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Chemical Structure| 220036-08-8 Chemical Structure| 220036-08-8

Structure of NU6027
CAS No.: 220036-08-8

Chemical Structure| 220036-08-8

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NU6027 is a potent ATR/CDK inhibitor, inhibits CDK1/2, ATR and DNA-PK with Ki of 2.5 μM/1.3 μM, 0.4 μM and 2.2 μM, enter cells more readily than the 6-aminopurine-based inhibitors.

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Product Details of NU6027

CAS No. :220036-08-8
Formula : C11H17N5O2
M.W : 251.29
SMILES Code : NC1=NC(OCC2CCCCC2)=C(N=O)C(N)=N1
MDL No. :MFCD05664735
InChI Key :DGWXOLHKVGDQLN-UHFFFAOYSA-N
Pubchem ID :398148

Safety of NU6027

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of NU6027

Hedgehog

Isoform Comparison

Biological Activity

Target
  • CDK2

    CDK2, Ki:1.3 μM

  • CDK1

    CDK1, Ki:2.5 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
RAW 264.7 murine macrophages 10 µM 1 hour NU6027 inhibited ATR signaling and prevented TVX-mediated increases in LPS-induced TNF mRNA and protein release J Pharmacol Exp Ther. 2014 Jul;350(1):164-70.
CP70-B1 and CP70-A2 cells 4 µM and 10 µM 24 hours NU6027 enhanced temozolomide cytotoxicity, with greater effects in MMR-proficient CP70-B1 cells Br J Cancer. 2011 Jul 26;105(3):372-81.
A2780 cells 4 µM and 10 µM 24 hours NU6027 significantly enhanced cisplatin cytotoxicity, with greater effects in p53 wild-type cells Br J Cancer. 2011 Jul 26;105(3):372-81.
MCF7 cells 6.7 µM (IC50 ) 24 hours NU6027 inhibits ATR activity with an IC50 of 6.7 μM Br J Cancer. 2011 Jul 26;105(3):372-81.
GM847KD cells 2.8 µM (IC50 ) 24 hours NU6027 inhibits ATR activity with an IC50 of 2.8 μM Br J Cancer. 2011 Jul 26;105(3):372-81.
Mouse cortical neurons 1 µM 24 hours NU6027 significantly reduced H2O2-induced neuronal death, confirmed by LDH release and PI staining. Mol Neurobiol. 2019 Apr;56(4):2822-2835.
THP-1 macrophages 25 µM 4 days NU-6027 inhibits growth of M. bovis BCG and M. tuberculosis in macrophages Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00996-19.
M. bovis BCG 1.56 µM (IC99 ) 7 days NU-6027 inhibits M. bovis BCG growth in a dose- and time-dependent manner Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00996-19.
HEK293 cells 1 µM NU6027 inhibited TRPC5-mediated currents, indicating a direct action on TRPC5 channels. Mol Neurobiol. 2019 Apr;56(4):2822-2835.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Sprague-Dawley rats Traumatic brain injury (TBI) model Intraperitoneal injection 1 mg/kg Immediately injected once, continued for one week NU6027 reduces TBI-induced neuronal death, zinc accumulation, oxidative stress, and glial activation by inhibiting TRPC5 channels and improves cognitive function Int J Mol Sci. 2020 Nov 4;21(21):8256
BALB/c mice Tuberculosis infection model Oral 100 mg/kg 5 days a week for 4 weeks NU-6027 inhibits M. tuberculosis growth in Mice tissues Antimicrob Agents Chemother. 2019 Aug 23;63(9):e00996-19.
Sprague-Dawley rats KA-induced seizure model Intraperitoneal injection 100 μg/kg Single dose, observed for 24 hours NU6027 significantly reduced mortality and neuronal death in KA-induced epileptic rats. Mol Neurobiol. 2019 Apr;56(4):2822-2835.

Protocol

Bio Calculators
Preparing Stock Solutions 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

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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