<Suppliers Price>

TC-G 24

Names

[ CAS No. ]:
1257256-44-2

[ Name ]:
TC-G 24

[Synonym ]:
3-Pyridinecarboxamide,N-(3-chloro-4-isoquinolinyl)-2-(cyclopropylamino)
N-(3-CHLOROISOQUINOLIN-4-YL)-2-CYCLOPROPYLAMINONICOTINAMIDE
N-(3-chloro-4-methylphenyl)-5-(4-nitrophenyl)-1,3,4-oxadiazol-2-amine
N-(3-chloro-4-methyl-phenyl)-3-methyl-benzamide
N-(3-chloro-4-isoquinolinyl)-2-cyclopropylamino-3-pyridinecarboxamide

Biological Activity

[Description]:

TC-G 24 (Compound 24) is a potent, selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 17.1 nM. TC-G 24 can cross the BBB and can be used for studying many diseases such as type 2 diabetes mellitus, stroke, Alzheimer, and other related diseases[1].

[Related Catalog]:

Signaling Pathways >> Stem Cell/Wnt >> GSK-3
Research Areas >> Metabolic Disease
Research Areas >> Neurological Disease
Signaling Pathways >> PI3K/Akt/mTOR >> GSK-3

[Target]

GSK-3β:17.1 nM (IC50)


[In Vitro]

TC-G 24 (Compound 24) binds to the ATP binding site of GSK-3β[1]. TC-G 24 (1 µM, 4 h) blocks the FBW7α-mediated degradation of TPP1 in human embryonic kidney (HEK) 293T cells[2]. Western Blot Analysis[2] Cell Line: 293T cells Concentration: 1 μM Incubation Time: 4 h Result: Blocked the FBW7α-mediated degradation of TPP1

[In Vivo]

TC-G 24 (Compound 24) (0-15 mg/kg; i.p.; once) significantly raises liver glycogen content in a dose-dependent manner without obvious toxicity and can cross the BBB[1]. Animal Model: Six-week-old male C57BL/6N mice with weights averaging 22 g[1] Dosage: 1, 5, and 15 mg/kg Administration: Intraperitoneal injection, once Result: Significantly raised liver glycogen content in a dose-dependent manner without obvious toxicity. Was detected in the brain at concentrations higher than in plasma for all three tested doses (38 ± 6, 113 ± 54 and 286 ± 58 ng/g brain tissue at 1, 5 and 15 mg/kg, respectively).

[References]

[1]. Khanfar MA, et al. Discovery of novel GSK-3β inhibitors with potent in vitro and in vivo activities and excellent brain permeability using combined ligand- and structure-based virtual screening. J Med Chem. 2010 Dec 23;53(24):8534-45.

[2]. Lihui Wang, et al. FBW7 Mediates Senescence and Pulmonary Fibrosis through Telomere Uncapping. Cell Metab. 2020 Nov 3;32(5):860-877.e9.

Chemical & Physical Properties

[ Molecular Formula ]:
C15H11ClN4O3

[ Molecular Weight ]:
330.73

[ Exact Mass ]:
330.05200

[ PSA ]:
100.00000

[ LogP ]:
4.29530

Related Compounds