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製品番号: 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)).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 3071170-20-9
分子式: C₂₇H₂₈N₄O₈
分子量:536.53

保管条件:

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

Data Sheet (281 KB)

FP-4 構造式

CAS 番号: 3071170-20-9

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

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

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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

PROTACs アイソフォーム固有の製品をすべて表示 :

Toll-like Receptor (TLR) アイソフォーム固有の製品をすべて表示 :

NF-κB アイソフォーム固有の製品をすべて表示 :

TNF Receptor アイソフォーム固有の製品をすべて表示 :

体外実験

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.

体内実験

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 :

化学情報

CAS 番号 3071170-20-9
分子量 536.53
分子式 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
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (281 KB)
COA (2659 KB)
元素分析報告書 (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)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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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生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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FP-4

PROTACs アイソフォーム固有の製品をすべて表示

Toll-like Receptor (TLR) アイソフォーム固有の製品をすべて表示

NF-κB アイソフォーム固有の製品をすべて表示

TNF Receptor アイソフォーム固有の製品をすべて表示

生物活性

製品説明

IC₅₀ & Target

体外実験

体内実験

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

Bioz

Keywords

最近チェックした製品

FP-4

PROTACs アイソフォーム固有の製品をすべて表示

Toll-like Receptor (TLR) アイソフォーム固有の製品をすべて表示

NF-κB アイソフォーム固有の製品をすべて表示

TNF Receptor アイソフォーム固有の製品をすべて表示

生物活性

製品説明

IC50 & Target

体外実験

体内実験

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

FP-4 関連分類

HY-188344 関連分類

Bioz

Keywords

最近チェックした製品

IC₅₀ & Target