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製品番号: HY-184797

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Zp17

Zp17 is a PROTAC degrader that targets the STING protein for degradation by recruiting cereblon, with a DC50 of 956 nM in THP-1 cells. Zp17 induces proteasome-dependent STING protein degradation and inhibits the activity of the STING signaling pathway. Zp17 alleviates renal function injury in a mouse model of acute kidney injury induced by Cisplatin (HY-17394). Zp17 exhibits STING-degrading activity in human monocytes and STING-inhibiting activity in mouse macrophage reporter cells. Zp17 can be used for research on inflammation and acute kidney injury.
(Pink: STING Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker (HY-133388)).

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。

分子式: C₃₄H₄₂N₆O₅
分子量:614.73

保管条件:

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

Zp17 構造式

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

Zp17 is a PROTAC degrader that targets the STING protein for degradation by recruiting cereblon, with a DC50 of 956 nM in THP-1 cells. Zp17 induces proteasome-dependent STING protein degradation and inhibits the activity of the STING signaling pathway. Zp17 alleviates renal function injury in a mouse model of acute kidney injury induced by Cisplatin (HY-17394). Zp17 exhibits STING-degrading activity in human monocytes and STING-inhibiting activity in mouse macrophage reporter cells. Zp17 can be used for research on inflammation and acute kidney injury^[1]. (Pink: STING Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker (HY-133388)).

PROTACs アイソフォーム固有の製品をすべて表示 :

CXCR 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 & ChemokinesOthers

Innate Immunity

Zp17 (0.03-20 μM; 2-48 h) potently degrades STING in THP-1 cells via a proteasome-dependent pathway, with a DC₅₀ of 956 nM. It achieves 95% of the maximum degradation rate within 24 h, and this degradation effect persists for at least 48 h^[1].
Zp17 (0.3-20 μM; 1.5-24 h) potently inhibits STING pathway activation in RAW-Lucia cells, with an IC₅₀ of 1.06 μM, and exhibits stronger activity than H151 and SP23^[1].

Innate Immunity

Cytokines & Chemokines

Zp17 (0.3-10 μM; 2-24 h) dose-dependently inhibits MSA-2-induced STING downstream signaling pathway in THP-1 cells, and its effects on reducing pTBK1/pIRF3 levels and pro-inflammatory cytokine gene expression are stronger than those of SP23^[1].

Others

Zp17 (5-40 μM; 48 h) exhibits favorable in vitro safety, showing only extremely low cytotoxicity at concentrations up to 40 μM in THP-1, RAW264.7 and HEK293T cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

THP-1
Concentration:

Zp17 5 μM; MG132 (HY-13259) 0.06-1 μM or 1 μM; Chloroquine (HY-17589A) 10 μM
Incubation Time:

MG132 or chloroquine pretreatment for 1 h; Zp17 treatment for 24 h
Result:

MG132 (HY-13259) concentration-dependently attenuated Zp17-induced STING degradation, whereas Chloroquine (HY-17589A) did not significantly reverse the degradation, supporting a proteasome-dependent degradation mechanism.

Cell Viability Assay^[1]

Cell Line:

THP-1, RAW264.7, HEK293T,
Concentration:

5, 10, 20, 40 μM
Incubation Time:

48 h
Result:

Exhibited minimal cytotoxicity at all tested concentrations, with high cell survival rates even at 40 μM.
Displayed consistently low cytotoxicity.

Real Time qPCR^[1]

Cell Line:

THP-1
Concentration:

1.25, 2.5, 5 μM
Incubation Time:

2 h pretreatment followed by 50 μM MSA-2 (HY-136927) for 4 h
Result:

Concentration-dependently reduced IFN-β, TNF-α, IL-6 and CXCL10 mRNA expression.
Showed strong inhibition of IFN-β, IL-6 and CXCL10 transcription.

体内実験

Renal RegulationCytokines & Chemokines

Renal Regulation

Cytokines & Chemokines

Zp17 (25 mg/kg; i.p.; once daily for 4 consecutive days) significantly alleviates Cisplatin (HY-17394)-induced acute kidney injury in mice, and exhibits excellent histocompatibility in cardiac and hepatic tissues^[1].

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

Animal Model:

C57BL/6 J (male, 8 weeks old, cisplatin-induced acute kidney injury)^[1]
Dosage:

25 mg/kg
Administration:

i.p.; once daily; 4 days (starting 1 hour before cisplatin exposure)
Result:

Reduced cisplatin-induced kidney swelling and pale appearance.
Significantly decreased elevated serum blood urea nitrogen (BUN), creatinine, and uric acid levels.
Reduced elevated serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels to a greater degree than SP23.
Suppressed cisplatin-induced upregulation of renal mRNA levels of pro-inflammatory factors IFNβ, TNFα, and IL6.
Ameliorated cisplatin-induced glomerular injury observed via H&E staining.
Caused no overt pathological damage to heart or liver tissue.

Related Protocols :

化学情報

分子量 614.73
分子式 C₃₄H₄₂N₆O₅
SMILES

O=C(NC1=CNC2=C1C=CC=C2)NCCCCCCCCCCCCNC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O
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

取扱説明書 (2659 KB)

参考文献

[1]. Zhou P, et al. Discovery of indolyl-urea compounds as effective STING PROTAC degraders for the treatment of acute kidney injury. Bioorganic chemistry. 2026 Jun 26;180:110165. [Content Brief]

Calculators

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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.

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MOQ

Minimum order quantity

100 mg

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生物活性
- 製品説明
- 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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Zp17

PROTACs アイソフォーム固有の製品をすべて表示

CXCR 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