GNF2133 HCl

• CAS: 2561414-57-9
• Catalog Number: ACM2561414579
• Category: Inhibitors
• Molecular Weight: 471.00
• Molecular Formula: C24H31ClN6O2
• Description: GNF2133 is a potent and selective DYRK1A inhibitor (IC50 = 6 nM). In vitro, GNF2133 is able to proliferate both rodent and human β-cells. In vivo, GNF2133 demonstrated significant dose-dependent glucose disposal capacity and insulin secretion in response to glucose-potentiated arginine-induced insulin secretion (GPAIS) challenge in rat insulin promoter and diphtheria toxin A (RIP-DTA) mice.
• Synonyms: GNF2133 HCl; GNF2133 hydrochloride; GNF2133; GNF-2133; GNF 2133
• IUPAC Name: 4-Ethyl-N-(4-(1-(tetrahydro-2H-pyran-4-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl)piperazine-1-carboxamide hydrochloride
• Canonical SMILES: O=C(N1CCN(CC)CC1)NC2=NC=CC(C3=CN(C4CCOCC4)C5=C3C=CN=C5)=C2.[H]Cl
• InChI: InChI=1S/C24H30N6O2.ClH/c1-2-28-9-11-29(12-10-28)24(31)27-23-15-18(3-8-26-23)21-17-30(19-5-13-32-14-6-19)22-16-25-7-4-20(21)22;/h3-4,7-8,15-17,19H,2,5-6,9-14H2,1H3,(H,26,27,31);1H
• InChI Key: PKSHRWPMQDLRRB-UHFFFAOYSA-N
• Solubility: Soluble in DMSO
• Appearance: Solid powder
• Shelf Life: >3 years if stored properly
• Storage: Dry, dark and at 0-4 °C for short term (days to weeks) or -20 °C for long term (months to years).
• Alternative CAS: 2561414-56-8 (free base); 2561414-57-9 (HCl)
• Biological Target: GNF2133 hydrochloride is a potent, selective and orally active DYRK1A inhibitor with IC50s of 0.0062, >50 µM for DYRK1A and GSK3β, respectively.
• Drug Formulation: This drug may be formulated in DMSO
• Elemental Analysis: C, 61.20; H, 6.63; Cl, 7.53; N, 17.84; O, 6.79
• Exact Mass: 434.243
• HS Tariff Code: 2934.99.9001
• In Vitro Activity: This report describes the discovery of a potent and selective DYRK1A inhibitor GNF2133, which was identified through optimization of a 6-azaindole screening hit. In vitro, GNF2133 is able to proliferate both rodent and human β-cells.; Reference: J Med Chem. 2020 Mar 26;63(6):2958-2973. https://pubmed.ncbi.nlm.nih.gov/32077280/
• In Vivo Activity: In vivo, GNF2133 demonstrated significant dose-dependent glucose disposal capacity and insulin secretion in response to glucose-potentiated arginine-induced insulin secretion (GPAIS) challenge in rat insulin promoter and diphtheria toxin A (RIP-DTA) mice.; Reference: J Med Chem. 2020 Mar 26;63(6):2958-2973. https://pubmed.ncbi.nlm.nih.gov/32077280/
• Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
• Stock Solution Storage: 0-4 °C for short term (days to weeks), or -20 °C for long term (months).