1. Immunology/Inflammation Apoptosis
  2. Interleukin Related Apoptosis
  3. SC144

SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells.

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SC144 Chemical Structure

SC144 Chemical Structure

CAS No. : 895158-95-9

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Customer Review

Based on 5 publication(s) in Google Scholar

Other Forms of SC144:

Top Publications Citing Use of Products

    SC144 purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Jan 8.  [Abstract]

    SC144 (20 mg/kg; dissolved in DMSO; i.p.; single) significantly inhibits the expression of gp130 in mouse lung tissue.
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    Description

    SC144 is a first-in-class, orally active gp130 (IL6-beta) inhibitor. SC144 binds gp130, induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes. SC144 shows potent inhibition of gp130 ligand-triggered signaling. SC144 induces apoptosis in human ovarian cancer cells[1].

    IC50 & Target[1]

    IL6-beta

     

    In Vitro

    SC144 inhibits cell growth in a panel of human ovarian cancer cell lines with IC50s in a submicromolar range (IC50=OVCAR-8, OVCAR-5, OVCAR-3= 0.72, 0.49, 0.95 μM)[1].
    ? The potency of SC144 toward NCI/ADR-RES (Paclitaxel- and Doxorubicin-resistant, IC50=0.43 μM) and HEY (Cisplatin-resistant, IC50=0.88 μM) suggests an ability to overcome drug resistance in ovarian cancer[1].
    ? SC144 (2 μM; 24 hours) causes significantly more apoptosis in OVCAR-8 and Caov-3 than normal kidney epithelial and normal endometrial cells[1].
    ? SC144 (0.5-2 μM; 0-6 hours) substantially increases the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cells in a time- and dose-dependent manner[1].
    ? SC144 is cytotoxic to ovarian cancer cells via a mechanism involving the inhibition of gp130 activity, leading to the inactivation of Akt and Stat3 as well as the suppression of Stat3-regulated gene expression. As are result, SC144 treatment eventually causes cell-cycle arrest, anti-angiogenesis, and apoptosis[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Apoptosis Analysis[1]

    Cell Line: OVCAR-8 and Caov-3 cells
    Concentration: 2 μM
    Incubation Time: 24 hours
    Result: Significantly caused cell death in OVCAR-8 and Caov-3 cells.

    Western Blot Analysis[1]

    Cell Line: OVCAR-8, Caov-3 cells
    Concentration: 0.5-2 μM
    Incubation Time: 0-6 hours
    Result: Substantially increased the phosphorylation of gp130 (S782) in both OVCAR-8 and Caov-3 cellsin a time- and dose-dependent manner.
    In Vivo

    SC144 (10 mg/kg; i.p.; daily for 58 days) suppresses tumor growth in human ovariancancer xenografts[1].
    ? SC144 (100 mg/kg;p.o.; daily for 35 days) treatment shows the average tumor volume in mice 82% smaller than that in the control group[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Athymic mice (human ovarian cancer xenograft)[1]
    Dosage: 10 mg/kg
    Administration: I.p; daily for 58 days
    Result: Significantly inhibited tumor growth by about 73%.
    Molecular Weight

    322.30

    Formula

    C16H11FN6O

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    O=C(C1=NC=CN=C1)NNC2=NC3=C(N4C2=CC=C4)C=CC(F)=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

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

    DMSO : 16.67 mg/mL (51.72 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 3.1027 mL 15.5135 mL 31.0270 mL
    5 mM 0.6205 mL 3.1027 mL 6.2054 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    Purity & Documentation
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    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.1027 mL 15.5135 mL 31.0270 mL 77.5675 mL
    5 mM 0.6205 mL 3.1027 mL 6.2054 mL 15.5135 mL
    10 mM 0.3103 mL 1.5513 mL 3.1027 mL 7.7567 mL
    15 mM 0.2068 mL 1.0342 mL 2.0685 mL 5.1712 mL
    20 mM 0.1551 mL 0.7757 mL 1.5513 mL 3.8784 mL
    25 mM 0.1241 mL 0.6205 mL 1.2411 mL 3.1027 mL
    30 mM 0.1034 mL 0.5171 mL 1.0342 mL 2.5856 mL
    40 mM 0.0776 mL 0.3878 mL 0.7757 mL 1.9392 mL
    50 mM 0.0621 mL 0.3103 mL 0.6205 mL 1.5513 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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    Product Name:
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    Cat. No.:
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