1. NF-κB Metabolic Enzyme/Protease
  2. Keap1-Nrf2 Endogenous Metabolite
  3. PRL-295

PRL-295 is an orally active inhibitor targeting Keap1-Nrf2 interaction。PRL-295 increases the thermal stability of Keap1 and disrupts its interaction with Nrf2, thereby activating the Nrf2-dependent transcriptional target NAD(P)H:quinone oxidoreductase 1 (NQO1). PRL-295 protects against Acetaminophen (HY-66005)-induced liver injury in mice.

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PRL-295 Chemical Structure

PRL-295 Chemical Structure

CAS No. : 2377770-85-7

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Description

PRL-295 is an orally active inhibitor targeting Keap1-Nrf2 interaction。PRL-295 increases the thermal stability of Keap1 and disrupts its interaction with Nrf2, thereby activating the Nrf2-dependent transcriptional target NAD(P)H:quinone oxidoreductase 1 (NQO1). PRL-295 protects against Acetaminophen (HY-66005)-induced liver injury in mice[1].

In Vitro

PRL-295 increases the thermostability of Keap1 in Keap1-mCherry-expressing U2OS cells lysates (15 μM, 1 h), HL-60 cells lysates (30 μM, 1 h) and HL-60 cells (10 μM, 3 h)[1].
PRL-295 (50 μM, 1 h) disrupts the Keap1-Nrf2 protein complex in single HeLa cell co-expressing sfGFP-Nrf2 and Keap1-mCherry[1].
PRL-295 (approximately 60 nM-10 μM, 48 h) concentration-dependently induces the Nrf2 target NAD(P)H:quinone oxidoreductase 1 (NQO1) in Hepa1c1c7 and ARPE-19 cells[1].

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

In Vivo

PRL-295 (10-50 mg/kg, p.o., 4 times, 24 h apart) dose-dependently increases the thermal stability of Keap1 and activates the Nrf2 transcriptional target NQO1 in murine liver[1].
PRL-295 (25 mg/kg, p.o., 3 days) protects against Acetaminophen (HY-66005)-induced liver injury in C57/BL6 mice[1].

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

Animal Model: 8-week-old male C57/BL6 mice were intraperitoneally Acetaminophen (HY-66005) (300 mg/kg)[1]
Dosage: 25 mg/kg
Administration: Oral gavage (p.o.); once a day, over a period of 3 days
Result: Reduced plasma levels of alanine aminotransferase and glutamine aminotransferase.
Animal Model: Male C57BL/6 wild-type mice[1]
Dosage: 10, 25, 50 mg/kg
Administration: Oral gavage (p.o.); 4 times, 24 h apart
Result: Increased hepatic NQO1 mRNA 2.2-fold or 2.8-fold in a dose-dependent manner at 10 mg/kg or 25 mg/kg, respectively.
Increased NQO1 mRNA moderately (1.5-fold) in kidneys at a dose of 25 mg/kg.
Did not significantly increase mRNA levels of NQO1 in the brain, colon, or lung.
Molecular Weight

639.62

Formula

C27H24F3N3O8S2

CAS No.
SMILES

O=C(CN(S(=O)(C1=CC=C(C=C1)OC)=O)C2=NC=C(N(S(=O)(C3=CC=C(C=C3)OC)=O)CC(F)(F)F)C4=C2C=CC=C4)O

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
PRL-295
Cat. No.:
HY-171035
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