ZMC2 

ZMC2 is a thiosemicarbazone-class metal ion chelator and zinc ionophore with a human mutant p53^R175H binding K_a 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^[1].

ZMC2 (>1 h (room temperature)) binds Zn²⁺ with an apparent K_d 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 p53^R175H and p53^R175L 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 p53^R175H TOV112D and SKBR3 cells^[1].
ZMC2 (1 μM; 6 h, 24 h) restores wild-type p53 transcriptional function in p53^R175H 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.

222.31

C₁₀H₁₄N₄S

71555-14-1

S=C(NN=C(C1=NC=CC=C1)C)N(C)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Yu X, et al. Thiosemicarbazones Functioning as Zinc Metallochaperones to Reactivate Mutant p53. Mol Pharmacol. 2017;91(6):567-575.  [Content Brief]