hf-1

BHF-177 is a positive allosteric modulator of the GABAB receptor. BHF-177 reduces self-administration of nicotine in animal studies.

CH-5137291 is a pure AR antagonist with AR nuclear translocation inhibition activity. It inhibits castration and prevents the growth of prostate cancer cells.

6-Hydroxyflavone (6-HF) is a noncompetitive inhibitors of cytochrome P450 2C9. It is a flavone, a type of chemical compound. It is reported in leaves of Barleria prionitis Linn. (a common Acanthaceae from India). 6-Hydroxyflavone may have a potential as a therapeutic drug capable for the treatment of anxiety-like disorders.

PF-07238025, a potent branched-chain ketoacid dehydrogenase kinase (BDK) inhibitor with an EC50 of 19 nM, enhances the stability of the BDK-BCKDH core E2 subunit interaction and inhibits the phosphorylation of the E1 subunit. By modulating BDK, which regulates the phosphorylation of BCKDH, a key enzyme in branched-chain amino acid (BCAA) degradation, PF-07238025 indirectly controls the rate-limiting step in BCAA catabolism. Dysregulated BCAA metabolism is implicated in various cardiometabolic disorders such as heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. Notably, PF-07238025 has been shown to ameliorate cardiometabolic endpoints and enhance glucose tolerance in mouse models [1].

PF-07247685, a potent BCKDC kinase (BDK) inhibitor (EC 50 = 2.2 nM), enhances the binding between BDK and the BCKDH E2 core subunit to block E1 phosphorylation. BDK regulation is crucial for BCKDH activity, which manages the rate-limiting step in the catabolism of branched-chain amino acids (BCAA). Dysfunctional BCAA metabolism is linked to various cardiometabolic disorders such as heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 has demonstrated an ability to improve cardiometabolic parameters and glucose tolerance in mice [1].

GRK2 Inhibitor 2 (Compound 8h), with an IC50 of 19 nM for GRK2 and 137 nM for Aurora-A, enhances β-AR-mediated cAMP accumulation in GRK2-overexpressing HEK293 cells. It is utilized in congestive heart failure (HF) research [1].

Human Follicular Gonadotropin Releasing Peptide (hF-GRP) is a hormonal peptide that, in vitro, can induce the secretion of pituitary luteinizing hormone (LH) and follicle-stimulating hormone (FSH) [1] [2].

Compound 43, also known as β-AR antagonist 2, is an antagonist of β-AR with an IC50 of 0.17 μM. It inhibits the growth of mouse A549 xenograft tumors and demonstrates cardioprotective efficacy against DOX-induced heart failure in C57 mice [1].