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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.
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | JAK/STAT Compound Library | Kinase Inhibitor Library | Stem Cell Signaling Compound Library | Anti-Cancer Compound Library | Small Molecule Immuno-Oncology Compound Library | Anti-Aging Compound Library | Differentiation Inducing Compound Library | Orally Active Compound Library | Anti-Breast Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Obesity Compound Library | Transcription Factor-Targeted Library | Targeted Diversity Library | Anti-Liver Cancer Compound Library | Anti-Prostate Cancer Compound Library | Cancer Stem Cells Compound Library | Highly Selective Inhibitors Library | 8α-Tigloyloxyhirsutinolide 13-O-acetate | Stafia-1-dipivaloyloxymethyl ester | Niclosamide monohydrate | Brevilin A | STAT3 degrader-1 | NSC-370284 | Broussonin E | RO8191 | Eflepedocokin alfa | Morusin | STAT3-IN-13 | Antitumor agent-73 | 1-(4-Chloro-3-(trifluoromethyl)phenyl)-3-(4-(4-cyanophenoxy)phenyl)urea | IST5-002 | Delphinidin chloride | SC-43 | Astaxanthin | LLL12 | MNK8 | Syk-IN-6 | STAT5-IN-2 | (+)-Ochromycinone | STAT3-IN-11 | HP590 | FLLL32 | SI-109 | Stafib-2 | SD-1029 | SH-4-54 | Colivelin
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货号: HY-100493
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