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保存条件 :Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
库存 :货期:1-2天
供应商 :MedChemExpress LLC
CAS号 :1334493-07-0
规格 :10 mM * 1 mL/5 mg/10 mg/50 mg
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BP-1-102
CAS No. : 1334493-07-0
MCE 国际站:BP-1-102
产品活性:BP-1-102 是有口服活性的转录因子 Stat3 的小分子抑制剂,其 IC50 值为 6.8 μM。
研究领域:JAK/STAT Signaling | Stem Cell/Wnt
作用靶点:STAT
In Vitro: BP-1-102 binds Stat3 with an affinity KD of 504 nM. BP-1-102 inhibits Stat3 DNA-binding activity in vitro, with an IC50 value of 6.8±0.8 μM. It blocks Stat3-phospho-tyrosine peptide interactions and Stat3 activation at 4-6.8 μM, and selectively inhibits growth, survival, migration, and invasion of Stat3-dependent tumor cells. BP-1-102-mediated inhibition of aberrantly active Stat3 in tumor cells suppresses the expression of c-Myc, Cyclin D1, Bcl-xL, Survivin, VEGF, and Krüppel-like factor 8.
In Vivo: Mice therapeutically given BP-1-102, an orally bioavailable compound targeting STAT3/NF-kB activation and cross-talk, exhibit reduced colon tumorigenesis and diminished expression of STAT3/NF-kB-activating cytokines in the neoplastic areas. BP-1-102 is orally bioavailable and that the agent accumulates in tumor tissues at levels sufficient to inhibit aberrantly active Stat3 functions and inhibit tumor growth.
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