HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates the abundance of p53, cracked caspase-7, and cracked PARP, and induces apoptosis in cancer cells.

 

Brand: BCM

 

Target: TOPK

 

Signaling Pathways: MAPK

 

In Vitro: HI-TOPK-032 inhibits anchorage-dependent and -independent colon cancer cell growth by reducing ERK-RSK phosphorylation as well as increasing colon cancer cell apoptosis through regulation of the abundance of p53, cleaved caspase-7, and cleaved PARP. However, HI-TOPK-032 at the highest concentration (5 μM) also inhibits MEK1 activity by 40%. HI-TOPK-032 strongly inhibits TOPK kinase activity. However, it also has little effect on extracellular signal-regulated kinase 1 (ERK1), c-jun-NH2-kinase 1, or p38 kinase activities. HI-TOPK-032 occupies the ATP-binding site of TOPK and fits the binding site very well. The compound forms hydrogen bonds with GLY83 and ASP151 and has a hydrophobic interaction with LYS30.

 

Boiling Point: 415.3±45.0 °C(Predicted)

 

pKa: 9.32±0.46(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; Insoluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: C1=CC=C2C(=C1)N=C3C(=C4C=C(C=CN4C3=N2)NC(=O)C5=CC=CS5)C#N  

 

InChIKey: BCSBXWKRZUPFHW-UHFFFAOYSA-N  

InChI: InChI=1S/C20H11N5OS/c21-11-13-16-10-12(22-20(26)17-6-3-9-27-17)7-8-25(16)19-18(13)23-14-4-1-2-5-15(14)24-19/h1-10H,(H,22,26) 

 

Attribute
[Chem Name]	N-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)thiophene-2-carboxamide
[Synonym]	HI-TOPK-032
[CAS No.]	487020-03-1
[MDL No.]	MFCD03286313
[Formula]	C20H11N5OS
[Molecular]	369.4
[Form]	Orange-brown powder
[Storage]	Sealed in dry. Stored at -20°C.

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