HTH-01-015

Catalog No.S7318

Molecular Weight(MW): 468.55

HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.

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5mg	USD 97	In stock
25mg	USD 297	In stock
100mg	USD 697	In stock
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Biological Activity

Description

HTH-01-015 is a potent and selective NUAK1 inhibitor with IC50 of 100 nM, >100-fold selectivity over NUAK2.

Targets

NUAK1 ^[1]
()

100 nM

In vitro

In HEK-293 cells express NUAK1 as well as NUAK2, HTH-01-015 suppresses NUAK1-mediated MYPT1 phosphorylation. HTH-01-015 suppresses cell migration In NUAK1+/+ MEFs, and inhibit U2OS cell invasion. Moreover, HTH-01-015 inhibits cell proliferation in both cell lines. ^[1] HTH-01-015 inhibitors markedly restricted cells from entering into mitosis in U2OS cells. ^[2]

Protocol

Kinase Assay:^[1]	+ Expand Kinase activity assays: In vitro activities of purified GST–NUAK1 and GST–NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-³²P]ATP into Sakamototide substrate peptide. Reactions are carried out in a 50 μL reaction volume for 30 min at 30°C and reactions are terminated by spotting 40 μL of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-³²P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalyses the incorporation of 1 nmol of [³²P]phosphate into the substrate over 1 h.
Cell Research:^[1]	+ Expand Cell lines: U2OS cells and MEFs Concentrations: 10 μM Incubation Time: 5 days Method: Cell proliferation assays are carried out colorimetrically in 96-well plates using the CellTiter 96® AQueous Non-Radioactive Cell Proliferation Assay kit following the manufacturer's protocol. Initially, 2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried out over 5 days in the presence or absence of 10 μM HTH-01-015. (Only for Reference)

Kinase Assay:^[1]

+ Expand

Kinase activity assays:

In vitro activities of purified GST–NUAK1 and GST–NUAK1[A195T] are measured using Cerenkov counting of incorporation of radioactive 32P from [γ-³²P]ATP into Sakamototide substrate peptide. Reactions are carried out in a 50 μL reaction volume for 30 min at 30°C and reactions are terminated by spotting 40 μL of the reaction mix on to P81 paper and immediately immersing in 50 mM orthophosphoric acid. Samples are washed three times in 50 mM orthophosphoric acid followed by a single acetone rinse and air drying. The kinase-mediated incorporation of [γ-³²P]ATP into Sakamototide is quantified by Cerenkov counting. One unit of activity is defined as that which catalyses the incorporation of 1 nmol of [³²P]phosphate into the substrate over 1 h.

Cell Research:^[1]

+ Expand

Cell lines: U2OS cells and MEFs
Concentrations: 10 μM
Incubation Time: 5 days
Method: Cell proliferation assays are carried out colorimetrically in 96-well plates using the CellTiter 96® AQueous Non-Radioactive Cell Proliferation Assay kit following the manufacturer's protocol. Initially, 2000 cells per well are seeded for U2OS cells and 3000 cells per well are seeded for MEFs. The proliferation assays are carried out over 5 days in the presence or absence of 10 μM HTH-01-015.
(Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	58 mg/mL warmed (123.78 mM)
	Ethanol	30 mg/mL (64.02 mM)
	Water	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download HTH-01-015 SDF

Molecular Weight	468.55
Formula	C₂₆H₂₈N₈O
CAS No.	1613724-42-7
Storage	3 years -20°C powder
Synonyms	N/A

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