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Art. -Nr.: HY-184204

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Keap1-p-p62-IN-1

Keap1-p-p62-IN-1 is a potent and selective Keap1-p-p62 inhibitor with an IC₅₀ of 0.11 μM. Keap1-p-p62-IN-1 shows 18.73-fold selectivity over Keap1-Nrf2 interaction. Keap1-p-p62-IN-1 normalizes Nrf2 ubiquitination, sensitizes cells to Sorafenib (HY-10201)-induced ferroptosis. Keap1-p-p62-IN-1 can be used for the research of p62 aberrant hepatocellular carcinoma.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₃₃H₃₅N₅O₅S
Molecular Weight:613.73

Speicherung:

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

Keap1-p-p62-IN-1 Chemical Structure

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

Biologische Aktivität

Beschreibung

In Vitro

Keap1-p-p62-IN-1 (compound 13) (0.625-5 μM; 48 h) induces ferroptosis in p62-aberrant Huh-1 HCC cells in a Keap1-dependent manner, as evidenced by concentration-dependent downregulation of ferroptosis-related proteins/genes, GSH depletion, iron overload, and increased lipid peroxidation (MDA, 4-HNE, Liperfluo)^[1].
Keap1-p-p62-IN-1 (0.03-5 μM; 24-72 h) selectively disrupts Keap1-p-p62 PPI in a dose- and time-dependent manner, causing increased Nrf2 ubiquitination in HEK293T and Huh-1 cells[1].
Keap1-p-p62-IN-1 (0.625-5 μM; 24-72 h) specifically inhibits Nrf2 activity in tumor
cells (Huh-1; Huh-7; AML 12; A549) with p62-dependent overactivation of Nrf2[1].
Keap1-p-p62-IN-1 (1.25-10 μM; 48 h) induces ferroptosis in specific HCC cells[1].

Keap1-p-p62-IN-1 (1.25-10 μM; 14 days) dose-dependently inhibits colony formation in Huh-1 HCC cells^[1].
Keap1-p-p62-IN-1 (1.25-10 μM; 24-72 h) selectively induces ferroptosis in Huh-1 HCC cells with p62-dependent overactivation of Nrf2^[1].
Keap1-p-p62-IN-1 (2.5-10 μM; 24 h-14 days)sensitizes Huh-1 cells bearing p62-mediated Nrf2 hyper-activation to Sorafenib by cooperatively inducing ferroptosis^[1].

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

Western Blot Analysis^[1]

Cell Line:

HEK293T, Huh-1 cells
Concentration:

0.03; 0.1; 0.3 μM (HEK293T), 2.5; 5 μM (Huh-1 cells)
Incubation Time:

24; 36; 48; 72 h
Result:

Effectively interfered with the Keap1−p-p62 interaction in a concentration-dependent manner without affecting the Keap1-Nrf2 interaction.
Barely disrupted the binding of both ETGE and DLGex motifs to Keap1.
Recovered the ability of Keap1 to interact with Nrf2 because of the elevated level of p62-free Keap1, leading to a decrease in the Nrf2 protein level of total cell lysate.
Elevated the accumulation of ubiquitinated Nrf2 upon MG132 (HY-13259) treatment.
Caused a time-dependent reduction in Nrf2 protein in both the nucleus and cytoplasm.
Showed a remarkable upregulation of the protein level of Keap1.

Real Time qPCR^[1]

Cell Line:

Huh-1 cells
Concentration:

2.5; 5 μM
Incubation Time:

24; 36; 48; 72 h
Result:

Had no significant effect on the transcription level of NFE2L2 (encoding Nrf2 protein) in Huh-1 cells.
Concentration-dependently reduced mRNA levels of SLC7A11, FTL, and GPX4.

