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Chemical Structure| 309271-94-1 Chemical Structure| 309271-94-1

Structure of Inauhzin
CAS No.: 309271-94-1

Chemical Structure| 309271-94-1

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Inauhzin is a small molecule that effectively reactivates p53 by inhibiting SIRT1 activity, and promotes p53-dependent apoptosis of human cancer cells without causing apparently genotoxic stress (IC50=3 μM, in A549 cell).

Synonyms: INZ

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Product Details of Inauhzin

CAS No. :309271-94-1
Formula : C25H19N5OS2
M.W : 469.58
SMILES Code : CCC(SC1=NN=C2C(NC3=C2C=CC=C3)=N1)C(N4C5=C(C=CC=C5)SC6=CC=CC=C46)=O
Synonyms :
INZ
MDL No. :MFCD01819836
InChI Key :VHUOXERIKQWIJE-UHFFFAOYSA-N
Pubchem ID :5494506

Safety of Inauhzin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H317
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Inauhzin

epigenetics

Isoform Comparison

Biological Activity

Target
  • SIRT1

In Vitro:

Cell Line
Concentration Treated Time Description References
HCT116 cells 2 µM 6 hours Induced p53 levels and activity EMBO Mol Med. 2012 Apr;4(4):298-312.
H1299 cells 2 µM 24 hours INZ(c) treatment decreased c-Myc mRNA and protein levels. Cancer Biol Ther. 2015;16(3):412-9.
A549 cells 0.5 µM 18 hours Induced p53 levels and activity EMBO Mol Med. 2012 Apr;4(4):298-312.
H460 cells 10 µM 18 hours Induced p53 levels EMBO Mol Med. 2012 Apr;4(4):298-312.
A549 0.5 µM 18 hours Combined treatment of INZ and DOX significantly induced the level of p53, p21, and cleaved PARP Neoplasia. 2013 May;15(5):523-34.
HCT116p53+/+ 0.5 µM 18 hours Combined treatment of INZ and CIS or DOX significantly induced the level of p53, p21, and cleaved PARP Neoplasia. 2013 May;15(5):523-34.
H460 0.5 µM 18 hours Combined treatment of INZ and CIS or DOX significantly induced the level of p53, p21, and cleaved PARP Neoplasia. 2013 May;15(5):523-34.
A549 cells 1 µM 18 hours To test the effect of Inauhzin alone or in combination with Nutlin-3 on p53 levels and activity. Results showed that the combination of Inauhzin and Nutlin-3 significantly increased the levels of p53 and its target proteins p21 and cleaved PARP. Cancer Biol Ther. 2012 Aug;13(10):915-24.
H460 cells 1 µM 18 hours To test the effect of Inauhzin alone or in combination with Nutlin-3 on p53 levels and activity. Results showed that the combination of Inauhzin and Nutlin-3 significantly increased the levels of p53 and its target proteins p21 and cleaved PARP. Cancer Biol Ther. 2012 Aug;13(10):915-24.
HCT116 p53+/+ cells 0.5 µM and 1 µM 18 hours To test the effect of Inauhzin alone or in combination with Nutlin-3 on p53 levels and activity. Results showed that Inauhzin alone or in combination with Nutlin-3 significantly increased the levels of p53 and its target proteins p21, PUMA, and cleaved PARP. Cancer Biol Ther. 2012 Aug;13(10):915-24.
HCT116 p53+/+ and HCT116 p53−/− cells 4 µM 18 hours Microarray analysis identified TFIIS.h as a potential p53 target gene, induced by INZ only in HCT116 p53+/+ cells. Sci Rep. 2016 Mar 23;6:23542.
Vero E6 cells 12.96 µM (EC50) 22 hours To evaluate the inhibitory effect of Inauhzin on SARS-CoV-2 replication, results showed antiviral activity in the cell-based model with an EC50 of 12.96 μM. Biochem J. 2021 Jul 16;478(13):2481-2497.
Raji cells 0, 0.63, or 2.5 µM 24 hours INZ(c) significantly inhibited cell proliferation and viability. Cancer Biol Ther. 2015;16(3):412-9.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice HCT116 subcutaneous xenograft model Oral gavage 15 mg/kg and 30 mg/kg Every 2 days for 14 days To evaluate the inhibitory effect of Inauhzin on the growth of HCT116 xenografts. Results showed that Inauhzin significantly suppressed tumor volume and weight, induced apoptosis in tumor tissues, and had no significant toxic effects on body weight and major organs. Redox Biol. 2022 Jul;53:102334
SCID mice HCT116 p53+/+ xenograft tumor model Intraperitoneal injection for Inauhzin, oral administration for Nutlin-3 15 mg/kg Inauhzin + 150 mg/kg Nutlin-3 Inauhzin once daily, Nutlin-3 twice daily for 4 days followed by 2 days off, for 21 days To test the inhibitory effect of Inauhzin and Nutlin-3 combination on xenograft tumor growth. Results showed that the combination significantly reduced tumor volume and weight, and increased the levels of p53 and its target proteins. Cancer Biol Ther. 2012 Aug;13(10):915-24.
SCID mice H460 xenograft tumor model Intraperitoneal injection 20 mg/kg INZ once per day for 21 days; CIS once per week for 3 weeks Combined treatment of INZ and CIS significantly suppressed tumor growth, reducing tumor volume and weight Neoplasia. 2013 May;15(5):523-34.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.06mL

21.30mL

4.26mL

2.13mL

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

References

 

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