IST5-002

IST5-002, a potent Stat5a/b inhibitor, selectively inhibits transcriptional activity of Stat5a/b ( IC 50 s: 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. IST5-002 (0-40 μM, 3 h) inhibits Bcr-Abl-induced Stat5a/b phosphorylation in K562 cells. IST5-002 (5-100 μM, 2 h) inhibits Stat5a/b phosphorylation in T47D cells, and inhibits dimerization in PC-3 cells. 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. IST5-002 (2-50 μM, 48 h) reduces expression of Stat5a/b target genes (Bcl-xL and cyclin D1) in CWR22Rv1 and LNCaP cells. IST5-002 (3.1-50 μM, 72 h) inhibits cell growth through induction of apoptosis in human prostate cancer cells. IST5-002 (25-100 μM, 7 days) induces epithelial cell death in patient-derived prostate cancers ex vivo in organ explant cultures. IST5-002 (5 μM, 24-72h) inhibits Stat5a/b phosphorylation and induces apoptosis of Imatinib -sensitive and -resistant CML cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: CWR22Rv1, LNCaP, and DU145 cells Concentration: 3.1, 6.3, 12.5, 25, 50 μM Incubation Time: 72 h Result: Decreased viable cells by 50% to 80% at 12.5 μM. Cell Cycle AnalysisCell Line: LNCaP and CWR22Rv1 cells Concentration: 6, 12, 25 μM Incubation Time: 72 h Result: Increased the fraction of dead cells (sub-G1) and decreased the fraction of living cells (G2–M). Western Blot AnalysisCell Line: Bcr-Abl–positive K562 cells Concentration: 0, 1, 5, 10, 20, 40 μM Incubation Time: 3 h Result: Inhibited Bcr-Abl-induced Stat5a/b phosphorylation at 5 μM, without affecting Bcr-Abl tyrosine phosphorylation levels. ImmunofluorescenceCell Line: PC-3 cells Concentration: 5, 10, 15. 20, 40 μM Incubation Time: 2 h Result: Inhibited Prl (Prolactin)-induced nuclear translocation of Stat5. In Vivo RORγt inverse agonist 29 (intraperitoneal injection, 25-100 mg/kg, daily for 10 days) inhibits tumor growth in prostate cancer xenograft model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Prostate cancer (CWR22Rv1) xenograft model Dosage: 25, 50, and 100 mg/kg Administration: Intraperitoneal injection, daily for 10 days Result: Induced massive loss of viable tumor cells and dead rounded cells accumulation. Induced cell death through apoptosis (shown by fragmented DNA in tumor sections). Decreased nuclear Stat5a/b content by 60%, 78%, and 90% at 25, 50, and 100 mg/kg, respectively. IC50& Target:STAT5a 1.5 μM (IC 50 ) STAT5b 3.5 μM (IC 50 )

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet