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Cat. No.: 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)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 3071170-20-9
화학식: C₂₇H₂₈N₄O₈
분자량:536.53

보관:

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

Data Sheet (281 KB)

FP-4 Chemical Structure

CAS No.: 3071170-20-9

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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

All PROTACs Isoforms :

All Toll-like Receptor (TLR) Isoforms :

All NF-κB Isoforms :

All TNF Receptor Isoforms :

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 No. 3071170-20-9
분자량 536.53
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Select Batch:

Purity: 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)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

상품명:
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Species:
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FP-4

All PROTACs Isoforms

All Toll-like Receptor (TLR) Isoforms

All NF-κB Isoforms

All TNF Receptor Isoforms