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CAS No. : 868612-83-3
MCE 国际站:IN-1130
产品活性:N-1130 是一种高度选择性的转化生长因子-β I 型受体激酶 (ALK5) 抑制剂,对 ALK5 介导的 Smad3 磷酸化的 IC50 为 5.3 nM。IN-1130 抑制酪蛋白的 ALK5 磷酸化 (IC50=36 nM),抑制 p38α 丝裂原活化的蛋白激酶 (IC50=4.3 μM)。IN-1130 可抑制阻塞性肾病中的肾纤维化,阻止乳腺癌的肺转移。
研究领域:TGF-beta/Smad
作用靶点:TGF-β Receptor
In Vitro: IN-1130 (0.5, 1 μM; for 2 hours) inhibits TGF-β-stimulated Smad2 phosphorylation and subsequent nuclear translocation in HepG2 and 4T1 cells.
IN-1130 (1 μM; for 72 hours) restores the TGF-β-mediated decrease in E-cadherin protein expression. IN-1130 (1 μM; for 72 hours) inhibits TGF-β-induced MMPs mRNA expression and the gelatinolytic activity of secreted MMPs in MCF10A cells.
IN-1130 (1 μM; pretreated for 30 min) inhibits TGF-β-induced MDA-MB-231 cells, NMuMG, and MCF10A cells mobility and invasion.
In Vivo: IN-1130 (10, 20 mg/kg/day; IP; for 7 and 14 days) reduces the extent of interstitial nephritis and fibrosis (arrowheads) with 10 mg/kg and significantly reduces or absent histopathological changes with 20 mg/kg in unilateral ureteral obstruction (UUO) rats.
IN-1130 (10, 20 mg/kg/day; for 14 days) dose-dependently decreases levels of TGF-β1 mRNA and suppresses phosphorylation of Smad2, α-SMA, myofibroblasts in rat UUO kidneys.
IN-1130 (40 mg/kg; IP; 3 times per week for 3 weeks) inhibits in vivo breast cancer metastasis to the lungs in MMTV/c-Neu mice (Eight-week-old female BALB/c mice).
相关产品:Bioactive Compound Library Plus | Immunology/Inflammation Compound Library | Kinase Inhibitor Library | TGF-beta/Smad Compound Library | Anti-Cancer Compound Library | Reprogramming Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Obesity Compound Library | Angiogenesis-Related Compound Library | Transcription Factor-Targeted Library | Targeted Diversity Library | Anti-Colorectal Cancer Compound Library | Human Metabolite Library | Anti-Prostate Cancer Compound Library | Anti-Pulmonary Fibrosis Compound Library | Osteogenesis Compound Library | Cancer Stem Cells Compound Library | Heterocyclic Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | LSKL, Inhibitor of Thrombospondin (TSP-1) (TFA) | ML347 | Nadecnemab | Zilurgisertib | TGFβRI-IN-3 | Vactosertib | Itacnosertib | Trafermin | Maohuoside A | Metelimumab | Stamulumab | SB-505124 hydrochloride | K02288 | J-1063 | ALK5-IN-25 | LY-364947 | GW-6604 | TP-008 | ALK2-IN-4 | Galunisertib | CJJ300 | ALK5-IN-7 | ALK5-IN-32 | A 83-01 | RepSox (GMP) | A 77-01 | Dorsomorphin | OD36 | BMS-986260
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-18758
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