2. Immunology/Inflammation
    Apoptosis
  3. Interleukin Related
    Apoptosis
  4. SC144 hydrochloride

SC144 hydrochloride 

Cat. No.: HY-15614A Purity: 99.34%
COA Handling Instructions

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

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

SC144 hydrochloride Chemical Structure

SC144 hydrochloride Chemical Structure

CAS No. : 917497-70-2

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10 mM * 1 mL in DMSO USD 61 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of SC144 hydrochloride:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE SC144 hydrochloride

WB

    SC144 hydrochloride purchased from MCE. 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.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    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].

    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: I.p; daily for 58 days
    Administration: 10 mg/kg
    Result: Significantly inhibited tumor growth by about 73%.
    Molecular Weight

    358.76

    Appearance

    Solid

    Formula

    C16H12ClFN6O
    CAS No.
    SMILES

    O=C(C1=NC=CN=C1)NNC2=NC3=C(N4C2=CC=C4)C=CC(F)=C3.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    Solvent & Solubility
    In Vitro: 

    DMSO : 10 mg/mL (27.87 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.7874 mL 13.9369 mL 27.8738 mL
    5 mM 0.5575 mL 2.7874 mL 5.5748 mL
    10 mM 0.2787 mL 1.3937 mL 2.7874 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

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

      Solubility: ≥ 1 mg/mL (2.79 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.34%

    COA (249 KB) LCMS (267 KB)

    Handling Instructions (2659 KB)
    References
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    Help & FAQs
    • 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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    Keywords:

    SC144917497-70-2SC 144SC-144Interleukin RelatedApoptosisILoralphosphorylationnucleartranslocationcell-cyclearrestanti-angiogenesisovariancancerInhibitorinhibitorinhibit

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