dRRM-1
dRRM-1 is a DCAF15-dependent RBM39/RBM23 molecular glue degrader. dRRM-1 stabilizes the interaction between DCAF15 and the novel substrates RBM39 and RBM23, thereby triggering their ubiquitination and degradation. dRRM-1 can be applied in research related to cancer.
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- CAS 番号: 253328-68-6
- 分子式: C16H14N2O2S
- 分子量:298.36
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
RBM39 |
RBM23 |
体外実験
dRRM-1 (3 days) exerts cytotoxic effects that reduce cell viability to varying degrees in KBM7, MV4;11, RS4;11, HCT116, and HEK293T cells[1].
dRRM-1 (5-20 µM; 10 h) exhibits the effect of degrading the RBM39 protein in RS4;11, KBM7, HEK293, and HCT116 cells[1].
dRRM-1 (10 µM; 10 h) rescues DCAF15 from autodegradation and significantly stabilizes DCAF15 protein abundance, while markedly reducing the protein levels of RBM23 and RBM39 in HEK293t DCAF15-/- cells expressing HiBit-DCAF15 and LgBit[1].
dRRM-1 (0.001-100 μM; 60 min) binds to purified DCAF15 in a concentration-dependent manner, and displaces pre-bound E7820 with low binding affinity over the concentration range of 0.001 to 100 μM[1].
dRRM-1 (10 μM; 2 h-22 h) induces proteasome-dependent degradation of RBM23 in HAP1 RBM23-NanoLuc knock-in cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293t DCAF15-/- cells reconstituted with HiBit-DCAF15
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Concentration:10 μM
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Incubation Time:10 h
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Result:Reduced RBM39 protein levels in DCAF15-reconstituted HEK293t cells.
Caused no reduction in RBM39 levels in DCAF15-/- cells, confirming DCAF15 dependency.
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Cell Line:RS4;11, KBM7, HEK293, HCT116 cells
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Concentration:5 µM, 20 µM
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Incubation Time:10 h
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Result:Effectively degraded RBM39 across multiple cellular backgrounds.
化学情報
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CAS 番号 253328-68-6
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分子量 298.36
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分子式 C16H14N2O2S
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SMILES
CC1=CC=C(C=C1)S(=O)(NC2=CC=C3N=CC=CC3=C2)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)