2. Immunology/Inflammation Apoptosis
  3. Interleukin Related Apoptosis
  4. 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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CAS No. : 895158-95-9

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 10 publication(s) in Google Scholar

Other Forms of SC144:

SC144 Related Antibodies

Top Publications Citing Use of Products

    SC144 purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Mar;72(3):493-507.  [Abstract]

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

    View All Interleukin Related Isoform Specific Products:

    View All Isoforms
    IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

    • Biological Activity

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    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

     

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    0.6 μM
    Compound: SC144
    Cytotoxicity against human HCT116 cells expressing p53 gene after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells expressing p53 gene after 72 hrs by MTT assay
    		[PMID: 17085054]
    HCT-116 IC50
    0.9 μM
    Compound: SC144
    Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by MTT assay
    Cytotoxicity against p53 deficient human HCT116 cells after 72 hrs by MTT assay
    		[PMID: 17085054]
    HT-29 IC50
    0.9 μM
    Compound: SC144
    Cytotoxicity against human HT29 cells after 72 hrs by MTT assay
    Cytotoxicity against human HT29 cells after 72 hrs by MTT assay
    		[PMID: 17085054]
    LNCaP IC50
    0.4 μM
    Compound: SC144
    Cytotoxicity against human LNCap cells after 72 hrs by MTT assay
    Cytotoxicity against human LNCap cells after 72 hrs by MTT assay
    		[PMID: 17085054]
    LNCaP IC50
    0.4 μM
    Compound: 7
    Cytotoxicity against human LNCaP cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Cytotoxicity against human LNCaP cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    		[PMID: 36971365]
    MDA-MB-435 IC50
    0.4 μM
    Compound: 7
    Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-435 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    		[PMID: 36971365]
    MDA-MB-435 IC50
    4 μM
    Compound: SC144
    Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-435 cells after 72 hrs by MTT assay
    		[PMID: 17085054]
    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.

    SC144 Related Antibodies

    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%.
    분자량

    322.30

    화학식

    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
    선적

    Room temperature in continental US; may vary elsewhere.
    보관
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    용액&용해도
    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.

    • 몰농도 계산기

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

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    Concentration
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Calculation results:
    Working solution concentration: mg/mL
    순도&문서
    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, 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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    SC144 Related Classifications

    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.

    Keywords:

    SC144895158-95-9SC 144SC-144Interleukin RelatedApoptosisILoralphosphorylationnucleartranslocationcell-cyclearrestanti-angiogenesisovariancancerInhibitorinhibitorinhibit

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    상품명:
    SC144
    Cat. No.:
    HY-15614
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