| Name | SC144 |
| Description | SC144 is an orally active small-molecule gp130 inhibitor. |
| Cell Research | MTT assay (Only for Reference) |
| 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] |
| 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] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 15 mg/mL (46.54 mM), Sonication is recommended.
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
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| Keywords | translocation | SC-144 | SC144 | SC 144 | phosphorylation | ovarian | oral | nuclear | Interleukin Related | Interleukin | Inhibitor | inhibit | gp130 | cell-cycle | cancer | arrest | Apoptosis | anti-angiogenesis |
| Inhibitors Related | Kaolin | Stavudine | Aceglutamide | Urea | Tamoxifen | D(+)-Raffinose pentahydrate | Metronidazole | Hydroxypropyl Cellulose | Formamide | Gluconate Calcium | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Nonsteroidal Anti-Inflammatory Compound Library | Apoptosis Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Hematonosis Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Active Compound Library |
United States
