1. Others
  2. Others
  3. CSN5i-3

CSN5i-3 

Cat. No.: HY-112134
Handling Instructions

CSN5i-3 is a potent, selective and orally available inhibitor of CSN5; 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

Size Stock
250 mg Get quote
500 mg Get quote

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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

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

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

Please store the product under the recommended conditions in the Certificate of Analysis.

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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CSN5i-3
Cat. No.:
HY-112134
Quantity: