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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- No. CAS: 253328-68-6
- Fòrmula: C16H14N2O2S
- Peso molecular:298.36
-
Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
Descripciòn
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. .
-
Cell Line:HEK293t DCAF15-/- cells reconstituted with HiBit-DCAF15
-
Concentration:10 μM
-
Incubation Time:10 h
-
Result:Reduced RBM39 protein levels in DCAF15-reconstituted HEK293t cells.
Caused no reduction in RBM39 levels in DCAF15-/- cells, confirming DCAF15 dependency.
-
Cell Line:RS4;11, KBM7, HEK293, HCT116 cells
-
Concentration:5 µM, 20 µM
-
Incubation Time:10 h
-
Result:Effectively degraded RBM39 across multiple cellular backgrounds.
Chemical Information
-
No. CAS 253328-68-6
-
Peso molecular 298.36
-
Fòrmula C16H14N2O2S
-
SMILES
CC1=CC=C(C=C1)S(=O)(NC2=CC=C3N=CC=CC3=C2)=O
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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
Powered by Bioz