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CSN5i-3 

Cat. No.: HY-112134 Purity: 99.12% ee.: 99.23%
Handling Instructions

CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM.

For research use only. We do not sell to patients.

CSN5i-3 Chemical Structure

CSN5i-3 Chemical Structure

CAS No. : 2375740-98-8

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 1090 In-stock
Estimated Time of Arrival: December 31
1 mg USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 980 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM[1].

IC50 & Target

IC50: 5.8 nM (CSN5)[1]

In Vitro

CSN5i-3 traps CRLs in the neddylated state, which leads to inactivation of a subset of CRLs by inducing degradation of their substrate recognition module[1].

In Vivo

CSN5i-3 shows a good pharmacokinetic profile. CSN5i-3 inhibits growth of human xenograft. Treatment with CSN5i-3 triggers the formation of cleaved PARP and cleaved caspase 3 indicative of apoptosis induction[1].

Molecular Weight

505.56

Formula

C₂₈H₂₉F₂N₅O₂

CAS No.

2375740-98-8

SMILES

O=C(C1=CC(C(F)F)=NN1C(C)C)NC2=CC(C3=CC=CC=C3)=C([[email protected]@H]4N5C(CCC[[email protected]@H]4O)=CN=C5)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (197.80 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9780 mL 9.8900 mL 19.7800 mL
5 mM 0.3956 mL 1.9780 mL 3.9560 mL
10 mM 0.1978 mL 0.9890 mL 1.9780 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.95 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay

Cell viability is measured using the CellTiter-Glo Assay. Cells (THP-1, HCT116, NCI-H2030 and TE-1) are treated with CSN5i-3 (1 nM, 10 nM, 100 nM, 1 μM, 10 μM) for 72 hours[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]

SU-DHL-1 xenografts were grown in SCID-bg mice and dosed by oral administration with either vehicle control or CSN5i-3 at the indicated doses (50 mg/kg BID, 100mg/kg QD) and schedules (3, 7, 10, 14 day). Tumour response is reported as percentage change in tumour volume at the last day of treatment relative to start of treatment.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

CSN5i-3OthersInhibitorinhibitorinhibit

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CSN5i-3
Cat. No.:
HY-112134
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