Home NF-κB IκB/IKK inhibitor SC-514

research use only

SC-514 IκB/IKK inhibitor

Cat.No.S4907

SC-514 (GK 01140) is an orally active, ATP-competitive IKK-2 inhibitor with IC50 of 3-12 μM, blocks NF-κB-dependent gene expression, does not inhibit other IKK isoforms or other serine-threonine and tyrosine kinases.
SC-514 IκB/IKK inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 224.3

Jump to

Quality Control

Batch: S490701 DMSO]45 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.9%
  • Cited in Nature Medicine for its top-tier quality
  • COA
  • NMR
  • HPLC
  • SDS
  • Datasheet
99.9

Solubility

In vitro
Batch:

DMSO : 45 mg/mL (200.62 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg
g
μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
% DMSO
+
%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 224.3 Formula

C9H8N2OS2

 Storage (From the date of receipt)
CAS No. 354812-17-2 Download SDF Storage of Stock Solutions

Synonyms GK 01140 Smiles C1=CSC=C1C2=CC(=C(S2)C(=O)N)N

Mechanism of Action

Targets/IC50/Ki
IKK2
3 μM-12 μM
CDK2/CyclinA
61 μM
AUR2
71 μM
PRAK
75 μM
MSK
123 μM
In vitro
SC-514 inhibits the native IKK complex or recombinant human IKK-1/IKK-2 heterodimer and IKK-2 homodimer similarly. This compound inhibits transcription of NF-κB-dependent IL-6, IL-8, and COX-2 genes in IL-1β-induced rheumatoid arthritis-derived synovial fibroblasts (RASFs) with IC50s of 20, 20 and 8 μM. 100 μM of this chemical blocks the phosphorylation and degradation of IκBα and also reduces the level of translocation of p65 into the nucleus in IL-1β-treated RASFs. It does not inhibit the phosphorylation and activation of the IKK complex. This inhibitor induces a delay but not a complete blockade in IκBα phosphorylation and degradation. Treatment with this compound shows a slightly slowed, decreased import of p65 into the nucleus and a faster export of p65 from the nucleus. It inhibits the phosphorylation of either IκBα or p65 similarly.
In vivo
SC-514 is efficacious in an acute model of inflammation, namely LPS-induced serum TNF-α production. This compound (50 mg/kg, i.p.) inhibits TNF-α production in vivo by ~70%.
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map