bh4

2,4-Diamino-6-hydroxypyrimidine (DAHP) (DAHP) is a selective, specific inhibitor of GTP cyclohydrolase I, the rate limiting step for de novo pterin synthesis

Tetrahydrobiopterin (BH4) is a cofactor for aromatic amino acid hydroxylases and an essential cofactor for nitric oxide synthase (NOS), which is used in the study of endothelial dysfunction such as hypertension, hypercholesterolemia, and diabetes.

TAT-BH4 (Bcl-xL), primarily localized at the mitochondria, inhibits apoptotic cell death. This compound comprises an N-terminal eosin-labeled cysteine and the protein transduction domain of the HIV TAT protein (amino acids 49 to 57), fused to the Bcl-xL BH4 peptide. It serves as a tool for research into diseases characterized by accelerated apoptosis [1].

TAT-BH4 (Bcl-xL) TFA, primarily localized at the mitochondria, inhibits apoptotic cell death. This compound comprises an eosin-labeled cysteine at the N-terminal and the protein transduction domain from the HIV TAT protein (amino acids 49 to 57), fused to the Bcl-xL BH4 peptide. It is utilized in research concerning diseases associated with accelerated apoptosis [1].

SPR inhibitor 3 is an effective sepiapterin reductase inhibitor. SPR inhibitor 3 decreases neuropathic and inflammatory pain through a reduction of BH4 levels. SPR inhibitor 3 shows a high binding affinity to human SPR in a cell-free assay (IC50=74 nM) an

(Rac)-BDA-366 (example 2) is the racemate of BDA-366, a potent Bcl-2 antagonist with a Ki of 3.3 nM. It shows high affinity and selectivity for the Bcl-2-BH4 domain. BDA-366 induces a conformational change in Bcl-2, neutralizing its anti-apoptotic function and converting Bcl-2 from a survival molecule into a cell death inducer. Additionally, BDA-366 can inhibit the growth of lung cancer cells.

Sapropterin is a naturally occurring essential cofactor of the three aromatic amino acid hydroxylase enzymes, used in the degradation of amino acid phenylalanine and in the biosynthesis of dopamine, epinephrine, melatonin, norepinephrine, neurotransmitter

L-Sepiapterin, also known as Sepiapterin, is a precursor compound crucial for the production of tetrahydrobiopterin (BH4), which serves as a coenzyme for endothelial nitric oxide synthase (eNOS). This compound demonstrates its efficacy by improving endothelial dysfunction in small mesenteric arteries from db/db mice and promoting angiogenesis. Moreover, L-Sepiapterin exerts inhibitory effects on cellular proliferation and migration in ovarian cancer cells through the down-regulation of p70S6K-dependent vascular endothelial growth factor receptor-2 (VEGFR-2) expression[1][2].

BDA-366, a potent Bcl2 antagonist, selectively binds the Bcl2-BH4 domain with high affinity (Ki = 3.3 nM), inducing a conformational change that nullifies its antiapoptotic function, thereby transforming it into a pro-apoptotic entity. This compound effectively suppresses lung cancer cell growth[1].

Sapropterin dihydrochloride (6R-BH4 dihydrochloride) is phenylalanine hydroxylase agonist that is approved for the treatment of BH4 responsive PKU.

CYD-2-88 (BDA-366 analog) is an analog of BDA-366 (Bcl2 BH4 antagonist). Administered through intraperitoneal injection at a dosage of 20 mg kg, CYD-2-88 effectively inhibits tumor growth in mice with NSCLC H460 xenografts.

6-(L-1,2,3-Trihydroxybutyl)-pterin is a derivative of L-biopterin and represents an oxidized form of tetrahydro-L-biopterin (BH4) as well as D-biopterin. Concurrent administration of 6-(L-1,2,3-Trihydroxybutyl)-pterin (0.5%) with the carcinogen 4-dimethylaminoazobenzene can reduce the incidence of liver tumors in rats induced by 4-dimethylaminoazobenzene. Furthermore, 6-(L-1,2,3-Trihydroxybutyl)-pterin has been utilized as an internal standard for quantifying biopterin and neopterin in rat plasma using LC-MS.