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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- 純度: 99.53%
- CAS 番号: 118719-16-7
- 分子式: C14H13BrN2O3S
- 分子量:369.23
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
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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.
化学情報
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CAS 番号 118719-16-7
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性状 Solid
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分子量 369.23
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
[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 関連分類
HY-W133627 関連分類
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