T3719

Daminozide (Succinic Acid) is a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily.

L-Allylglycine is an amino acid derivative that reduces glutamate decarboxylase (GAD) activity by 60% when administered at a dose of 39.8 μmol/g per hour ex vivo in mouse brain preparations. L-Allylglycine (1.2 mmol/kg, i.p.) induces convulsions and decreases GABA concentration throughout the cerebellum, pons, medulla, striatum, cortex, and hippocampus in mice. Chronic administration (3.2 μg/0.5 μl per hour for 13 days) of L-allylglycine in rats increases locomotor activity in an open field test and impairs attention in the 5-choice serial reaction time task (5CSRTT). In vitro, L-allylglycine inhibits GAD only when used at high concentrations (1-80 mM). The more potent in vivo activity can be attributed to metabolic conversion of L-allylglycine to 2-keto-4-pentanoic acid, a more potent convulsant and GAD inhibitor.

5-AAM-2-CP is one of the major metabolites of Acetamiprid. Acetamiprid, a nAChR agonist, is a neonicotinoid insecticide used worldwide.

5-HT1A modulator 2 hydrochloride, a derivative of 8-OH-DPAT, is a modulator of 5-HT1A with a Ki of 53 nM for 5-HT1A binding [1]. [1]. Naiman, N., et al. 2-(Alkylamino)tetralin derivatives: interaction with 5-HT1A serotonin binding sites. Journal of Medicinal Chemistry, 1989; 32(1), 253-256.

Mu-6S-Palm-β-Glc is a fluorogenic substrate specifically designed for palmitoyl-protein thioesterase (PPT). It is enzymatically cleaved by PPT1 to release the fluorescent 4-methylumbelliferone (MU) moiety, enabling sensitive quantification of enzyme activity. This substrate is a critical tool in the study of infantile neuronal ceroid lipofuscinosis (INCL), a lysosomal storage disorder. It is utilized for both prenatal and postnatal diagnostic assays, as well as in the evaluation of bi-functional IgG-lysosomal enzyme fusion proteins for brain-targeted drug delivery.

4-Methylumbelliferyl-2-acetamido-2-deoxy-β-D-Glucopyranoside is a fluorogenic substrate for β-hexosaminidases that releases fluorescent 4-methylumbelliferone upon enzymatic cleavage, enabling sensitive quantification of enzyme activity across pH-dependent excitation and emission ranges, and is extensively used in clinical and research assays for GM2 gangliosidoses such as Tay-Sachs disease.

Selective FTO inhibitor (IC50 = 0.81 μM). Exhibits >30-fold selectivity for FTO over ALKBH2, 3 and 5 and >100-fold selectivity over PHD2 and JMJD2A. Increases levels of modified N6-methyladenosine (m6A) in HeLa cells in a concentration-dependent manner.

Bilaid C is a tetrapeptide μ-opioid receptor agonist (Ki= 210 nM in HEK293 cell membranes expressing the human receptor) that has been found inPenicillium.1It inhibits forskolin-induced cAMP accumulation by 77% in HEK293 cells expressing the human μ-opioid receptor when used at a concentration of 10 μM. Bilaid C induces inward rectifying potassium channel (Kir) currents in rat locus coeruleus slices that endogenously express high levels of the μ-opioid receptor (EC50= 4.2 μM). 1.Dekan, Z., Sianati, S., Yousuf, A., et al.A tetrapeptide class of biased analgesics from an Australian fungus targets the μ-opioid receptorProc. Natl. Acad. Sci. USA116(44)22353-22358(2019)