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Description: Rio2 kinase (RIOK2) inhibitor; inhibits ERG protein
Chemical Name: 1-[2-(2-Thiazolyl)diazenyl]-2-naphthalenol
Purity: ≥99% (HPLC)
Biological Activity for ERGi-USU
ERGi-USU is a high affinity Rio Kinase 2 (RIOK2) inhibitor (Kd = 200 nM). Exhibits >6-fold selectivity for RIOK2 over a panel of 456 kinases. Inhibits ERG protein and potently inhibits growth of ERG-positive VCaP prostate cancer cells in vitro (IC50 = 169 nM) but not ERG-negative cell lines. Also inhibits growth of VCaP xenografts in mice.
Technical Data for ERGi-USU
| M. Wt | 255.3 |
| Formula | C13H9N3OS |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 1147-56-4 |
| PubChem ID | 6308684 |
| InChI Key | GCBAKGGJQPMJLL-QINSGFPZSA-N |
| Smiles | OC1=C(C2=CC=CC=C2C=C1)/N=N/C3=NC=CS3 |
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 ERGi-USU
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 25.53 | 100 |
Preparing Stock Solutions for ERGi-USU
The following data is based on the product molecular weight 255.3. 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 | 3.92 mL | 19.58 mL | 39.17 mL |
| 5 mM | 0.78 mL | 3.92 mL | 7.83 mL |
| 10 mM | 0.39 mL | 1.96 mL | 3.92 mL |
| 50 mM | 0.08 mL | 0.39 mL | 0.78 mL |
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Product Datasheets for ERGi-USU
References for ERGi-USU
References are publications that support the biological activity of the product.
Mohamed et al (2018) Identification of a small molecule that selectively inhibits ERG-positive cancer cell growth. Cancer Res. 78 3659 PMID: 29712692
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Keywords: ERGi-USU, ERGi-USU supplier, Rio2, kinase, RIOK2, atypical, protein, aPK, ribosome, biogenesis, inhibitors, inhibits, high, affinity, ERG, prostate, cancer, Other, Kinases, 6632, Tocris Bioscience
1 Citation for ERGi-USU
Citations are publications that use Tocris products. Selected citations for ERGi-USU include:
Marc et al (2021) Extracellular signal-regulated kinase mediates chromatin rewiring and lineage transformation in lung cancer. Elife 10 PMID: 34121659
Do you know of a great paper that uses ERGi-USU from Tocris? Please let us know.
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