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ERGi-USU

Chemical Structure : ERGi-USU

CAS No.: 1147-56-4

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ERGi-USU (NSC139021)

Catalog No.: PC-63456Not For Human Use, Lab Use Only.

NSC139021 (NSC 139021, ERGi-USU) is a specific RIOK2 inhibitor, selectively inhibits ERG-positive cancer cell growth, directly binds (Kd=200 nM) and inhibits RIOK2 protein with IC50 of 220 nM (VCaP) and 360 nM (COLO320).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

NSC139021 (NSC 139021, ERGi-USU) is a specific RIOK2 inhibitor, selectively inhibits ERG-positive cancer cell growth, directly binds (Kd=200 nM) and inhibits RIOK2 protein with IC50 of 220 nM (VCaP) and 360 nM (COLO320).
ERGi-USU selectively inhibited growth of ERG-positive cancer cell lines with minimal effect on normal prostate or endothelial cells or ERG-negative tumor cell lines.
Combination of ERGi-USU with enzalutamide showed additive effects in inhibiting growth of VCaP cells.
ERGi-USU directly bound the ribosomal biogenesis regulator atypical kinase RIOK2 and induced ribosomal stress signature.
ERGi-USU treatment inhibited growth of ERG-positive VCaP tumor xenografts with no apparent toxicity.
ERGi-USU acts as a highly selective inhibitor for the growth of ERG-positive cancer cells and has potential for further development of ERG-targeted therapy of prostate cancer and other malignancies.

Physicochemical Properties

M.Wt 255.295
Formula C13H9N3OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-[2-Thiazolylazo]-2-naphthol

References

1. Mohamed AA, et al. Cancer Res. 2018 Apr 30. pii: canres.2949.2017.

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