| Name | CSN5i-3 |
| Description | CSN5i-3 is a potent, selective, and orally available inhibitor of the proteolytic subunit of the CSN complex, CSN5. It inhibits CSN-catalyzed Cul1 deneddylation with an IC50 value of 5.8 nM. CSN5i-3 has a killing effect on a variety of cancer cells and can be used as an anticancer drug. [2] |
| In vitro | METHODS: BV2 microglial cell line cells were pretreated with 1 or 4 μM CSN5i-3 for 2-4 hours to test whether treatment of BV2 cells with CSN5i-3 would result in an increase in NEDDylated CUL1 levels.
RESULTS Treatment of BV2 cells with CSN5i-3 for 4 hours under basal conditions required only normal "cell culture stress" to result in an increase in NEDDylated CUL1, accompanied by a decrease in unmodified CUL1 levels, and CSN5i-3-treated BV2 cells showed a shift from a de-NEDDylated cullin band to a NEDD8-CUL1 band. [1] |
| In vivo | METHODS: Subcutaneous SU-DHL-1 xenografts were implanted in SCID-bg mice and CSN5i-3 (50, 100 mg/kg, oral, once daily) was used to observe the growth of CSN5i-3 human xenograft models in vivo.
RESULTS CSN5i-3 inhibited tumor growth in the mouse model of human xenografts. [2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 247.5 mg/mL (489.56 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5 mg/mL (9.89 mM), Sonication is recommended.
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| Keywords | CSN5i-3 | CSN-5i-3 | CSN5i3 | CSN5i 3 | Apoptosis |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Apoptosis Compound Library | Bioactive Compound Library | Anti-Breast Cancer Compound Library | Inhibitor Library | Orally Active Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library |
United States
