1. NF-κB Anti-infection Apoptosis JAK/STAT Signaling
  2. NF-κB HCV Apoptosis Pim c-Myc
  3. RS47

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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RS47

RS47 Chemical Structure

CAS No. : 301655-16-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Description

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[1][2].

Cellular Effect
Cell Line Type Value Description References
Huh-5-2 CC50
> 141 μM
Compound: 1a-SPECS
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
[PMID: 27474921]
Huh-5-2 CC50
> 282 μM
Compound: 1a-synth
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
[PMID: 27474921]
In Vitro

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.

Cell Proliferation Assay[1]

Cell Line: HCT116, SW620
Concentration: 0.5 μM, 1 μM, 2 μM
Incubation Time: 72 h
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.

Apoptosis Analysis[1]

Cell Line: BJAB, U2932
Concentration: 0 μM, 0.5 μM, 1 μM, 2 μM
Incubation Time: 72 h
Result: Significantly promoted apoptosis in a dose-dependent manner.

Real Time qPCR[1]

Cell Line: BJAB, primary B cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Inhibited BAFF-induced Pim2 mRNA expression in BJAB cells and primary B cells.
In Vivo

RS47 (50 mg/kg; i.p.; 21 days) inhibits tumor growth of human B lymphoma PDX xenografts in BALB/c athymic nude mice[1].
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.

Animal Model: BALB/c athymic nude mice (male, 6-week-old, induced by subcutaneous injection of human B lymphoma tissue from PDX models)[1]
Dosage: 50 mg/kg
Administration: i.p.; daily
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.
Molecular Weight

354.43

Formula

C18H18N4O2S

CAS No.
Appearance

Solid

Color

Yellow to brown

SMILES

OC1=CC=C(C(/C(C)=N/NC2=C3C(CCCC4)=C4SC3=NC=N2)=C1)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8214 mL 14.1072 mL 28.2143 mL
5 mM 0.5643 mL 2.8214 mL 5.6429 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.0%

References

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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