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Cat. No.: 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)).

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

화학식: C₃₄H₄₂N₆O₅
분자량:614.73

보관:

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

Zp17 Chemical Structure

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
- In Vitro
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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)).

All PROTACs Isoforms :

All CXCR Isoforms :

All TNF Receptor Isoforms :

In Vitro

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.

In Vivo

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 :

Chemical Information

분자량 614.73
화학식 C₃₄H₄₂N₆O₅
SMILES

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

Handling Instructions (2659 KB)

References

[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

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

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

견적 받기

Amount: USD 0.00

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

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

상품명:
CAS No.:
Species:
Purity:
수량:

Zp17

All PROTACs Isoforms

All CXCR Isoforms

All TNF Receptor Isoforms