HTH-01-015 is a potent selective NUAK1 inhibitor with an IC50 of 100 nM, which is more than 100 times more selective than that used for NUAK2.

 

Brand: BCM

 

Target: AMPK

 

Signaling Pathways: Chromatin/Epigenetic; PI3K/Akt/mTOR signaling

 

In Vitro: In HEK-293 cells expressing NUAK1 and NUAK2, HTH-01-015 inhibits NuAK1-mediated phosphorylation of MYPT1. HTH-01-015 inhibits cell migration in NUAK1+/+ MEFs and inhibits U2OS cell invasion. In addition, HTH-01-015 inhibited cell proliferation in two cell lines. In U2OS cells, HTH-01-015 inhibitors significantly restricted the entry of cells into the mitotic phase.

 

Boiling Point: 759.6±70.0 °C(Predicted)

 

pKa: 9.84±0.10(Predicted)

 

Solubility: Soluble in DMSO (warmed with 50ºC water bath); soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric SMILES: CC1=C2C(=NC(=N1)NC3=CN(N=C3)C4CCNCC4)N(C5=CC6=CC=CC=C6C=C5C(=O)N2C)C  

 

InChIKey: CHSDJDLAKKAWCI-UHFFFAOYSA-N  

 

InChI: InChI=1S/C26H28N8O/c1-16-23-24(31-26(29-16)30-19-14-28-34(15-19)20-8-10-27-11-9-20)32(2)22-13-18-7-5-4-6-17(18)12-21(22)25(35)33(23)3/h4-7,12-15,20,27H,8-11H2,1-3H3,(H,29,30,31) 

 

Attribute
[Chem Name]	2,7,9-trimethyl-5-[(1-piperidin-4-ylpyrazol-4-yl)amino]-2,4,6,9-tetrazatetracyclo[9.8.0.03,8.013,18]nonadeca-1(19),3,5,7,11,13,15,17-octaen-10-one
[Synonym]	HTH-01-015
[CAS No.]	1613724-42-7
[MDL No.]	MFCD28167816
[Formula]	C26H28N8O
[Molecular]	468.55
[Form]	White to light brown powder
[Storage]	Keep in dark place. Sealed in dry. Store in freezer, under -20°C

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