Startseite>>Signaling Pathways>> Proteases>> Endogenous Metabolite>>PF-07238025

PF-07238025

Katalog-Nr.GC71322

PF-07238025 ist ein BCKDC-Kinase (BDK)-Hemmer (EC50=19 nM).

Products are for research use only. Not for human use. We do not sell to patients.

PF-07238025 Chemische Struktur

Größe Preis Lagerbestand Menge
1 mg
167,00 $
Auf Lager
5 mg
333,00 $
Auf Lager
10 mg
571,00 $
Auf Lager

Tel:(909) 407-4943 Email: sales@glpbio.com


Kundenbewertungen

Basiert auf Kundenrezensionen.

  • GlpBio Citations

    GlpBio Citations
  • Bioactive Compounds Premium Provider

    Bioactive Compounds Premium Provider

Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents
PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM). PF-07238025 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice.

PF-07238025 (0.2-6 μM; 48 h) reduces pBCKDH in a dose-dependent manner in Hek293 cells, and increases BDK accumulation by 50%[1].

PF-07238025 (20 mg/kg, 100 mg/kg; 8 weeks) reduces glucose excursion after 2 days in HFD-fed mice, and leads significant reduction in both BCAAs and BCKAs by day 7[1].

References:
[1]. Roth Flach RJ, et al. Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels. Nat Commun. 2023 Aug 9;14(1):4812.

Bewertungen

Review for PF-07238025

Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%
Review for PF-07238025

GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.

Required fields are marked with *

You may receive emails regarding this submission. Any emails will include the ability to opt-out of future communications.