产品说明书

HTH-01-015

Print
Chemical Structure| 1613724-42-7 同义名 : -
CAS号 : 1613724-42-7
货号 : A321152
分子式 : C26H28N8O
纯度 : 99%+
分子量 : 468.553
MDL号 : MFCD28167816
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(224.09 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • AMPK

    NUAK1 , IC50:100 nM
描述 HTH-01-015 is a selective NUAK1 inhibitor with IC50 value of 100nM. HTH-01-015 at 10μM inhibited the phosphorylation of the only well-characterized substrate, MYPT1 (myosin phosphate-targeting subunit 1) that is phosphorylated by NUAK1 at Ser-445. HTH-01-015 significantly inhibited MEFs proliferation and migration in a wound-healing assay. HTH-01-015 inhibited the proliferation and impaired the invasive potential of U2OS cells in a 3D cell invasion assay. The 195 site of NUAK1 is important for the inactivation effect of HTH-01-015 for a mutation (A195T) renders NUAK1 ∼50-fold resistant to HTH-01-015[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.67mL

2.13mL

1.07mL

21.34mL

4.27mL

2.13mL
参考文献

[1]Banerjee S, Buhrlage SJ, et al. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25.

[2]Banerjee S, Buhrlage SJ, Huang HT, Deng X, Zhou W, Wang J, Traynor R, Prescott AR, Alessi DR, Gray NS. Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases. Biochem J. 2014 Jan 1;457(1):215-25. doi: 10.1042/BJ20131152. PMID: 24171924; PMCID: PMC3969223.