4 降解剂 (PROTAC),对 CDK4/D1 和 CDK6/D1 的 IC50 分别为 50.6 nM 和 30 nM。BSJ-04-132 不诱导 CDK6 和 IKZF1/3 降解,具有抗癌活性。

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BSJ-04-132 Chemical Structure

BSJ-04-132 Chemical Structure

CAS No. : 2349356-39-2

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Description

BSJ-04-132 is a potent and selective Ribociclib-based CDK4 degrader (PROTAC), with IC50s of 50.6 nM and 30 nM for CDK4/D1 and CDK6/D1, respectively. BSJ-04-132 does not induce CDK6 and IKZF1/3 degradation. BSJ-04-132 has anti-cancer activity[1].

IC50 & Target[1]

CDK4/D1

50.6 nM (IC50)

CDK6/D1

30 nM (IC50)

In Vitro

BSJ-04-132 (0.1-5 μM; for 4 hours) only resultes in degradation of CDK4 in WT cells, not CDK6 and IKZF1/3[1].

Western Blot Analysis[1]

Cell Line: Wildtype (WT) or Crbn-/- Jurkat cells
Concentration: 0.1, 0.5, 1, 5 μM
Incubation Time: For 4 hours
Result: Only resulted in degradation of CDK4 in WT cells, not CDK6 and IKZF1/3.
Molecular Weight

819.91

Formula

C₄₂H₄₉N₁₁O₇

CAS No.

2349356-39-2

SMILES

O=C(C1=CC2=CN=C(NC3=NC=C(N4CCN(CCCCNC(COC5=CC=CC(C(N6C(CC7)C(NC7=O)=O)=O)=C5C6=O)=O)CC4)C=C3)N=C2N1C8CCCC8)N(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 摩尔计算器

  • 稀释计算器

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× = ×
C1   V1   C2   V2

Keywords:

BSJ-04-132PROTACCDKProteolysis-targeting chimeraCyclin dependent kinaseRibociclibIKZF1/3JurkatInhibitorinhibitorinhibit

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产品名称:
BSJ-04-132
目录号:
HY-136252
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