IST5-002，一种有效的
Stat5a/b抑制剂，选择性地抑制 Stat5a/b 的转录活性，
IC50值分别为 1.5 μM (Stat5a) 和 3.5 μM (Stat5b)。 IST5-002 诱导前列腺癌细胞和慢性粒细胞白血病 (CML) 细胞凋亡 (
apoptotic) 和死亡。IST5-002 可用于前列腺癌和慢性粒细胞白血病 (CML) 的研究。
| 生物活性 |
IST5-002, a potentStat5a/binhibitor, selectively inhibits transcriptional activity of Stat5a/b (IC50s: 1.5 μM for Stat5a, 3.5 μM for Stat5b). IST5-002 inducs cellapoptoticand death of prostatecancercells and chronic myeloid leukemia (CML) cells. IST5-002 can be used in the research of prostatecancerand chronic myeloid leukemia (CML)[1].
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| IC50& Target[1] |
STAT5a 1.5 μM (IC50) |
STAT5b 3.5 μM (IC50) |
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体外研究
(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 cancersex vivoin 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].
Cell Viability Assay[1]
| Cell 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 Analysis[1]
| Cell 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 Analysis[1]
| Cell 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. |
Immunofluorescence[1]
| Cell Line: |
PC-3 cells |
| Concentration: |
5, 10, 15. 20, 40 μM |
| Incubation Time: |
2 h |
| Result: |
Inhibited Prl (Prolactin)-induced nuclear translocation of Stat5. |
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体内研究
(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].
| Animal Model: |
Prostate cancer (CWR22Rv1) xenograft model[1] |
| 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. |
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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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