Biological Activity
Nitric oxide-independent activator of soluble guanylyl cyclase (sGC). Significantly elevates cGMP levels and inhibits collagen-stimulated aggregation of washed rabbit platelets (IC50 = 14.6 μM); induces relaxation in denuded phenylephrine-contracted rabbit aortic rings (EC50 = 1.9 μM). Also displays antiproliferative activity in vitro and in vivo by inducing G1 cell cycle arrest in two human hepatocellular carcinoma (HCC) cell lines, and in HCC xenografts in athymic SCID mice. Exhibits low cytotoxicity in non-malignant cells.
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Technical Data
M. Wt | 304.34 |
Formula | C19H16N2O2 |
Storage | Store at RT |
Purity | ≥99% (HPLC) |
CAS Number | 170632-47-0 |
PubChem ID | 5712 |
InChI Key | OQQVFCKUDYMWGV-UHFFFAOYSA-N |
Smiles | OCC4=CC=C(O4)C2=NN(CC3=CC=CC=C3)C1=CC=CC=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 30.43 | 100 | |
ethanol | 15.22 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 304.34. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 3.29 mL | 16.43 mL | 32.86 mL |
5 mM | 0.66 mL | 3.29 mL | 6.57 mL |
10 mM | 0.33 mL | 1.64 mL | 3.29 mL |
50 mM | 0.07 mL | 0.33 mL | 0.66 mL |
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References
References are publications that support the products' biological activity.
Ko et al (1994) YC-1, a novel activator of platelet guanylate cyclase. Blood. 84 4226 PMID: 7527671
Martin et al (2001) YC-1 activation of human soluble guanylyl cyclase has both heme-dependent and heme-independent components. Proc.Natl.Sci.U.S.A. 98 12938 PMID: 11687640
Wang et al (2005) YC-1 [3-(5'-hydroxymethyl-2'-furyl)-1-benzyl indazole] exhibits a novel antiproliferative effect and arrests the cell cycle in G0-G1 in human hepatocellular carcinoma cells. J.Pharmacol.Exp.Ther. 312 917 PMID: 15525795
Teixeira et al (2006) Molecular mechanisms underlying rat mesenteric artery vasorelaxation induced by the nitric oxide-independent soluble guanylyl cyclase stimulators BAY 41-2272 [5-cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4 J.Pharmacol.Exp.Ther. 317 258 PMID: 16352702
Keywords: YC 1, supplier, YC1, soluble, guanylyl, cyclase, sGC, activators, platelet, aggregation, cGMP, antiproliferatives, G1, cell, cycle, arrest, inducers, p21, CDK2, Guanylyl, Cyclase, Cell, Cycle, Inhibitors, Enzyme, Substrates, /, Activators, Guanylyl, Cyclase, Tocris Bioscience