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Biological Activity for Cysmethynil
Cysmethynil is an isoprenylcysteine carboxylmethyltransferase (ICMT) inhibitor (IC50 = 2.4 μM). Cysmethynil reduces growth of RAS-mutant cell lines in vitro and in vivo (EC50 = 20 μM) and reduces cell viability in a variety of cell lines (IC50 = 16.8-23.3 μM). Tumor growth, mTOR signaling and cell proliferation are inhibited by cysmethynil; apoptosis is induced. Cysmethynil increases p27 and p21 proteins and arrests cell-cycle at the G1 phase.
Technical Data for Cysmethynil
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Cysmethynil
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Cysmethynil
The following data is based on the product molecular weight 376.54. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.66 mL||13.28 mL||26.56 mL|
|5 mM||0.53 mL||2.66 mL||5.31 mL|
|10 mM||0.27 mL||1.33 mL||2.66 mL|
|50 mM||0.05 mL||0.27 mL||0.53 mL|
References for Cysmethynil
References are publications that support the biological activity of the product.
Moore et al (2020) RAS-targeted therapies: is the undruggable drugged? Nat.Rev.Drug Discov. 19 533 PMID: 32528145
Manu et al (2017) Inhibition of isoprenylcysteine carboxylmethyltransferase induces cell-cycle arrest and apoptosis through p21 and p21-regulated BNIP3 induction in pancreatic cancer. Mol.Cancer Ther. 16 914 PMID: 28167504
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Keywords: Cysmethynil, Cysmethynil supplier, ICMT, isoprenylcysteine, carboxymethyltransferase, inhibitors, inhibits, apoptosis, p27, p21, G1, cell, cycle, arrests, RAS, mutant, Other, Transferases, Cell, Cycle, Inhibitors, 7337, Tocris Bioscience
Citations for Cysmethynil
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