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Cat. No.: HY-150111

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IKKβ-IN-2

IKKβ-IN-2 is an orally effective IκB kinase β (IKKβ) inhibitor. IKKβ-IN-2 inhibits the activity of IKKβ, thereby blocking TNFα-induced downstream NF-κB pathway activation and transcription, thus exerting inhibitory effects on inflammation and tumor growth. IKKβ-IN-2 can be used for research on colon cancer and pancreatic cancer.

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

CAS No.: 2345648-37-3
Formula: C₁₉H₁₄BrFN₆O
Molecular Weight:441.26

Storage:

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

IKKβ-IN-2 Chemical Structure

CAS No.: 2345648-37-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

IKKβ

Mcl-1

All IKK Isoforms :

All Bcl-2 Family Isoforms :

All PARP Isoforms :

All NF-κB Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	GI₅₀	3.8 μM	Cell-based growth inhibition against human HCT116 cells assessed as GI50. Cell-based growth inhibition against human HCT116 cells assessed as GI50.	WO2019109069A1
SW-620	GI₅₀	8.4 μM	Cell-based growth inhibition against human SW620 cells assessed as GI50. Cell-based growth inhibition against human SW620 cells assessed as GI50.	WO2019109069A1
HT-29	GI₅₀	3.1 μM	Cell-based growth inhibition against human HT29 cells assessed as GI50. Cell-based growth inhibition against human HT29 cells assessed as GI50.	WO2019109069A1
DLD-1	GI₅₀	8.4 μM	Cell-based growth inhibition against human DLD1 cells assessed as GI50. Cell-based growth inhibition against human DLD1 cells assessed as GI50.	WO2019109069A1
MIA PaCa-2	GI₅₀	3.2 μM	Cell-based growth inhibition against human MiaPaCa2 cells assessed as GI50. Cell-based growth inhibition against human MiaPaCa2 cells assessed as GI50.	WO2019109069A1
ASPC1	GI₅₀	7.2 μM	Cell-based growth inhibition against human AsPC1 cells assessed as GI50. Cell-based growth inhibition against human AsPC1 cells assessed as GI50.	WO2019109069A1

In Vitro

Anti-cancerApoptosisOthers

Anti-cancer

IKKβ-IN-2 (compound 39-100) inhibits the growth of HCT116, SW620, HT29, DLD1, MiaPaCa2, AsPC1, Suit2, and S2013 cells with GI₅₀ values of 3.1-8.4 µM^[1].

Apoptosis

IKKβ-IN-2 (5-20 μM) dose-dependently decreased the phosphorylation level of IκBα (p-IκBα), downregulated the anti-apoptotic protein Mcl-1, and induced PARP cleavage in cells in vitro^[1].

Others

IKKβ-IN-2 inhibits TNFα-induced NFκB transcriptional activity in cell-based experiments with an inhibition rate of 83.8%^[1].

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

Parmacokinetics

Species	Dose	Route	C₀	AUC_last	AUC_0-∞	T_1/2	CL/F	MRT	V_ss	T_max	C_max	Bioavailability
Mice^[1]	1 mg/kg	i.v.	709.9 ng/mL	594.7 ng·h/mL	597.5 ng·h/mL	3.9 h	1.67 L/h/kg	1.4 h	2.4 L/kg	/	/	/
Mice^[1]	10 mg/kg	p.o.	/	12413.4 ng·h/mL	12425.9 ng·h/mL	2.35 h	0.80 L/h/kg	3.9 h	/	2.0 h	2328.3 ng/mL	208 %

In Vivo

Anti-cancer

IKKβ-IN-2 (compound 39-100) (40 mg/kg; 2 weeks) significantly inhibited colon cancer tumor growth in the HCT116 colon cancer subcutaneous xenograft mouse model^[1].
IKKβ-IN-2 (40 mg/kg; p.o.; once daily; 4 weeks) reduced tumor volume and decreased tumor mass in a syngeneic orthotopic pancreatic cancer mouse model^[1].

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

Animal Model:

syngeneic orthotopic pancreatic cancer model in mice^[1]
Dosage:

40 mg/kg
Administration:

p.o.; once daily; 4 weeks
Result:

Visibly reduced the final tumor volume and tumor mass compared to the control group, demonstrating anti-pancreatic tumor efficacy in an orthotopic setting.

Related Protocols :

Chemical Information

CAS No. 2345648-37-3
Molecular Weight 441.26
Formula C₁₉H₁₄BrFN₆O
SMILES

O=C(NC1=CC=C(F)C(Br)=C1)NC=2C=CC=3N=CC(=NC3C2)C=4C=NN(C4)C
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

Handling Instructions (2659 KB)

References

[1]. Amarnath Natarajan, et al. Quinoxaline urea inhibitors of IKK-beta and NF-kB. WO2019109069A1. WIPO. 2019-06-06.

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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IKKβ-IN-2

All IKK Isoforms

All Bcl-2 Family Isoforms

All PARP Isoforms

All NF-κB Isoforms