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Chemical Structure| 71555-25-4 Chemical Structure| 71555-25-4

Structure of NSC319726
CAS No.: 71555-25-4

Chemical Structure| 71555-25-4

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NSC319726 is a mutant p53R175 reactivator inhibiting growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM) and showing no inhibition for p53 wild-type cells.

Synonyms: ZMC1

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Product Details of NSC319726

CAS No. :71555-25-4
Formula : C11H14N4S
M.W : 234.32
SMILES Code : S=C(N1CCC1)N/N=C(C2=NC=CC=C2)\C
Synonyms :
ZMC1
MDL No. :MFCD01665446

Safety of NSC319726

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

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Glioblastoma-patient-derived cells 12 pM to 25 nM 48 hours NSC319726 induces oxidative stress and cell cycle arrest by binding copper Cell Chem Biol. 2018 May 17;25(5):585-594.e7.
MEF p53R172H/R172H 1 µM 24 hours evaluates the growth inhibitory effect of NSC319726 on mouse p53R172H mutant cells Cancer Cell. 2012 May 15;21(5):614-625.
SKOV3 (p53−/−) 1 µM 24 hours evaluates the growth inhibitory effect of NSC319726 on p53 null cells Cancer Cell. 2012 May 15;21(5):614-625.
OVCAR3 (p53R248W) 1 µM 24 hours evaluates the growth inhibitory effect of NSC319726 on p53R248W mutant cells Cancer Cell. 2012 May 15;21(5):614-625.
TOV112D (p53R175H) 1 µM 24 hours induces a WT-like conformational change in the p53R175H mutant protein and apoptosis Cancer Cell. 2012 May 15;21(5):614-625.
TOV112D 1 μM 72 hours Evaluate the synergy of ZMC1 with cytotoxic chemotherapy or radiation, results showed that ZMC1 alone was effective but did not show synergy when combined with chemotherapy or radiation. Mol Cancer Ther. 2019 Aug;18(8):1355-1365.
Escherichia coli 10 μg/mL 16-20 hours To evaluate the antimicrobial activity of NSC319726 against E. coli AHDRCC 81113, showing an IC50 of 5.432 ± 2.731 μg/mL (0.0232 ± 0.012 μM). Biomolecules. 2018 Dec 7;8(4):166.
TOV112D cells 1 μM 4 hours Monitor ZMC1-induced refolding of p53 mutants Elife. 2020 Dec 2;9:e61487.
H1299 cells 0.002 μM – 0.005 μM Test the cell-killing effect of ZMC1 on p53 mutants Elife. 2020 Dec 2;9:e61487.
H460 >2 μM 3 days Assessed cell growth inhibition, showing low toxicity to p53 wild-type cells Mol Pharmacol. 2017 Jun;91(6):567-575.
H1299 >2 μM 3 days Assessed cell growth inhibition, showing low toxicity to p53 null cells Mol Pharmacol. 2017 Jun;91(6):567-575.
HOP92 0.291 μM 3 days Assessed cell growth inhibition, showing specific toxicity to p53-R175L mutant cells Mol Pharmacol. 2017 Jun;91(6):567-575.
SKBR3 0.009 μM 3 days Assessed cell growth inhibition, showing specific toxicity to p53-R175H mutant cells Mol Pharmacol. 2017 Jun;91(6):567-575.
TOV112D 0.087 μM 3 days Assessed cell growth inhibition, showing specific toxicity to p53-R175H mutant cells Mol Pharmacol. 2017 Jun;91(6):567-575.
HT-1080 fibrosarcoma cells 31 nM 48 hours NSC319726 induces cell growth inhibition via a copper-dependent mechanism Cell Chem Biol. 2018 May 17;25(5):585-594.e7.
HCT116 cells 1 μM To evaluate the effect of NSC319726 on cell viability, results showed that NSC319726 reduced cell survival. Cell Biol Toxicol. 2024 May 1;40(1):26.
UOK276 cells 1 nM or 10 nM 90 hours Assessed the effect of NSC319726 on UOK276 cell invasion, showing dose-dependent suppression of invasion. Genes Chromosomes Cancer. 2017 Oct;56(10):719-729.
UOK276 cells 10 nM 5 days Evaluated the effect of NSC319726 on UOK276 cell growth, showing approximately 70% reduction in growth over 5 days. Genes Chromosomes Cancer. 2017 Oct;56(10):719-729.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice P53R172H/R172H knock-in mice Intraperitoneal injection 10 mg/kg/day or 5 mg/kg/day Daily for up to 7 days Evaluates the toxicity and therapeutic effect of NSC319726 on p53R172H mutant mice, showing p53R172H/R172H mice are more sensitive to NSC319726 Cancer Cell. 2012 May 15;21(5):614-625.
Nude mice NCR nu/nu TOV112D xenograft model Intraperitoneal injection 2.5 mg/kg Daily for 17 days Evaluate the in vivo synergy of ZMC1 with Nutlin 3a or ABT-199, results showed that ZMC1 combined with Nutlin 3a or ABT-199 significantly inhibited tumor growth. Mol Cancer Ther. 2019 Aug;18(8):1355-1365.
Nude mice Xenograft tumor model Intraperitoneal injection 5 mg/kg Daily Test the efficacy of ZMC1 on p53 stability mutants in vivo Elife. 2020 Dec 2;9:e61487.
Galleria mellonella larvae C. auris infection model Injection 6 and 12 mg/kg Single dose, observed for 72 hours Evaluation of the efficacy of NSC319726 in an invertebrate infection model, showing significantly improved survival rates compared to the untreated group Microbiol Spectr. 2021 Dec 22;9(3):e0139521
ICR mice Male reproductive system injury model Intraperitoneal injection 1 mg/kg Once daily for 5 weeks To evaluate the toxicity of NSC319726 on the male reproductive system, results showed that NSC319726 caused testis index reduction, decreased sperm count, increased sperm malformation rate, structural damage in the testis and epididymis, impaired blood-testis barrier integrity, and decreased testosterone levels. Cell Biol Toxicol. 2024 May 1;40(1):26.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.27mL

0.85mL

0.43mL

21.34mL

4.27mL

2.13mL

42.68mL

8.54mL

4.27mL

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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