Cat. No.: HY-172620

LIB3S0280

Customer Review

Based on 1 Customer Validation

LIB3S0280 is a potent TBK1 inhibitor with an IC₅₀ value of 493.9 nM. LIB3S0280 exhibits better anticancer effects in pancreatic cancer cell lines with high TBK1 expression. LIB3S0280 inhibits TBK1 downstream signaling pathways, including PI3K/AKT and NF-κB. LIB3S0280 induces G2/M arrest, apoptosis and cellular senescence. LIB3S0280 can be used for pancreatic ductal adenocarcinoma (PDAC) research.

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

Purity: 99.89%
Formula: C₂₂H₂₅ClN₄O₅
Molecular Weight:460.91

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

LIB3S0280 Chemical Structure

Size

Price

Stock

Quantity

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

TBK1

493.9 nM (IC₅₀)

All IKK Isoforms :

All Akt Isoforms :

All PI3K Isoforms :

All NF-κB Isoforms :

All CDK Isoforms :

All Caspase Isoforms :

All PARP Isoforms :

In Vitro

LIB3S0280 (72-96 h) shows significant inhibition against high TBK1-expressing pancreatic cancer cell lines with the GI₅₀ values of 2.24 μM (MIA PaCa-2) and 4.71 μM (PANC-1) , and IC₅₀ values of 6.64 μM (MIA PaCa-2) and 10.98 μM (PANC-1) at 96 h^[1].
LIB3S0280 (10-20 μM, 3 h) inhibits TBK1 downstream signaling, including the PI3K/AKT and NF-κB pathways, by effectively reducing the phosphorylation of its key targets, AKT (Ser473) and IκBα, in MIA PaCa-2 and PANC-1 cells^[1].
LIB3S0280 (10-20 μM, 48-96 h) induces G₂/M arrest, apoptosis, and cellular senescence in pancreatic cancer cells (MIA PaCa-2 and PANC-1) by modulating key regulators like p-cdc2, p-MPM2, cyclin B1, and p21^[1].

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

Western Blot Analysis^[1]

Cell Line:

MIA PaCa-2 and PANC-1 cells
Concentration:

10 and 20 μM
Incubation Time:

3, 48, 72 and 96 h
Result:

Decreased the phosphorylation of IκBα in a dose-dependent manner.
Reduced the phosphorylation level of AKT on the ser473 site.
Increased p21 levels from 48 h to 96 h.

Cell Viability Assay^[1]

Cell Line:

MIA PaCa-2, PANC-1, and SW1990 cells
Concentration:

10 μM
Incubation Time:

72 and 96 h
Result:

Significantly inhibited cell proliferation and cell viability in a concentration-dependent manner, with efficacy comparable to BX-795 (HY-10514).
Demonstrated greater potency against the MIA PaCa-2 cell line.
Showed no inhibition in SW1990 cells.

Cell Cycle Analysis^[1]

Cell Line:

MIA PaCa-2 and PANC-1 cells
Concentration:

10 and 20 μM
Incubation Time:

48, 72 and 96 h
Result:

Significantly increased the G2/M phase population and slightly increased the sub-G1 population at 48 h.
Downregulated the expression level of p-MPM2, and upregulated p-cdc2 (tyr15) and cyclin B1 levels after 48 h.
Slightly decreased the G2/M population but increased sub-G1 population at 72 h, compared to 48 h.
Exhibited a significant increase in the sub-G1 population and a further decrease in the G2/M phase at 96 h.

Apoptosis Analysis^[1]

Cell Line:

MIA PaCa-2 and PANC-1 cells
Concentration:

10 and 20 μM
Incubation Time:

48, 72 and 96 h
Result:

Induced apoptosis at 72-96 h.
Slightly increased cleaved PARP and cleaved caspase 3 levels after 48 h.
Increased the granularity in MIA PaCa-2 and PANC-1 cells at 48 h, 72 h, and 96 h.
Induced senescence in MIA PaCa-2 and PANC-1 cells.

Chemical Information

Appearance Solid
Molecular Weight 460.91
Formula C₂₂H₂₅ClN₄O₅
Color Off-white to gray
SMILES

OC1=C(OC)C=C(CCNC2=NC(NC3=CC(OC)=C(OC)C(OC)=C3)=NC=C2Cl)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (108.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1696 mL

10.8481 mL

21.6962 mL

5 mM

0.4339 mL

2.1696 mL

4.3392 mL

10 mM

0.2170 mL

1.0848 mL

2.1696 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

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

Mass Mass

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Molecular Weight Molecular Weight

Dilution Calculator

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wan-Hsi Shih, et al. Discovery of novel TANK-Binding Kinase 1 (TBK1) inhibitor against pancreatic ductal adenocarcinoma. Int J Biol Macromol. 2024 Dec;283(Pt 1):137296. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1696 mL	10.8481 mL	21.6962 mL	54.2405 mL
	5 mM	0.4339 mL	2.1696 mL	4.3392 mL	10.8481 mL
	10 mM	0.2170 mL	1.0848 mL	2.1696 mL	5.4241 mL
	15 mM	0.1446 mL	0.7232 mL	1.4464 mL	3.6160 mL
	20 mM	0.1085 mL	0.5424 mL	1.0848 mL	2.7120 mL
	25 mM	0.0868 mL	0.4339 mL	0.8678 mL	2.1696 mL
	30 mM	0.0723 mL	0.3616 mL	0.7232 mL	1.8080 mL
	40 mM	0.0542 mL	0.2712 mL	0.5424 mL	1.3560 mL
	50 mM	0.0434 mL	0.2170 mL	0.4339 mL	1.0848 mL
	60 mM	0.0362 mL	0.1808 mL	0.3616 mL	0.9040 mL
	80 mM	0.0271 mL	0.1356 mL	0.2712 mL	0.6780 mL
	100 mM	0.0217 mL	0.1085 mL	0.2170 mL	0.5424 mL

Keywords

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LIB3S0280

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

NF-κB Signaling Compound Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Antioxidant Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Pyroptosis Compound Library

Cytoskeleton Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Mitochondria-Targeted Compound Library

Transcription Factor-Targeted Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Radioprotector Library

Mitophagy Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Lactylation Compound Library

All IKK Isoforms

All Akt Isoforms

All PI3K Isoforms

All NF-κB Isoforms

All CDK Isoforms

All Caspase Isoforms

All PARP Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

LIB3S0280 Related Classifications

Cat. No.: HY-172620