2. NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. IKK NF-κB Bcl-2 Family Reactive Oxygen Species (ROS) Apoptosis
  4. IKKβ-IN-7

IKKβ-IN-7 is an IKKβ inhibitor with an IC50 value of 9.44 μM. IKKβ-IN-7 induces DNA damage, S-phase cell cycle arrest, ROS accumulation, mitochondrial membrane potential loss, and apoptosis. IKKβ-IN-7 inhibits phosphorylation of p65 and IκBα, suppresses p65 nuclear translocation, and regulates NF-κB-controlled genes. IKKβ-IN-7 suppresses tumor growth in xenograft models and shows activity against colorectal cancer with low normal cell cytotoxicity. IKKβ-IN-7 can be used for the research of colorectal cancer.

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

IKKβ-IN-7

IKKβ-IN-7 Chemical Structure

CAS No. : 3117527-92-8

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

IKKβ-IN-7 Related Antibodies

Top Publications Citing Use of Products

View All IKK Isoform Specific Products:

View All Isoforms
IKK-α IKK-β IKK IKKε TBK1

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All Bcl-2 Family Isoform Specific Products:

View All Isoforms
Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

IKKβ-IN-7 is an IKKβ inhibitor with an IC50 value of 9.44 μM. IKKβ-IN-7 induces DNA damage, S-phase cell cycle arrest, ROS accumulation, mitochondrial membrane potential loss, and apoptosis. IKKβ-IN-7 inhibits phosphorylation of p65 and IκBα, suppresses p65 nuclear translocation, and regulates NF-κB-controlled genes. IKKβ-IN-7 suppresses tumor growth in xenograft models and shows activity against colorectal cancer with low normal cell cytotoxicity. IKKβ-IN-7 can be used for the research of colorectal cancer[1].

IC50 & Target[1]

IKKβ

9.44 μM (IC50)

p65

 

Bax

 

Bcl-2

 

Bcl-xL

 

In Vitro

IKKβ-IN-7 (6i2) (24 h) potently inhibits the proliferation of multiple cancer cell lines, including A549 cells (IC50 = 5.11 μM), HepG2 cells (IC50 = 9.81 μM), HCT-116 cells (IC50 = 1.08 μM), HT-29 cells (IC50 = 4.17 μM), RKO cells (IC50 = 4.72 μM), and CT-26 cells (IC50 = 0.86 μM), while showing low cytotoxicity toward normal transformed human liver epithelial THLE-2 cells (IC50 > 16 μM)[1].
IKKβ-IN-7 (1 h) directly inhibits IKKβ kinase activity with an IC50 of 9.44 μM[1].
IKKβ-IN-7 (2.0 μM; 30 min) potently inhibits Topo I activity, achieving a 96.84% inhibition rate at a concentration of 2.0 μM after 30 min incubation at 37°C[1].
IKKβ-IN-7 (0.5-2.0 μM; 24 h) exerts multiple biological effects on HCT-116 cells in vitro in a dose-dependent manner: induces DNA damage via increased γ-H2AX expression and reduces Topo I protein levels (maximal effects at 2.0 μM); dose-dependently inhibits the phosphorylation of IκBα and p65 to suppress NF-κB pathway activation; inhibits p65 nuclear translocation without altering total p65 protein levels; modulates Bcl-2 family protein expression (increases pro-apoptotic Bax and decreases anti-apoptotic Bcl-2, Bcl-xl, and Mcl-1) indicating induction of mitochondria-mediated apoptosis; induces apoptosis with a 68.29% apoptosis rate at 2.0 μM; induces S-phase cell cycle arrest with 44.6% of cells in S phase at 2.0 μM; increases intracellular ROS levels; reduces mitochondrial membrane potential[1].
IKKβ-IN-7 (0.5-2.0 μM; 24 h, 48 h) inhibits wound healing migration of human colorectal carcinoma HCT-116 cells in a dose-dependent manner[1].

