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IST5-002

Chemical Structure : IST5-002

CAS No.: 13484-66-7

IST5-002 (Inhibitor of Stat5-002, N6-Benzyladenosine-5'-phosphate)

Catalog No.: PC-20634Not For Human Use, Lab Use Only.

IST5-002 is a specific small molecule taregeting STAT5 SH2-domain, inhibits both Stat5a/b phosphorylation and dimerization, robustly inhibits transcriptional activity of Stat5a (IC50=1.5 μM) and Stat5b (IC50=3.5 μM) in PC-3 cells.

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Biological Activity

IST5-002 is a specific small molecule taregeting STAT5 SH2-domain, inhibits both Stat5a/b phosphorylation and dimerization, robustly inhibits transcriptional activity of Stat5a (IC50=1.5 μM) and Stat5b (IC50=3.5 μM) in PC-3 cells.
IST5-002 blocks Bcr-Abl-induced Stat5a/b phosphorylation at 5 μM in Bcr-Abl-positive K562 cells.
IST5-002 blocks phosphorylation of Stat5a/b (CWR22Rv1, IC50=22 μM; HC-11, IC50=12 μM; T47D, IC50=24.8 μM), while total Stat5a/b levels remains unaffected.
IST5-002 shows no specific inhibition of other kinases in a panel of 50 kinases, does not block transcriptional activity of Stat3.
IST5-002 suppresses downstream signaling events and target gene expression induced by Stat5a/b in PC and CML cells.
IST5-002 suppresses Stat5a/b-mediated growth of PC through induction of apoptosis in experimental models of PC in vitro, in vivo and ex vivo.

Physicochemical Properties

M.Wt 437.34
Formula C17H20N5O7P
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

((2R,3S,4R,5R)-5-(6-(benzylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methyl dihydrogen phosphate

References

1. Liao Z, et al. Mol Cancer Ther. 2015 Aug;14(8):1777-93.

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