2. NF-κB PI3K/Akt/mTOR Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. IKK Akt Apoptosis PI3K NF-κB CDK Caspase PARP
  4. LIB3S0280

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.

LIB3S0280

LIB3S0280 Chemical Structure

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Based on 1 publication(s) in Google Scholar

LIB3S0280 Related Antibodies

Top Publications Citing Use of Products

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IKK-α IKK-β IKK IKKε TBK1

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Akt Akt1 Akt2 Akt3

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

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[1].

IC50 & Target[1]

TBK1

493.9 nM (IC50)

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.

LIB3S0280 Related Antibodies

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.
Molecular Weight

460.91

Formula

C22H25ClN4O5
Appearance

Solid

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1696 mL 10.8481 mL 21.6962 mL
5 mM 0.4339 mL 2.1696 mL 4.3392 mL
View the Complete Stock Solution Preparation Table

* 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.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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LIB3S0280 Related Classifications

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:

LIB3S0280IKKAktApoptosisPI3KNF-κBCDKCaspasePARPIκB kinaseI kappa B kinase PKBProtein kinase BPhosphoinositide 3-kinaseNuclear factor-κBNuclear factor-kappaBCyclin dependent kinasepoly ADP ribose polymeraseTBK1pancreatic cancerPDACPI3K/AKTG2/M arrestapoptosiscellular senescenceInhibitorinhibitorinhibit

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