1. NF-κB
    Anti-infection
  2. NF-κB
    Influenza Virus
  3. SC75741

SC75741 

Cat. No.: HY-10496 Purity: 99.51%
Handling Instructions

SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65. SC75741 blocks influenza viruses (IV) replication in non-toxic concentrations. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins.

For research use only. We do not sell to patients.

SC75741 Chemical Structure

SC75741 Chemical Structure

CAS No. : 913822-46-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 112 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 160 In-stock
Estimated Time of Arrival: December 31
25 mg USD 310 In-stock
Estimated Time of Arrival: December 31
50 mg USD 560 In-stock
Estimated Time of Arrival: December 31
100 mg USD 990 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

SC75741 is a broad and efficient NF-κB inhibitor with an IC50 of 200 nM for p65[1]. SC75741 blocks influenza viruses (IV) replication in non-toxic concentrations. SC75741 impairs DNA binding of the NF-κB subunit p65, resulting in reduced expression of cytokines, chemokines, and pro-apoptotic factors. SC75741 subsequently inhibits caspase activation and blocks caspase-mediated nuclear export of viral ribonucleoproteins[2].

IC50 & Target[1,2]

p65

200 nM (IC50)

In Vitro

SC75741 (5 μM; 24-96 hours) inhibits long-term A549 cells proliferation[2].
SC75741 (1-10 μM; 5.5-65 hours) reduces A549 cells viability in a concentration-dependent manner indicating a cytostatic effect for A549 cells within a time frame of about 50 and 65 hours[2].
SC75741 (5 μM; 24 hours) strongly inhibits cleavage of the effector caspase 3 induced upon H7N7-infection[2].

Cell Proliferation Assay[2]

Cell Line: A549 cells
Concentration: 5 μM
Incubation Time: 24, 48, 72 and 96 hours
Result: Inhibited long-term cell proliferation

Cell Viability Assay[2]

Cell Line: A549 cells
Concentration: 1, 2, 5 or 10 μM
Incubation Time: 5.5, 29, 50, 65 hours
Result: Reduced cells viability in a concentration-dependent manner.

Western Blot Analysis[2]

Cell Line: MDCK cells
Concentration: 5 μM
Incubation Time: 24 hours
Result: Inhibited cleavage of the effector caspase 3 induced upon H7N7-infection.
In Vivo

SC75741 (intraperitoneal injection; 15 mg/kg; for 2 days) leads to a reduced propagation of the H5N1 virus mRNA by 90% in the lungs of infected mice[2].
The plasma-levels of SC74751 (intravenously of 5 mg/kg and intraperitoneally of 15 mg/kg; for 3.5 and 6 hours) after i.v. administration decreases mono-exponentially and half-life is roughly 40 min. After i.p. administration, elimination of SC75741 seems to be limited by a slow uptake from the peritoneum and a half-life of 55 min is observed[1].

Animal Model: Inbred female C57BL/6 mice at the age of 6-8 weeks[2]
Dosage: 15 mg/kg
Administration: Intraperitoneal injection; for 2 days
Result: Reduced the amount of viral mRNA by 90%.
Animal Model: Inbred female C57BL/6 mice at the age of 6-8 weeks[1]
Dosage: 5 mg/kg or 15 mg/kg
Administration: Intravenously of 5 mg/kg and intraperitoneally of 15 mg/kg; 3.5 and 6 hours
Result: Half-life was roughly 40 min and 55 min for i.v. and i.p. administration, respectively.
Molecular Weight

565.67

Formula

C₂₉H₂₃N₇O₂S₂

CAS No.

913822-46-5

SMILES

O=C(NC1=NC(C=CC(C(C2=CC=CC=C2)=O)=C3)=C3N1)C4=CSC(C(CC5)CCN5C6=NC=NC7=C6SC=C7)=N4

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 : ≥ 125 mg/mL (220.98 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7678 mL 8.8391 mL 17.6782 mL
5 mM 0.3536 mL 1.7678 mL 3.5356 mL
10 mM 0.1768 mL 0.8839 mL 1.7678 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (3.68 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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SC75741
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