SML1446

HTH-01-015

≥98% (HPLC)

• Synonym(s): 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
• Empirical Formula (Hill Notation): C₂₆H₂₈N₈O
• CAS Number: 1613724-42-7
• Molecular Weight: 468.55
• MDL number: MFCD28167816
• PubChem Substance ID: 329825886
• NACRES: NA.77

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: powder
• color: white to light brown
• solubility: DMSO: 5 mg/mL, clear (warmed)
• storage temp.: −20°C
• SMILES string: CC1=C2C(N(C)C(C=C(C=CC=C3)C3=C4)=C4C(N2C)=O)=NC(NC5=CN(C6CCNCC6)N=C5)=N1
• 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

Description

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.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable