ChemicalBook > CAS DataBase List > HTH-01-015

HTH-01-015

Product Name
HTH-01-015
CAS No.
1613724-42-7
Chemical Name
HTH-01-015
Synonyms
CS-2296;HTH-01-015;HTH-01-015 >=98% (HPLC);CHSDJDLAKKAWCI-UHFFFAOYSA-N;inhibit,AMPK,AMP-activated protein kinase,HTH 01 015,HTH01015,Inhibitor;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;4,5,13-Trimethyl-2-((1-(piperidin-4-yl)-1H-pyrazol-4-yl)amino)-5,13-dihydro-6H-naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6-one;6H-Naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6-one, 5,13-dihydro-4,5,13-trimethyl-2-[[1-(4-piperidinyl)-1H-pyrazol-4-yl]amino]-
CBNumber
CB22715641
Molecular Formula
C26H28N8O
Formula Weight
468.55
MOL File
1613724-42-7.mol
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HTH-01-015 Property

Boiling point:
759.6±70.0 °C(Predicted)
Density 
1.41±0.1 g/cm3(Predicted)
storage temp. 
-20°C
solubility 
≥23.45 mg/mL in DMSO; insoluble in H2O; ≥14.67 mg/mL in EtOH with ultrasonic
form 
powder
pka
9.84±0.10(Predicted)
color 
white to light brown
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1446
Product name
HTH-01-015
Purity
≥98% (HPLC)
Packaging
5MG
Price
$130
Updated
2024/03/01
Sigma-Aldrich
Product number
SML1446
Product name
HTH-01-015
Purity
≥98% (HPLC)
Packaging
25MG
Price
$520
Updated
2024/03/01
Cayman Chemical
Product number
19091
Product name
HTH-01-015
Purity
≥95%
Packaging
1mg
Price
$73
Updated
2024/03/01
Cayman Chemical
Product number
19091
Product name
HTH-01-015
Purity
≥95%
Packaging
5mg
Price
$110
Updated
2024/03/01
Cayman Chemical
Product number
19091
Product name
HTH-01-015
Purity
≥95%
Packaging
10mg
Price
$201
Updated
2024/03/01
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HTH-01-015 Chemical Properties,Usage,Production

Description

NUAK1 (also known as AMPK-related kinase 5) and NUAK2 (also known as SNF1/AMPK-related kinase) are members of the AMP-activated protein kinase (AMPK) family of protein kinases that are activated by the liver kinase B1 tumor suppressor kinase. NUAK kinases are thought to have roles in regulating cell adhesion, cancer cell invasion, embryonic development, senescence, proliferation, neuronal polarity, and axon branching. HTH-01-015 is a selective inhibitor of NUAK1 (IC50 = 100 nM) and does not affect the activity of a panel of 139 other kinases, including additional AMPK family members. At 10 μM, HTH-01-015 has been shown to partially inhibit the phosphorylation of the NUAK1 substrate, myosin phosphate-targeting subunit 1 at Ser445. When administered to mouse embryonic fibroblasts in vitro, 10 μM HTH-01-015 inhibits proliferation and migration in a wound-healing assay. It has also been shown to impair the invasive potential of U2OS cells at similar concentrations in a 3D cell invasion assay.

Uses

HTH 01-015 is a highly specific protein kinase inhibitor of NUAK1. It inhibits the NUAK1 phosphorylation of myosin phosphate-targeting subunit 1 (MYPT1) substrate.

Biochem/physiol Actions

HTH-01-015 is a potent and selective inhibitor of NUAK1 kinase, a member of the AMPK family that are that are activated by the LKB1 (liver kinaseB1) tumour suppressor kinase and involved in development and proliferation. HTH-01-015 has an IC50 of 100 nM for NUAK1, >100-fold higher than NUAK2, and has no significant inhibition of 139 other kinases tested, including ten AMPK-related kinase family members. Treatment with HTH-01-015 was found to suppress proliferation, restricting cells from entering into mitosis.

storage

Store at -20°C

References

1. sourav b, sara j b, hai-tsang h, et al. characterization of wz4003 and hth-01-015 as selective inhibitors of the lkb1-tumour-suppressor-activated nuak kinases. biochemical journal, 2014, 457(1): 215-225.

HTH-01-015 Preparation Products And Raw materials

Raw materials

Preparation Products

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HTH-01-015 Suppliers

China 63 India 2 United Kingdom 1 United States 11 Global 77
Shanghai Boyle Chemical Co., Ltd.
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Chembest Research Laboratories Limited
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LETOPHARM LIMITED
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+86-21-5106 2861
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Sigma-Aldrich
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Shanghai EFE Biological Technology Co., Ltd.
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  • 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
  • CS-2296
  • CHSDJDLAKKAWCI-UHFFFAOYSA-N
  • 6H-Naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6-one, 5,13-dihydro-4,5,13-trimethyl-2-[[1-(4-piperidinyl)-1H-pyrazol-4-yl]amino]-
  • HTH-01-015 >=98% (HPLC)
  • inhibit,AMPK,AMP-activated protein kinase,HTH 01 015,HTH01015,Inhibitor
  • 4,5,13-Trimethyl-2-((1-(piperidin-4-yl)-1H-pyrazol-4-yl)amino)-5,13-dihydro-6H-naphtho[2,3-e]pyrimido[5,4-b][1,4]diazepin-6-one
  • 1613724-42-7
  • Inhibitors