HTH-01-015 - ≥98%(HPLC), high purity , CAS No.1613724-42-7, Inhibitor of NUAK family kinase 1

Item Number
H286770
Grouped product items
SKUSizeAvailabilityPrice Qty
H286770-5mg
5mg
In stock
$107.90
H286770-10mg
10mg
In stock
$151.90
H286770-50mg
50mg
In stock
$467.90
H286770-100mg
100mg
In stock
$576.90

Potent and selective NUAK1 inhibitor

Basic Description

Specifications & PurityMoligand™, ≥98%(HPLC)
Biochemical and Physiological MechanismsPotent and selective NUAK1 inhibitor (IC50= 100 nM). Exhibits no significant inhibition against a panel of 139 kinases, including ten AMPK family members. Inhibits NUAK1-mediated MYPT1 phosphorylation. Also inhibits cell proliferation in U2OS cellsin vitr
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor of NUAK family kinase 1

Associated Targets(Human)

NUAK1 Tchem NUAK family SNF1-like kinase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NUAK1 Tchem NUAK family SNF1-like kinase 1 (1769 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NUAK2 Tchem NUAK family SNF1-like kinase 2 (630 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

Pubchem Sid488202380
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488202380
IUPAC 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
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)
InChi Key CHSDJDLAKKAWCI-UHFFFAOYSA-N
Canonical SMILES CC1=C2C(=NC(=N1)NC3=CN(N=C3)C4CCNCC4)N(C5=CC6=CC=CC=C6C=C5C(=O)N2C)C
Isomeric SMILES CC1=C2C(=NC(=N1)NC3=CN(N=C3)C4CCNCC4)N(C5=CC6=CC=CC=C6C=C5C(=O)N2C)C
PubChem CID 78357766
Molecular Weight 468.55

Certificates

Certificate of Analysis(COA)

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8 results found

Lot NumberCertificate TypeDateItem
D23141619Certificate of AnalysisMar 06, 2023 H286770
D23141620Certificate of AnalysisMar 06, 2023 H286770
D23141755Certificate of AnalysisMar 06, 2023 H286770
D23141919Certificate of AnalysisMar 06, 2023 H286770
D23141990Certificate of AnalysisMar 06, 2023 H286770
D23142007Certificate of AnalysisMar 06, 2023 H286770
D23142030Certificate of AnalysisMar 06, 2023 H286770
D23142072Certificate of AnalysisMar 06, 2023 H286770

Chemical and Physical Properties

Solubility≥23.45 mg/mL in DMSO; insoluble in H2O; ≥14.67 mg/mL in EtOH with ultrasonic

Related Documents

References

1. Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS.  (2014)  Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases..  Biochem J,  457  (1): (215-25).  [PMID:24171924] [10.1021/op500134e]

Solution Calculators