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Art. -Nr.: HY-189671

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PGC-01

PGC-01 is a PROTAC degrader targeting GSDMD, with a DC₅₀ of 3.32 μM in THP-1 cells. PGC-01 mediates CRBN-dependent ubiquitination and proteasomal degradation of full-length GSDMD, blocking pyroptosis at the source. PGC-01 concentration-dependently inhibits Nigericin (HY-127019)-induced macrophage pore formation, cell death, and IL-1β release. PGC-01 can be used for colitis research.
(Pink: GSDMD ligand (HY-189672); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-42773)).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₄₇H₄₉F₂N₇O₇
Molecular Weight:861.93

Speicherung:

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

PGC-01 Chemical Structure

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Preis

Verfügbarkeit

Menge

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

PGC-01 is a PROTAC degrader targeting GSDMD, with a DC₅₀ of 3.32 μM in THP-1 cells. PGC-01 mediates CRBN-dependent ubiquitination and proteasomal degradation of full-length GSDMD, blocking pyroptosis at the source. PGC-01 concentration-dependently inhibits Nigericin (HY-127019)-induced macrophage pore formation, cell death, and IL-1β release. PGC-01 can be used for colitis research^[1]. (Pink: GSDMD ligand (HY-189672); Blue: Cereblon ligand (HY-W087383); Black: linker (HY-42773)).

IC₅₀ & Target

^[1]

GSDMD

3.32 μM (DC₅₀)

Alle PROTACs Isoform-spezifische Produkte anzeigen :

In Vitro

InflammasomeAnti-cancerCytokines and ChemokinesPyroptosis

Inflammasome

Anti-cancer

PGC-01 (0.31-20 μM; 1-48 h) degrades GSDMD in THP-1 cells with a DC₅₀ of 3.32 μM and a D_max of 85%^[1].
PGC-01 (10 μM; 8 h)-induced GSDMD degradation in THP-1 cells requires CRBN binding and a functional ubiquitin-proteasome pathway^[1].

Cytokines and Chemokines

Anti-cancer

Pyroptosis

PGC-01 (5-10 μM; 8 h) inhibits Nigericin (HY-127019)-induced pyroptosis in THP-1 macrophages and suppresses IL-1β release, with an IC₅₀ of 3.22 μM^[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 cells
Concentration:

1, 10, 20 μM (GSDMD degradation screening); 10 μM (time course); 0.31, 0.62, 1.25, 2.5, 5, 10, 20 μM (dose-response at 12 h)
Incubation Time:

1, 2, 4, 8, 12, 24, 48 h (10 μM time course); 12 h (dose-response)
Result:

Degraded GSDMD by 23% at 1 μM, 85% at 10 μM, and 83% at 20 μM.
At 10 μM, GSDMD decreased rapidly to approximately 85% degradation within 8 h, and this degradation was sustained up to 12 h or longer.
In the 12-h dose-response experiment, DC₅₀ = 3.32 μM and D_max = 85%.

Western Blot Analysis^[1]

Cell Line:

THP-1 cells
Concentration:

10 μM
Incubation Time:

8 h
Result:

Co-incubation with Thalidomide (HY-14658) blocked PGC-01-mediated GSDMD degradation.
GSDMD protein levels were restored upon co-incubation with MG132 (HY-13259) or Carfilzomib (HY-10455).

Parmacokinetics

Species	Dose	Route	C_max	T_1/2α	T_1/2β	AUC	CL	MRT	V_ss	V₁
Rat^[1]	2 mg/kg	i.v.	143.5 ng/mL	10.40 min	283.50 min	5691 min·ng/mL	363.31 mL/min/kg	285.86 min	103.33 L/kg	16.36 L/kg

In Vivo

PGC-01 (2-10 mg/kg; rectal administration; daily; for 7 days) dose-dependently alleviates the symptoms and pathological damage of DSS-induced colitis in mice^[1].

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

Animal Model:

C57BL/6J (male; weight 20-22 g; age 6-8 weeks)^[1]
Dosage:

2 mg/kg; 10 mg/kg
Administration:

rectal; daily; for 7 days
Result:

10 mg/kg PGC-01 significantly ameliorated body weight loss, diarrhea, rectal bleeding, colon shortening, and increased spleen weight index.
This dose also mitigated endoscopic mucosal damage, histopathological abnormalities, and intestinal epithelial cell loss.
The 2 mg/kg dose also significantly alleviated these symptoms, but its effects were milder than those of the 10 mg/kg dose.

Related Protocols :

Chemical Information

Molecular Weight 861.93
Formel C₄₇H₄₉F₂N₇O₇
SMILES

O=C(C1=CC=C(C=C1)C(NC2=CC=C(C=C2)N3CCN(CC3)C(CC4=C(C=C(C=C4)F)F)=O)=O)NCCCCCCCCNC5=CC=C6C(N(C(C6=C5)=O)C7CCC(NC7=O)=O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Wang QQ, et al. Discovery and characterization of PGC-01: An effective GSDMD-targeting PROTAC. European journal of medicinal chemistry. 2026 Sep 01;319:119294.

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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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