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CSN5i-3

SKU: orb1709975

Description

CSN5i-3 is a potent, selective, and orally bioavailable small molecule inhibitor of the CSN5 subunit, exhibiting an IC50 of 5.8 nM for CSN-mediated Cul1 deneddylation. Its anticancer activity, demonstrated through in vitro cytotoxicity against various cancer cell lines, makes it a valuable chemical probe for studying CSN complex biology and oncology research.

Research Area

Cell Biology

Images & Validation

Key Properties

CAS Number2375740-98-8
MW505.56
Purity99.87%
FormulaC28H29F2N5O2
SMILESCC(C)n1nc(cc1C(=O)Nc1ccc([C@H]2[C@@H](O)CCCc3cncn23)c(c1)-c1ccccc1)C(F)F
TargetOthers,Apoptosis
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (9.89 mM);DMSO:247.5 mg/mL (489.56 mM)

Bioactivity

Target IC50
CSN5:5.8 nM|CSN:∼5.4 nM
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.
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Apoptosis, CSN5i 3, CSN5i3, CSN-5i-3, CSN5i-3

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Quality Guarantee

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Key Properties

No computed properties available.

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CSN5i-3 (orb1709975)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 5,460.00
5 mg
¥ 11,180.00
1 ml x 10 mM (in DMSO)
¥ 12,090.00
10 mg
¥ 16,510.00
25 mg
¥ 24,310.00
50 mg
¥ 32,630.00
100 mg
¥ 43,810.00
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