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CSN5i-3

Name: CSN5i-3
Brand: TargetMol
SKU: T10895
Price: 378 USD
Availability: InStock
Rating: 5 (10 reviews)

🥰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: 99.73%

Catalog No. T10895Cas No. 2375740-98-8

Pack Size	Price	Availability
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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This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. However, due to objective factors, there is a small probability that the synthesis may not be successful during the R&D process. We appreciate your understanding. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.73%

ee:100%

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COA LCMS CSFC FNMR HNMR ORP

Product Introduction

Bioactivity

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	CSN:∼5.4 nM, 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]

Chemical Properties

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/Shipping at ambient temperature.

Solubility Information

DMSO: 247.5 mg/mL (489.56 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.89 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9780 mL	9.8900 mL	19.7800 mL	98.9002 mL
5 mM	0.3956 mL	1.9780 mL	3.9560 mL	19.7800 mL
10 mM	0.1978 mL	0.9890 mL	1.9780 mL	9.8900 mL
20 mM	0.0989 mL	0.4945 mL	0.9890 mL	4.9450 mL
50 mM	0.0396 mL	0.1978 mL	0.3956 mL	1.9780 mL
100 mM	0.0198 mL	0.0989 mL	0.1978 mL	0.9890 mL

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In Vivo Formulation Calculator (Clear solution)

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 . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(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 TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

All types of co-solvents required for the protocol, such asDMSO, PEG300/ PEG400, Tween 80, SBE-β-CD, corn oil are available for purchase on the TargetMol website with a simple click.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc