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MedChemExpressModel IST5-002 -13484-66-7

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IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML)[1].
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IST5-002

MCE China:IST5-002

Brand:MedChemExpress (MCE)

Cat. No.HY-19527

CAS:13484-66-7

Synonyms:N6-Benzyladenosine-5'-phosphate

Purity:99.36%

Storage:Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description:IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cell apoptotic and death of prostate cancer cells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostate cancer and chronic myeloid leukemia (CML).

In Vitro:IST5-002 (1.5-25 μM, 2 h) inhibits transcriptional activity of Stat5a and Stat5b in a dose-dependent manner[1]. IST5-002 (0-40 μM, 3 h) inhibits Bcr-Abl-induced Stat5a/b phosphorylation in K562 cells[1]. IST5-002 (5-100 μM, 2 h) inhibits Stat5a/b phosphorylation in T47D cells, and inhibits dimerization in PC-3 cells[1]. IST5-002 (5-100 μM, 2 h) suppresses Stat5 nuclear translocation in PC-3 cells, and inhibits DNA binding of Stat5 target genes and COS-7 cells[1]. IST5-002 (2-50 μM, 48 h) reduces expression of Stat5a/b target genes (Bcl-xL and cyclin D1) in CWR22Rv1 and LNCaP cells[1]. IST5-002 (3.1-50 μM, 72 h) inhibits cell growth through induction of apoptosis in human prostate cancer cells[1]. IST5-002 (25-100 μM, 7 days) induces epithelial cell death in patient-derived prostate cancers ex vivo in organ explant cultures[1]. IST5-002 (5 μM, 24-72h) inhibits Stat5a/b phosphorylation and induces apoptosis of Imatinib (HY-15463)-sensitive and -resistant CML cells[1].

In Vivo:RORγt inverse agonist 29 (intraperitoneal injection, 25-100 mg/kg, daily for 10 days) inhibits tumor growth in prostate cancer xenograft model[1].

IC50 & Target:STAT5a 1.5 μM (IC50) STAT5b 3.5 μM (IC50)

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References:

[1]. Zhiyong Liao, et al. Structure-Based Screen Identifies a Potent Small Molecule Inhibitor of Stat5a/b with Therapeutic Potential for Prostate Cancer and Chronic Myeloid Leukemia. Mol Cancer Ther. 2015 Aug;14(8):1777-93.  [Content Brief]

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