A selective NUAK1 inhibitor
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HTH-01-015

Item No. 19091

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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
CAS Number
1613724-42-7
Molecular Formula
C26H28N8O
Formula Weight
468.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 20 mg/ml
λmax
228, 254 nm
SMILES
CC1=C(N(C)C(C2=CC(C=CC=C3)=C3C=C2N4C)=O)C4=NC(NC5=CN(N=C5)C6CCNCC6)=N1
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    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.1 At 10 µM, HTH-01-015 has been shown to partially inhibit the phosphorylation of the NUAK1 substrate, myosin phosphate-targeting subunit 1 at Ser445.1 When administered to mouse embryonic fibroblasts in vitro, 10 µM HTH-01-015 inhibits proliferation and migration in a wound-healing assay.1 It has also been shown to impair the invasive potential of U2OS cells at similar concentrations in a 3D cell invasion assay.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Banerjee, S., Buhrlage, S.J., Huang, H.T., et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem. J. 457(1), 215-225 (2014).