RS47
Based on 1 Customer Validation
RS47 is a selective RelB inhibitor with a Kd value of 1.1 μM. RS47 also acts as an inhibitor of HCV replication. RS47 can block the non-canonical NF-κB signaling pathway without affecting the canonical pathway. RS47 exerts anti-tumor effects of inhibiting proliferation and promoting apoptosis on colorectal cancer, B-cell lymphoma and other related tumors both in vitro and in vivo by disrupting the binding of RelB to target DNA. RS47 can be used for the research of tumors and infectious diseases.
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- Pureza: 98.0%
- No. CAS: 301655-16-3
- Fòrmula: C18H18N4O2S
- Peso molecular:354.43
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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
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-5-2 | CC50 |
>141 μM
Compound: 1a-SPECS
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Cytotoxicity against human HuH5.2 cells assessed as reduction in metabolic activity after 72 hrs by MTS assay
Cytotoxicity against human HuH5.2 cells assessed as reduction in metabolic activity after 72 hrs by MTS assay
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[PMID: 27474921] |
| Huh-5-2 | CC50 |
>282 μM
Compound: 1a-synth
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Cytotoxicity against human HuH5.2 cells assessed as reduction in metabolic activity after 72 hrs by MTS assay
Cytotoxicity against human HuH5.2 cells assessed as reduction in metabolic activity after 72 hrs by MTS assay
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[PMID: 27474921] |
RS47 (0-10 μM) inhibits HCT116, BJAB and U2932 cells viability with IC50 values of 1.28 , 0.255 and 0.159 μM[1].
RS47 (0-3 μM; 0-7 days) can inhibit the proliferation, colony formation, and invasion of HCT116 cells[1].
RS47 (0-2 μM; 72 h) induces apoptosis and cell cycle arrest in HCT116/SW620 colorectal cancer cells[1].
RS47 (0-2 μM; 72 h) promotes apoptosis in BJAB and U2932 cells[1].
RS47 (1 μM; 24 h) inhibits the expression of BAFF-inducible target genes (e.g., Pim2) in the non-canonical NF-κB pathway in BJAB cells and primary B cells[1].
RS47 inhibits HCV replication in Huh5-2 cells (EC50 < 2.2 μM)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116, SW620
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Concentration:0.5 μM, 1 μM, 2 μM
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Incubation Time:72 h
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Result:Caused a significant decrease in S phase population and an increase in G0/G1 and G2/M phase populations in a dose-dependent manner.
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Cell Line:BJAB, U2932
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Concentration:0 μM, 0.5 μM, 1 μM, 2 μM
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Incubation Time:72 h
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Result:Significantly promoted apoptosis in a dose-dependent manner.
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Cell Line:BJAB, primary B cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Inhibited BAFF-induced Pim2 mRNA expression in BJAB cells and primary B cells.
RS47 (50 mg/kg; i.p.; 21 days) significantly inhibits tumor growth and downregulates c-Myc expression in BALB/c nude mice with colorectal cancer xenografts[1]。
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c athymic nude mice (male, 6-week-old, induced by subcutaneous injection of human B lymphoma tissue from PDX models)[1]
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Dosage:50 mg/kg
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Administration:i.p.; daily
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Result:Remarkably reduced the tumor volume and weight of B lymphoma PDX xenografts. Immunohistochemical staining showed a decreased percentage of Ki-67-positive proliferating cells, and TUNEL assay revealed an increased number of apoptotic cells in the tumor tissues.
Downregulated the mRNA and protein expression of Bcl-2 and MYC, which are associated with cell survival and proliferation.
Had no/little toxicity to mice.
Chemical Information
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No. CAS 301655-16-3
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Appearance Solid
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Peso molecular 354.43
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Fòrmula C18H18N4O2S
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Color Yellow to brown
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SMILES
OC1=CC=C(C(/C(C)=N/NC2=C3C(CCCC4)=C4SC3=NC=N2)=C1)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
DMSO : 25 mg/mL (70.54 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)
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Li C, et al. Development of RelB-targeting small-molecule inhibitors of non-canonical NF-κB signaling with antitumor efficacy. Mol Ther. 2025;33(4):1519-1534. [Content Brief]
[2]. Bassetto M, et al. Computer-aided identification, synthesis and evaluation of substituted thienopyrimidines as novel inhibitors of HCV replication. Eur J Med Chem. 2016;123:31-47. [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 | 2.8214 mL | 14.1072 mL | 28.2143 mL | 70.5358 mL |
| 5 mM | 0.5643 mL | 2.8214 mL | 5.6429 mL | 14.1072 mL | |
| 10 mM | 0.2821 mL | 1.4107 mL | 2.8214 mL | 7.0536 mL | |
| 15 mM | 0.1881 mL | 0.9405 mL | 1.8810 mL | 4.7024 mL | |
| 20 mM | 0.1411 mL | 0.7054 mL | 1.4107 mL | 3.5268 mL | |
| 25 mM | 0.1129 mL | 0.5643 mL | 1.1286 mL | 2.8214 mL | |
| 30 mM | 0.0940 mL | 0.4702 mL | 0.9405 mL | 2.3512 mL | |
| 40 mM | 0.0705 mL | 0.3527 mL | 0.7054 mL | 1.7634 mL | |
| 50 mM | 0.0564 mL | 0.2821 mL | 0.5643 mL | 1.4107 mL | |
| 60 mM | 0.0470 mL | 0.2351 mL | 0.4702 mL | 1.1756 mL |
RS47 Related Classifications
HY-171579 Related Classifications
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