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

IKKβ-IN-7 Related Antibodies

Western Blot Analysis[1]

Cell Line: human colorectal carcinoma HCT-116 cells
Concentration: 0.5, 1, 2.0 μM
Incubation Time: 24 h
Result: Decreased Topo I levels by more than 50% at 2.0 μM, and increased γ-H2AX expression by 2–3-fold in a dose-dependent manner compared with untreated controls.
Reduced the phosphorylation levels of IκBα and p65 gradually to less than 0.5-fold of control levels as concentration increased from 0.5 to 2.0 μM.
Left total p65 protein levels unchanged, but decreased nuclear p65 levels significantly and increased cytoplasmic p65 levels in a dose-dependent manner compared with controls.
Increased Bax expression in a dose-dependent manner, while significantly reduced the expression of anti-apoptotic proteins Bcl-2, Bcl-xL and Mcl-1 in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: human colorectal carcinoma HCT-116 cells
Concentration: 0.5, 1, 2.0 μM
Incubation Time: 24 h
Result: Induced apoptosis rates of 39.45% (0.5 μM), 58.14% (1.0 μM), and 68.29% (2.0 μM), compared to 8.86% in untreated controls.

Cell Cycle Analysis[1]

Cell Line: human colorectal carcinoma HCT-116 cells
Concentration: 0.5, 1, 2.0 μM
Incubation Time: 24 h
Result: Induced S-phase arrest, with the proportion of cells in S phase reaching 44.6% at 2.0 μM, in a dose-dependent manner.

Cell Migration Assay[1]

Cell Line: human colorectal carcinoma HCT-116 cells
Concentration: 0.5, 1, 2.0 μM
Incubation Time: 24 h; 48 h
Result: Inhibited wound healing in a dose-dependent manner, with wound healing rates of 25.23% (24 h, 0.5 μM), 5.70% (24 h, 1.0 μM), 4.69% (24 h, 2.0 μM), 69.67% (48 h, 0.5 μM), 54.78% (48 h, 1.0 μM), and 18.35% (48 h, 2.0 μM), compared to 43.05% (24 h) and 94.61% (48 h).
In Vivo

IKKβ-IN-7 (6i2) (2.5-60 mg/kg; i.p.; once every 2 days, consecutive 2 days) shows significant in vivo antitumor efficacy in CT-26 xenografts with good safety and low acute toxicity, and has certain plasma stability with sustained SN-38 (HY-13704) release[1].

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

Animal Model: Female immunocompetent BALB/c mice (5-6 weeks old) were subcutaneously injected with CT-26 cells (3 × 106 cells per mouse in 100 μL sterile PBS)[1]
Dosage: 2.5 mg/kg, 5 mg/kg
Administration: Intraperitoneal (IP) injection; once every other day
Result: Exhibited potent antitumor efficacy with tumor growth inhibition (TGI) rates of 68.81% (2.5 mg/kg) and 95.41% (5 mg/kg).
No significant body weight loss or animal mortality observed during the treatment period.
H&E staining of major organs (heart, liver, spleen, lung, kidney) revealed no obvious morphological abnormalities.
Superior safety profile compared to 10-HCPT (which caused inflammatory cell infiltration in spleen and glomerular atrophy in kidney at 2.5 mg/kg).
Animal Model: Female immunocompetent BALB/c mice (20.0 g) were used for acute toxicity test[1]
Dosage: 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg, 60 mg/kg
Administration: Intraperitoneal (IP) injection; once daily; each dose administered for 2 consecutive days (total 12 days)
Result: No animal death observed at doses up to 20 mg/kg.
Minimal lethal dose (MLD) and median lethal dose (LD50) were determined based on survival status, with lower toxicity than 10-HCPT (which caused mortality at 5 mg/kg).
Molecular Weight

786.82

Formula

C45H42N2O11
CAS No.
SMILES

O=C(C([C@@H]1CC/C(COC(C2=CC=CC=C2C(OC3=CC4=C(C5=C(N=C4C=C3)C6=CC7=C(C(N6C5)=O)COC([C@]7(O)CC)=O)CC)=O)=O)=C\CC8)=C)O[C@@H]1[C@H]9O[C@@]98C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

IKKβ-IN-7 Related Classifications

  • 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
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IKKβ-IN-73117527-92-8IKKNF-κBBcl-2 FamilyReactive Oxygen Species (ROS)ApoptosisIκB kinaseI kappa B kinase Nuclear factor-κBNuclear factor-kappaBTopo ICT-26 cellsIκBαcolorectal cancerp65IKKβHCT-116 cellsTHLE-2 cellsapoptosisInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
IKKβ-IN-7
Cat. No.:
HY-181837
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.