ZMC2
ZMC2 is a thiosemicarbazone-class metal ion chelator and zinc ionophore with a human mutant p53R175H binding Ka of 27.4 nM.ZMC2 binds Fe, Cu, Mn, Zn, and other transition metals.ZMC2 facilitates zinc transport across membranes.ZMC2 restores zinc binding to zinc-deficient p53 mutants, restoring wild-type structure and function, including site-specific DNA binding.ZMC2 generates reactive oxygen species (ROS).ZMC2 can be used for the research of cancer.
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- CAS No.: 71555-14-1
- Formule: C10H14N4S
- Masse moléculaire:222.31
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 41M | IC50 |
0.22 nM
Compound: 1
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Cytotoxicity against human 41M cells after 96 hrs by MTT assay
Cytotoxicity against human 41M cells after 96 hrs by MTT assay
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[PMID: 17315858] |
| HuT78 | ED50 |
0.55 ng/mL
Compound: 28
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Compound was evaluated for inhibition of Herpes simplex virus -1 (HSV-1) - induced cytopathic effect in HUT78 cells (in vitro)
Compound was evaluated for inhibition of Herpes simplex virus -1 (HSV-1) - induced cytopathic effect in HUT78 cells (in vitro)
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[PMID: 1354751] |
| MT4 | ED50 |
0.11 ng/mL
Compound: 28
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Compound was evaluated for inhibition of HIV-1- induced cytopathic effect in MT-4 cells (in vitro)
Compound was evaluated for inhibition of HIV-1- induced cytopathic effect in MT-4 cells (in vitro)
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[PMID: 1354751] |
| SK-BR-3 | IC50 |
2.7 nM
Compound: 1
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Cytotoxicity against human SKBR3 cells after 96 hrs by MTT assay
Cytotoxicity against human SKBR3 cells after 96 hrs by MTT assay
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[PMID: 17315858] |
| SK-N-MC | IC50 |
0.001 μM
Compound: HAp44mT
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Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
Antiproliferative activity against human SK-N-MC cells after 72 hrs by MTT assay
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[PMID: 19216562] |
| TOV112D | EC50 |
0.001 μM
Compound: A1
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Growth inhibition of human TOV112D cells harbouring p53 R175H mutant incubated for 3 days by MTS assay
Growth inhibition of human TOV112D cells harbouring p53 R175H mutant incubated for 3 days by MTS assay
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[PMID: 33538587] |
ZMC2 (>1 h (room temperature)) binds Zn2+ with an apparent Kd of 27.4 nM, an affinity compatible with functioning as a zinc metallochaperone in cell-free conditions[1].
ZMC2 (180 μM; 20 min (on ice)) restores Zn2+ content to apoized WT and p53-R175H DBD proteins, promoting a native, non-misfolded conformation in cell-free conditions[1].
ZMC2 (4-fold molar excess relative to DBD; added after ~60 s of stalled refolding) efficiently rescues the folding of Zn2+-trapped misfolded WT and p53-R175H DBD proteins in cell-free conditions[1].
ZMC2 (20 μM), in combination with ZnCl2, restores site-specific DNA binding activity to apo p53-R175H DBD in cell-free conditions[1].
ZMC2 (1 μM; monitored over 600 s (room temperature)) functions as a Zn2+ ionophore, facilitating specific Zn2+ transport across DOPC liposome membranes without causing non-specific leakage in cell-free conditions[1].
ZMC2 (0.0001-10 μM; 3 days) potently inhibits the growth of p53R175H and p53R175L mutant human tumor cell lines (EC50 0.009-0.168 μM) in a p53-dependent manner, with minimal activity in p53 null or WT cell lines[1].
ZMC2 (0.1-1 μM; 6 hours) completely abrogates long-term colony formation by p53-R175H TOV112D cells after 10 days of drug-free culture[1].
ZMC2 (1 μM; 6 hours) induces a WT-like conformational change in the mutant p53 protein in p53R175H TOV112D and SKBR3 cells[1].
ZMC2 (1 μM; 6 h, 24 h) restores wild-type p53 transcriptional function in p53R175H TOV112D and SKBR3 cells, significantly increasing mRNA levels of the p53 target genes p21 and PUMA at 6 hours post-treatment, with p21 mRNA levels declining by 24 hours, while p21 protein levels remain elevated through 24 hours[1].
ZMC2 (1 μM; 24 hours) induces cellular ROS levels by ~3-fold above baseline in p53-R175H TOV112D cells and also induces significant ROS levels in p53 null H1299 cells after 24 hours of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human tumor cell lines TOV112D (p53-R175H), SKBR3 (p53-R175H), HOP92 (p53-R175L), H1299 (p53 null), H460 (p53 WT)
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Concentration:0.0001-10 μM; up to 2 μM for H1299 and H460
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Incubation Time:3 days
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Result:Exhibited preferential growth inhibition in p53 mutant cell lines, with EC50 values of 0.087 μM (TOV112D), 0.009 μM (SKBR3), and 0.168 μM (HOP92).
EC50 values were not reached in p53 null (H1299) or p53 WT (H460) cell lines at concentrations tested.
p53 knockdown via siRNA abrogated this preferential sensitivity in TOV112D cells.
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Cell Line:TOV112D (p53-R175H) human tumor cell line
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Concentration:0.1-1 μM
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Incubation Time:6 hours; followed by 10 days of drug-free culture
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Result:Completely inhibited colony formation in TOV112D cells after 10 days of drug-free culture at 0.1 μM and 1 μM.
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Cell Line:TOV112D and SKBR3 (p53-R175H) human tumor cell lines
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Concentration:1 μM
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Incubation Time:6 hours
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Result:Induced a conformation change in p53-R175H protein, resulting in increased recognition by the WT-specific PAB1620 antibody and reduced recognition by the mutant-specific PAB240 antibody in both TOV112D and SKBR3 cells.
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Cell Line:TOV112D (p53-R175H) and H1299 (p53 null) human tumor cell lines
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Concentration:1 μM
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Incubation Time:24 hours
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Result:Increased 8-oxy-dG staining by ~3-fold relative to baseline in TOV112D cells, indicating a significant induction of cellular ROS.
Induced a significant increase in 8-oxy-dG staining in H1299 cells.
Chemical Information
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CAS No. 71555-14-1
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Masse moléculaire 222.31
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Formule C10H14N4S
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SMILES
S=C(NN=C(C1=NC=CC=C1)C)N(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)