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Art. -Nr.: HY-188344

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FP-4

FP-4 is a PROTAC degrader targeting TLR4, with a DC₅₀ of 2.5 μM. FP-4 mediates CRBN-dependent TLR4 ubiquitination and proteasomal degradation through the TLR4/MD-2 interface, and inhibits TLR4/MyD88-NF-κB inflammatory signaling and the downstream expression of TNF-α, ICAM-1, and VCAM-1. FP-4 reduces intracellular reactive oxygen species (ROS) and promotes endothelial cell migration. FP-4 ameliorates endothelial injury in LPS-treated zebrafish larvae and restores the number of intersegmental vessels. FP-4 can be used for research on vascular endothelial injury and LPS-induced vascular endothelial injury.
(Pink: TLR4 ligand (HY-N0060); Blue: Cereblon ligand (HY-41547); Black: linker (HY-140208)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 3071170-20-9
Formel: C₂₇H₂₈N₄O₈
Molecular Weight:536.53

Speicherung:

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

Data Sheet (281 KB)

FP-4 Chemical Structure

CAS. Nr.: 3071170-20-9

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Preis

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

FP-4 is a PROTAC degrader targeting TLR4, with a DC₅₀ of 2.5 μM. FP-4 mediates CRBN-dependent TLR4 ubiquitination and proteasomal degradation through the TLR4/MD-2 interface, and inhibits TLR4/MyD88-NF-κB inflammatory signaling and the downstream expression of TNF-α, ICAM-1, and VCAM-1. FP-4 reduces intracellular reactive oxygen species (ROS) and promotes endothelial cell migration. FP-4 ameliorates endothelial injury in LPS-treated zebrafish larvae and restores the number of intersegmental vessels. FP-4 can be used for research on vascular endothelial injury and LPS-induced vascular endothelial injury^[1]. (Pink: TLR4 ligand (HY-N0060); Blue: Cereblon ligand (HY-41547); Black: linker (HY-140208)).

IC₅₀ & Target

^[1]

TLR4

2.5 μM (DC₅₀)

MD-2

NF-κB

MyD88

TNF-α

ICAM-1

VCAM-1

Alle PROTACs Isoform-spezifische Produkte anzeigen :

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen :

Alle NF-κB Isoform-spezifische Produkte anzeigen :

Alle TNF Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Innate ImmunityCytokines and ChemokinesLysosomal MetabolismLocal Vascular RegulationOxidative StressOthers

Innate Immunity

FP-4 (10 μM; 24 h) produces the strongest TLR4 degradation in LPS-stimulated HUVECs^[1].
FP-4 (10 μM; 24 h) suppresses TLR4/MyD88-NF-κB pathway proteins and adhesion molecules in LPS-stimulated HUVECs^[1].
FP-4 (0.1-40 μM; 24 h) degrades TLR4 in LPS-stimulated HUVECs with DC₅₀ = 2.5 μM and D_max = 50.4%^[1].
FP-4 (10 μM; 2-48 h) degrades TLR4 in LPS-stimulated HUVECs beginning at 6 h and peaking at 48 h^[1].
FP-4 (10 μM)-induced TLR4 degradation in HUVECs is CRBN-dependent^[1].
FP-4 (0-50 μM) protects TLR4 from Pronase E digestion in HUVEC lysates in a concentration-dependent manner^[1].

Innate Immunity

Cytokines and Chemokines

FP-4 (10 μM; 24 h) reduces IL-6, IL-1β, and TNF-α mRNA in LPS-stimulated HUVECs^[1].

Innate Immunity

Lysosomal Metabolism

FP-4 (10 μM)-induced TLR4 degradation in HUVECs requires proteasome and Cullin-RING neddylation pathways and is not mediated by endolysosomal degradation^[1].

Local Vascular Regulation

FP-4 (0-48 h) restores LPS-impaired HUVEC migration in the scratch-wound-healing assay, with significant improvement at 12, 24, and 48 h^[1].

Oxidative Stress

FP-4 (10 μM; 24 h) lowers intracellular ROS in LPS-stimulated HUVECs^[1].

Others

FP-4 (0.00001-100 μM) inhibits HUVEC viability in the CCK-8 assay with IC₅₀ = 31.57 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:

HUVECs
Concentration:

10 μM
Incubation Time:

24 h
Result:

Had the strongest TLR4-degrading activity in this screening and significantly reduced TLR4 levels compared with the model group.\nSignificantly reduced TLR4, MyD88, p-p65/p65, TNF-α, ICAM-1, and VCAM-1 levels compared with the model group.

Real Time qPCR^[1]

Cell Line:

HUVECs
Concentration:

10 μM
Incubation Time:

24 h
Result:

Reduced IL-6, IL-1β, and TNF-α mRNA expression compared with the model group.

In Vivo

Innate ImmunityCytokines & ChemokinesLocal Vascular Regulation

Innate Immunity

Cytokines & Chemokines

Local Vascular Regulation

FP-4 (0.5-2 μM; immersion; once at 12 h after initial LPS exposure; 24 h) ameliorates LPS-induced vascular endothelial injury in zebrafish larvae by increasing endothelial fluorescence and ISV number and by suppressing TLR4/MyD88/NF-κB signaling^[1].

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

Animal Model:

Tg(fli:EGFP) (transgenic larvae)^[1]
Dosage:

0.5 μM (FP-4-L); 1 μM (FP-4-M); 2 μM (FP-4-H)
Administration:

immersion; once at 12 h after initial LPS exposure; 24 h
Result:

At 0.5 μM, endothelial fluorescence showed little difference from the model group.
At 1 μM and 2 μM, endothelial-cell fluorescence intensity increased relative to the model group.
ISV number was restored in a dose-dependent manner, with the 2 μM group showing efficacy comparable to the Dexamethasone (HY-14648) positive control.
In zebrafish, TLR4, MyD88, TNF-α, p-p65/p65, ICAM-1, and VCAM-1 protein levels were reduced relative to the model group.

Related Protocols :

Chemical Information

CAS. Nr. 3071170-20-9
Molecular Weight 536.53
Formel C₂₇H₂₈N₄O₈
SMILES

O=C(NCCOCCNC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)/C=C/C4=CC=C(O)C(OC)=C4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 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)

Verweise

[1]. Wang X, et al. Enhancing Natural Product Therapy with PROTACs: Targeted Degradation of TLR4 Confers Potent Endothelial Protection. ACS Med Chem Lett. 2026.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

MOQ

Minimum order quantity

100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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Art. -Nr.:
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FP-4

Alle PROTACs Isoform-spezifische Produkte anzeigen

Alle Toll-like Receptor (TLR) Isoform-spezifische Produkte anzeigen

Alle NF-κB Isoform-spezifische Produkte anzeigen

Alle TNF Receptor Isoform-spezifische Produkte anzeigen