SC144

Catalog No.S7124

SC144 Chemical Structure

Molecular Weight(MW): 322.3

SC144 is the first-in-class orally active small-molecule gp130 inhibitor that induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes.

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Cited by 3 Publications

1 Customer Review

  • Suppression of gp130/STAT3 blocks the protective effect of SPRC against Dox-induced cell apoptosis. Cardiomyocytes were pretreated with/without SC144 before SPRC incubation, followed by Dox (1 μM) stimulation for 24 h. (a) Morphological apoptosis was determined by Hoechst 33258 staining. Scale bars, 50 μm.

    Cell Death Dis, 2016, 7(8):e2339.. SC144 purchased from Selleck.

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Biological Activity

Description SC144 is the first-in-class orally active small-molecule gp130 inhibitor that induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes.
Targets
gp130 [1]
In vitro

SC144 exhibits potent cytotoxicity against a panel of drug-sensitive and drug-resistant cancer cell lines. SC144 shows synergism with both 5-fluorouracil and oxaliplatin when co-treated in colorectal cancer HT29 cells. Pretreatment with SC144 in oxaliplatin-resistant HTOXAR3 cells is more effective than oxaliplatin pretreatment. In addition, the combination of SC144 and paclitaxel exhibited synergism in MDA-MB-435 cells with a schedule-dependent block in cell cycle. [1] SC144 treatment in vitro induces gp130 phosphorylation and deglycosylation, resulting in the downregulation of surface-bound gp130 and the abrogation of gp130-associated Stat3 activation. In addition, SC144 selectively inhibits the downstream signaling activation induced by gp130 substrates, including IL-6 and LIF. Protein expression regulated by the gp130/Stat3 axis in OVCAR-8 cells is also down-regulated after SC144 treatment, including Bcl-2, Bcl-XL, survivin, cyclin D1, MMP-7, gp130 and Ape1/Rel-1. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LNCap cells MVTDfZRwfG:6aXPpeJkh[XO|YYm= MkfUO|IhcA>? MlHsR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG5E[XBiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3ME2wMlQh|ryP MVixO|A5PTB3NB?=
HCT116 cells MX;DfZRwfG:6aXPpeJkh[XO|YYm= MXG3NkBp MWTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh\XiycnXzd4lv\yCyNUOg[4Vv\SCjZoTldkA4OiCqcoOgZpkhVVSWIHHzd4F6NCCLQ{WwQVAvPiEQvF2= NI\XcFcyPzB6NUC1OC=>
HT29 cells M2nIeWN6fG:2b4jpZ4l1gSCjc4PhfS=> MkX0O|IhcA>? MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIWFI6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD65JO69VQ>? NV;Y[W9GOTdyOEWwOVQ>
HCT116 cells MULDfZRwfG:6aXPpeJkh[XO|YYm= NFTJXZk4OiCq MXrDfZRwfG:6aXPpeJkh[WejaX7zeEBxPTNiZHXmbYNq\W62IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwOTFOwG0> MmD3NVcxQDVyNUS=
MDA-MB-435 cells NG\XbFNEgXSxdH;4bYNqfHliYYPzZZk> NGnFcnQ4OiCq MWXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvNEO1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:PCEQvF2= NVzGPHprOTdyOEWwOVQ>

... Click to View More Cell Line Experimental Data

In vivo SC144 significantly inhibits tumor growth in a mouse xenograft model of human ovarian cancer via i.p. or p.o. administration. After SC144 treatment for two months, gp130, Bcl-2, Bcl-XL, MMP-7 and Ape1/Ref-1 protein levels are substantially decreased in the tumor site in the treatment group compared with the control group. [2] In an MDA-MB-435 mouse xenograft model, co-administration of SC144 and paclitaxel delays tumor growth in an SC144 dose-dependent manner. Evaluation of the pharmacokinetics of SC144 reveals that intraperitoneal administration of SC144 shows a two-compartmental pharmacokinetics elimination profile that is not observed in the oral dosing. [1]

Protocol

Cell Research:

[2]

+ Expand
  • Cell lines: OVCAR-8, OVCAR-5, OVCAR-3, Caov-3, SKOV-3, HEY NCI/ADR-RES
  • Concentrations: ~10 μM
  • Incubation Time: 96 h
  • Method:

    MTT assay


    (Only for Reference)
Animal Research:

[2]

+ Expand
  • Animal Models: Human Ovarian Cancer OVCAR-8 Xenograft
  • Formulation: 0.9% NaCl with 40% propylene glycol
  • Dosages: 10 mg/kg daily
  • Administration: i.p. or p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 28 mg/mL (86.87 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 322.3
Formula

C16H11FN6O

CAS No. 895158-95-9
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID