Bestatin

Bestatin (Ubenimex) competitively inhibits many aminopeptidases, including B, N and leucine aminopeptidases. Ubenimex is a microbial metabolite and dipeptide with potential immunomodulatory and antitumor activities. Aminopeptidases has been implicated in the process of cell adhesion and invasion of tumor cells. Therefore, inhibiting aminopeptidases may partially attribute to the antitumor effect of ubenimex. This agent also activates T lymphocyte, macrophage, and bone marrow stem cell as well as stimulates the release of interleukin-1 and -2, thus further enhances its antitumor activity.

Bestatin-amido-Me, a derivative of Bestatin, acts as an IAP ligand and interacts with ABL inhibitor through a linker to produce SNIPER[1].

Bestatin-CoA (Bestatin-coenzyme A) is a derivative of coenzyme A.

Bestatin hydrochloride (Ubenimex hydrochloride) is an inhibitor of aminopeptidase N (APN)/CD13 and aminopeptidase B.

Bestatin-amide-PEG3-CH2-acid is an E3 Ligase Ligand-linker conjugate. It is utilized in the synthesis of PROTACRAR Degrader-1.

Bestatin trifluoroacetate (Ubenimex trifluoroacetate) is a CD13 (Aminopeptidase N)/APN and leukotriene A4 hydrolase inhibitor that is often used in cancer research.

Bestatin methyl ester (600, 900 µM; 24 h) inhibits spore cell differentiation in Dictyostelium discoideum.

Obestatin (rat) acetate is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin (rat) acetate has anti-inflammatory, anti-myocardial infarction and antioxidant properties. Obestatin (rat) acetate suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain.

Ketomethylenebestatin is a carba-analog of bestatin,the aminopeptidase (AP) inhibitor. Ketomethylenebestatin is 10 fold less effective as an inhibitor of aminopeptidases than bestatin.

4-Hydroxybestatin is a major active metabolite of bestatin.

Epibestatin Hydrochloride is a stabilizer of 14-3-3 PPIs, as well as a diastereoepimer of aminopeptidase inhibitor bestatin.

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)

Obestatin (human) is an endogenous ligand for G-protein eurythmic entity 39 formed by shearing of preproghrelin, which inhibits feeding in a dose-dependent manner, and can be used in the study of obesity.

Obestatin(rat) TFA is a cpeptide derived from the Ghrelin gene, consisting of 23 amino acids. This compound modulates physiological processes by suppressing food intake, inhibiting jejunal contraction, and reducing body-weight gain. It functions as an endogenous ligand for G-protein coupled receptor 39 (GPR39). Additionally, Obestatin(rat) TFA exhibits anti-inflammatory, anti-myocardial infarction, and antioxidant activities [1] [2].

Obestatin(human) TFA, an endogenous peptide originating from the same prepropeptide as ghrelin, is known to suppress food intake and reduce weight gain in rats.

Obestatin(11-23)mouse, rat is a polypeptide that regulates energy balance and suppresses appetite by reducing food consumption, body weight, and jejunal contractions in rodents [1].

Gibbestatin B inhibits the expression of gibberellin-induced α-amylase in de-embryonated rice and barley, with an IC50 of 25-50 ppm. It does not exhibit antibacterial, anti-yeast, or antifungal activity at a concentration of 100 ppm.

Gibbestatin C is a bioactive compound.

Endogenous peptide that suppresses food intake and body weight-gain

ZK-304709 is an oral multitarget tumor growth inhibitor with activity against cell-cycle progression and angiogenesis.

Biotin-BS is a chemical compound composed of two distinct ligands: methyl-bestatin (MeBS) for cIAP1 and biotin. These ligands are interconnected through linkers. MeBS serves as a ligand specifically for the cellular inhibitor of apoptosis protein 1 (cIAP1) ubiquitin ligase[1].

BzNH-BS is a chemical compound comprising two distinct ligands: methyl-bestatin (MeBS) for cIAP1 and benzoyl-amide. The ligands are interconnected through linkers. MeBS functions as a ligand for cIAP1, a ubiquitin ligase involved in cellular inhibition of apoptosis processes [1].

ATRA-hydroxyimino, also known as CRABP-II ligand 1, is a chemical compound derived from Retinoic acid (ATRA). This compound binds to the cIAP1 ligand, specifically Bestatin, through a linker, resulting in the formation of a complex called SNIPER. The purpose of this complex is to degrade CRABP-II within IMR-32 cells[1].

Estrone-N-O-C1-amido (ERα ligand 1) is an estrogen ligand derivative of Estrone that specifically binds to estrogen receptor α (ERα). With a linker, it complexes with the cIAP1 ligand Bestatin, forming SNIPER[1].