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NU6027

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Chemical Structure| 220036-08-8 同义名 : -
CAS号 : 220036-08-8
货号 : A488693
分子式 : C11H17N5O2
纯度 : 98%
分子量 : 251.29
MDL号 : MFCD05664735
存储条件：

粉末 Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(47.75 mM)，配合低频超声，并水浴加热至45℃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

  • CDK2

    CDK2, Ki:1.3 μM

  • CDK1

    CDK1, Ki:2.5 μM
描述 Cyclin-dependent kinases (CDKs) are the catalytic subunits of a family of mammalian heterodimeric serine/threonine kinases that have been implicated in the control of cell-cycle progression, transcription and neuronal function[3]. NU6027 is a potent and ATP-competitive inhibitor of both CDK1 and CDK2, with Kis of 2.5 µM and 1.3 µM, respectively. NU6027 is also a potent inhibitor of ATR and enhances hydroxyurea and cisplatin cytotoxicity in an ATR-dependent manner[4]. NU6027 attenuated G2/M arrest following DNA damage, inhibited RAD51 focus formation and increased the cytotoxicity of the major classes of DNA-damaging anticancer cytotoxic therapy but not the antimitotic, paclitaxel. NU6027 was synthetically lethal when DNA single-strand break repair is impaired either through poly(ADP-ribose) polymerase (PARP) inhibition or defects in XRCC1[5]. NU6027 prevented the Trovafloxacin-mediated increases in LPS-induced TNF mRNA and protein release, Trovafloxacin prolonged TNF mRNA stability, and this effect was largely attenuated by NU6027[6]. NU-6027 inhibits Mycobacterium bovis BCG growth in vitro and also displayed cross-reactivity with Mycobacterium tuberculosis protein kinase D (PknD) and protein kinase G (PknG)[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.98mL

0.80mL

0.40mL

19.90mL

3.98mL

1.99mL

39.79mL

7.96mL

3.98mL
参考文献

[1]Charrier JD, Durrant SJ, et al. Discovery of potent and selective inhibitors of ataxia telangiectasia mutated and Rad3 related (ATR) protein kinase as potential anticancer agents. J Med Chem. 2011 Apr 14;54(7):2320-30.

[2]Arris CE, Boyle FT, et al. Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem. 2000 Jul 27;43(15):2797-804.

[3]Marcos Malumbres,et al. Mammalian cyclin-dependent kinases. Trends Biochem Sci. 2005.30(11), 630-41.

[4]Arris CE, et, al. Identification of novel purine and pyrimidine cyclin-dependent kinase inhibitors with distinct molecular interactions and tumor cell growth inhibition profiles. J Med Chem. 2000. 43(15), 2797-804.

[5]Peasland A, et, al. Identification and evaluation of a potent novel ATR inhibitor, NU6027, in breast and ovarian cancer cell lines. Br J Cancer. 2011. 105(3), 372-81.

[6]Kyle L Poulsen,et al. J Pharmacol Exp Ther. 2014. 350(1), 164-70.

[7]Saqib Kidwai,et al. NU-6027 Inhibits Growth of Mycobacterium tuberculosis by Targeting Protein Kinase D and Protein Kinase G. Antimicrob Agents Chemother. 2019. 63(9), e00996-19.