HTH-01-015|cas 1613724-42-7|DC Chemicals

Cas No.:	1613724-42-7
Chemical 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
Synonyms:	HTH-01-015;HTH 01 015;5,13-Dihydro-4,5,13-trimethyl-2-[[1-(4-piperidinyl)-1H-pyrazol-4-yl]amino]-6H-naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6-one;GTPL8977;BCP14400;s7318;AK316255;2,7,;2,7,9-Trimethyl-5-[(1-piperidin-4-ylpyrazol-4-yl)amino]-2,4,6,9-tetrazatetracyclo[9.8.0.03,8.013,18]
SMILES:	O=C1C2=C([H])C3=C([H])C([H])=C([H])C([H])=C3C([H])=C2N(C([H])([H])[H])C2C(=C(C([H])([H])[H])N=C(N=2)N([H])C2C([H])=NN(C=2[H])C2([H])C([H])([H])C([H])([H])N([H])C([H])([H])C2([H])[H])N1C([H])([H])[H]
Formula:	C₂₆H₂₈N₈O
M.Wt:	468.5535
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

HTH-01-015 is a selective NUAK1 inhibitor (IC50 is 100 nM). HTH-01-015 inhibits NUAK1 with >100-fold higher potency than NUAK2 (IC50 of >10 μM).

In Vitro:

HTH-01-015 is a specific NUAK1 inhibitor. The related NUAK1 and NUAK2 are members of the AMPK (AMP-activated protein kinase) family of protein kinases that are activated by the LKB1 (liver kinase B1) tumor suppressor kinase. HTH-01-015 inhibits NUAK1 with an IC50 of 100 nM, but does not significantly inhibit NUAK2 (IC50 of >10 μM). In all cell lines tested, HTH-01-015 inhibits the phosphorylation of the only well-characterized substrate, MYPT1 (myosin phosphate-targeting subunit 1) that is phosphorylated by NUAK1 at Ser445. In U2OS cells, HTH-01-015 suppresses proliferation and phosphorylation of MYPT1 to the same extent as shRNA-mediated NUAK1 knockdown. In mouse embryonic fibroblasts (MEFs), treatment with 10 μM HTH-01-015 suppresses proliferation and phosphorylation of MYPT1 to the same extent as NUAK1-knockout. To test whether NUAK1 inhibition impaired the ability of the invasive U2OS cells to enter a matrix, 3D Matrigel Transwell invasion assays demonstrate that 10 μM HTH-01-015 markedly inhibits the invasiveness of U2OS cells in this assay[1].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC8296	Dorsomorphin(BML-275)	Dorsomorphin(Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits the bone morphogenetic protein type 1 receptors ACTR-I (ALK2), B
DC11466	PF-06409577	PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.
DC11405	MK-3903	MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM. generation of catalytically active enzyme.
DC7705	HTH-01-015	HTH-01-015 is a selective inhibitor of NUAK1 kinase with an IC50 value of 100 nM.
DC11634	EX-229	EX229 is a small molecule AMPK activator that dose-dependently increases AMPK activity of α1-, α2-, β1- and β2-containing complexes at 50 uM
DC8182	Bempedoic Acid(ETC-1002;ESP-55016)	ETC-1002(ESP-55016) is a novel, first-in-class, orally available, once-daily LDL-C lowering small molecule; activator of hepatic AMP-activated protein kinase (AMPK); also has potent inhibitory activity against hepatic ATP-citrate lyase(IC50=29 uM).
DC7115	Dorsomorphin dihydrochloride	Dorsomorphin 2Hcl (Compound C; BML-275) has been shown to act as a potent and selective inhibitor of AMPK (AMP-activated protein kinase; Ki = 109 nM), induced by AICAR and metformin; also inhibits ALK2, ALK3, and ALK 6 .
DC7047	AICAR (Acadesine)	Acadesine results in accumulation of ZMP, which mimics the stimulating effect of AMP on AMPK and AMPK kinase. Phase 3.
DC7045	A-769662	A-769662 is a potent, reversible AMPK activator with EC50 of 0.8 μM, little effect on GPPase/FBPase activity.