Western Blot Analysis^[1]

Cell Line:

Huh-1; Huh-7; AML 12; A549
Concentration:

0.625; 1.25; 2.5; 5 μM
Incubation Time:

24; 36; 48; 72 h
Result:

Decreased the protein levels of Nrf2 and its downstream genes in a concentration- and time-dependent manner, including gluta-
mate-cysteine ligase catalytic subunit (GCLC), NAD(P)H dehydrogenase (quinone) 1 (NQO1), and heme oxygenase-1 (HO-1).
Downregulate the protein levels of these ferroptosis-related genes in a concentration-dependent manner.

Real Time qPCR^[1]

Cell Line:

Huh-1; Huh-7; AML 12; A549
Concentration:

0.625; 1.25; 2.5; 5 μM
Incubation Time:

24; 36; 48; 72 h
Result:

Significantly downregulated the
mRNA levels of Nrf2-regulated genes GCLC, NQO1, and HO-1, with IC₅₀ values of 4.62 μM, 4.24 μM, and 3.51 μM, respectively.
Induced a time-dependent decrease in the mRNA expression of GCLC, NQO1, and HO-1.

Cell Viability Assay^[1]

Cell Line:

Huh-1 HCC cells
Concentration:

1.25; 2.5; 5; 10 μM
Incubation Time:

48 h
Result:

Decreased cell viability in a dose-dependent manner.
The growth inhibition induced by 13 in Huh-1 cells was mitigated by Fer-1 (5 μM).

Cell Proliferation Assay^[1]

Cell Line:

Huh-1 HCC cells
Concentration:

1.25; 2.5; 5; 10 μM
Incubation Time:

14 days
Result:

Inhibited colony formation of Huh-1 HCC cells in a dose-dependent manner.

Parmacokinetics

Species	Dose	Route	C_max	T_max	AUC_0-∞	T_1/2	V_z	CL	F
Rat^[1]	5 mg/kg	i.v.	5758.67 ng/mL	0.02 h	2111.50 ng·h/mL	2.82 h	10593.60 mL/kg	2825.97 mL/h/kg	/
Rat^[1]	25 mg/kg	i.p.	2502.67 ng/mL	0.50 h	6022.41	3.08 h	19131.56 mL/kg	4279.65 mL/h/kg	57.04 %

In Vivo

Keap1-p-p62-IN-1 (compound 13) (20-40 mg/kg; i.p.; daily; 28 days) inhibits tumor growth in p62 aberrant Huh-1 xenograft mice, with reduced Nrf2 pathway activity and induction of ferroptosis-related changes in tumor tissue^[1].

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

Animal Model:

BALB/c nude mice (female) subcutaneously inoculated with Huh-1 cells^[1]
Dosage:

20; 40 mg/kg
Administration:

i.p.; daily; 28 days
Result:

Achieved a tumor growth inhibition (TGI) rate of 11.1% at 20 mg/kg.
Achieved a TGI of 30.1% at 40 mg/kg.
Decreased protein levels of Nrf2, glutamate-cysteine ligase catalytic subunit (GCLC), solute carrier family 7 member 11 (SLC7A11), and glutathione peroxidase 4 (GPX4) in tumor tissues.
Reduced glutathione (GSH) levels in tumor tissues.
Increased ferrous iron (Fe²⁺) levels in tumor tissues.
Increased malondialdehyde (MDA) levels in tumor tissues.
Caused no significant body weight loss or histopathological lesions in major organs.

Chemical Information

Molecular Weight 613.73
Formel C₃₃H₃₅N₅O₅S
SMILES

CC1=CC(C)=C(S(N(C2=C(C=CC=C3)C3=C(OC(C4=CC=C(C(C)(C)C)C=C4)C(O)=O)C=C2)CC5=NN=NN5)(=O)=O)C(C)=C1
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]. Zhao Z, et al. Discovery of a Biased Kelch-like ECH-Associated Protein 1-p62 (Keap1-p62) Protein-Protein Interaction (PPI) Inhibitor for the Management of p62 Aberrant Hepatocellular Carcinoma. J Med Chem. 2026 Jun 11;69(11):13141-13164. [Content Brief]

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.

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100 mg

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