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: Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker (HY-133388)).
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- Formule: C34H42N6O5
- Masse moléculaire:614.73
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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].
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].
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.
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Cell Line:THP-1
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Concentration:Zp17 5 μM; MG132 (HY-13259) 0.06-1 μM or 1 μM; Chloroquine (HY-17589A) 10 μM
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Incubation Time:MG132 or chloroquine pretreatment for 1 h; Zp17 treatment for 24 h
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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.
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Cell Line:THP-1, RAW264.7, HEK293T,
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Concentration:5, 10, 20, 40 μM
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Incubation Time:48 h
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Result:Exhibited minimal cytotoxicity at all tested concentrations, with high cell survival rates even at 40 μM.
Displayed consistently low cytotoxicity.
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Cell Line:THP-1
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Concentration:1.25, 2.5, 5 μM
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Incubation Time:2 h pretreatment followed by 50 μM MSA-2 (HY-136927) for 4 h
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 J (male, 8 weeks old, cisplatin-induced acute kidney injury)[1]
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Dosage:25 mg/kg
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Administration:i.p.; once daily; 4 days (starting 1 hour before cisplatin exposure)
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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.
Chemical Information
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Masse moléculaire 614.73
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Formule C34H42N6O5
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SMILES
O=C(NC1=CNC2=C1C=CC=C2)NCCCCCCCCCCCCNC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Zp17 Related Classifications
HY-184797 Related Classifications
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