ERGi-USU (NSC139021)

Chemical Structure : ERGi-USU

CAS No.: 1147-56-4

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

ERGi-USU (NSC 139021) 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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100 mg	$48	In stock
250 mg	$78	In stock
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Biological Activity

ERGi-USU (NSC 139021) 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.