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CSN5i-3
🥰Excellent
Catalog No. T10895Cas No. 2375740-98-8
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]
CSN5i-3
🥰Excellent
Purity: 100%
Catalog No. T10895Cas No. 2375740-98-8
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]
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $378 | In Stock | |
| 5 mg | $813 | In Stock | |
| 10 mg | $1,230 | In Stock | |
| 25 mg | $1,830 | In Stock | |
| 50 mg | $2,470 | In Stock | |
| 100 mg | $3,330 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $886 | In Stock |
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Purity:100%
ee:100%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| 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] |
| Targets&IC50 | CSN5:5.8 nM |
| 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] |
| Molecular Weight | 505.56 |
| Formula | C28H29F2N5O2 |
| Cas No. | 2375740-98-8 |
| Smiles | CC(C)n1nc(cc1C(=O)Nc1ccc([C@H]2[C@@H](O)CCCc3cncn23)c(c1)-c1ccccc1)C(F)F |
| Relative Density. | 1.35 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 50 mg/mL (98.9 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
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Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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