dCeMM1
Based on 1 Customer Validation
dCeMM1 is a molecular glue degrader that targets RBM39. dCeMM1 serves as a positive control for the screening of DCAF15-dependent molecular glue degraders. dCeMM1 promotes the DCAF15-RBM39 interaction, thereby recruiting RBM39 to the CRL4DCAF15 E3 ubiquitin ligase complex, inducing ubiquitination and subsequent proteasomal degradation of RBM39. Meanwhile, dCeMM1 stabilizes DCAF15 by mediating neo-substrate recruitment to protect DCAF15 from autodegradation. dCeMM1 reduces the viability of leukemia cells in a neddylation-dependent and proteasome-dependent manner, and can be applied in leukemia-related research.
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- Pureza : 99.53%
- No. CAS: 118719-16-7
- Fòrmula: C14H13BrN2O3S
- Peso molecular:369.23
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
In Vitro
dCeMM1 (500 nM-10 μM; 3 days) shows selective anti-proliferative activity in neddylation-proficient wildtype KBM7 and HCT116 cells, but not in hypo-neddylated UBE2MG12C-mutant counterparts[2].
dCeMM1 (50 μM; 24 h) exerts anti-proliferative effects on HAP1 leukemia cancer cells in a UBE2M-dependent, Cullin E3 ligase-dependent manner[4].
dCeMM1 (50 μM; 24 h) exerts anti-proliferative effects on HAP1 leukemia cancer cells in a NEDDylation-dependent manner[4].
dCeMM1 (9 μM; 14 days) activity requires functional UBE2M and the CRL4DCAF15 ligase complex in KBM7-Cas9 cells[2].
dCeMM1 (10 μM; 10 h) induces degradation of RBM39 in HEK293t DCAF15-/- cells with reconstituted HiBit-DCAF15, and this effect is dependent on the presence of DCAF15[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:isogenic wildtype and UBE2M-mutant KBM7 and HCT116 cells
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Concentration:500 nM-10 μM (primary screening); dose-ranging concentrations (validation)
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Incubation Time:3 days (primary screening); 3 days (validation)
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Result:Inhibited proliferation of wildtype KBM7 cells while sparing UBE2M-mutant KBM7 cells.
Confirmed differential viability profile in both KBM7 and HCT116 isogenic cell pairs.
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Cell Line:HAP1 leukemia cancer cells
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Concentration:50 μM
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Incubation Time:24 h
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Result:Impaired HAP1 cell viability in siControl cells.
Significantly attenuated anti-proliferative effect in siUBE2M (hyponeddylation) cells.\nImpaired HAP1 cell viability in DMSO-pre-treated cells.
Significantly attenuated anti-proliferative effect in MLN4924-pre-treated cells.
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Cell Line:HEK293t DCAF15-/- cells with reconstitution of 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 relative to DMSO-treated cells.
Showed no reduction in RBM39 levels in DCAF15 knockout cells treated with dCeMM1, confirming DCAF15-dependent degradation effect.
Chemical Information
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No. CAS 118719-16-7
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Appearance Solid
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Peso molecular 369.23
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Fòrmula C14H13BrN2O3S
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Color White to off-white
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SMILES
O=S(C1=CC=C(C)C=C1)(NN=CC2=CC(Br)=CC=C2O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (270.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Protocolo
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (630 KB)
- English - EN (630 KB)
- Français - FR (630 KB)
- Deutsch - DE (630 KB)
- Norwegian - NO (630 KB)
- Español - ES (630 KB)
- Swedish - SV (630 KB)
- Italian - IT (630 KB)
- Korean - KR (630 KB)
- Portuguese - PT (630 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Dong G, et al. Molecular Glues for Targeted Protein Degradation: From Serendipity to Rational Discovery. Journal of medicinal chemistry. 2021 Aug 12;64(15):10606-10620. [Content Brief]
[2]. Mayor-Ruiz C, et al. Rational discovery of molecular glue degraders via scalable chemical profiling. Nature chemical biology. 2020 Nov;16(11):1199-1207. [Content Brief]
[4]. King EA, et al. Chemoproteomics-enabled discovery of a covalent molecular glue degrader targeting NF-κB. Cell chemical biology. 2023 Apr 20;30(4):394-402.e9. [Content Brief]
[6]. 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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7083 mL | 13.5417 mL | 27.0834 mL | 67.7085 mL |
| 5 mM | 0.5417 mL | 2.7083 mL | 5.4167 mL | 13.5417 mL | |
| 10 mM | 0.2708 mL | 1.3542 mL | 2.7083 mL | 6.7708 mL | |
| 15 mM | 0.1806 mL | 0.9028 mL | 1.8056 mL | 4.5139 mL | |
| 20 mM | 0.1354 mL | 0.6771 mL | 1.3542 mL | 3.3854 mL | |
| 25 mM | 0.1083 mL | 0.5417 mL | 1.0833 mL | 2.7083 mL | |
| 30 mM | 0.0903 mL | 0.4514 mL | 0.9028 mL | 2.2569 mL | |
| 40 mM | 0.0677 mL | 0.3385 mL | 0.6771 mL | 1.6927 mL | |
| 50 mM | 0.0542 mL | 0.2708 mL | 0.5417 mL | 1.3542 mL | |
| 60 mM | 0.0451 mL | 0.2257 mL | 0.4514 mL | 1.1285 mL | |
| 80 mM | 0.0339 mL | 0.1693 mL | 0.3385 mL | 0.8464 mL | |
| 100 mM | 0.0271 mL | 0.1354 mL | 0.2708 mL | 0.6771 mL |
dCeMM1 Related Classifications
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