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 No.: 253328-68-6
- 화학식: C16H14N2O2S
- 분자량:298.36
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
RBM39 |
RBM23 |
In Vitro
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.
Chemical Information
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CAS No. 253328-68-6
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분자량 298.36
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화학식 C16H14N2O2S
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SMILES
CC1=CC=C(C=C1)S(=O)(NC2=CC=C3N=CC=CC3=C2)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Hanzl A, et al. E3-Specific Degrader Discovery by Dynamic Tracing of Substrate Receptor Abundance. Journal of the American Chemical Society. 2023 Jan 18;145(2):1176-1184. [Content Brief]
[2]. Best AJ, et al. High-throughput sensitive screening of small molecule modulators of microexon alternative splicing using dual Nano and Firefly luciferase reporters. Nature communications. 2024 Jul 27;15(1):6328. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
dRRM-1 Related Classifications
HY-177779 Related Classifications
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