product name
A 83-01, ≥98% (HPLC)
质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 5 mg/mL, clear (warmed)
储存温度
−20°C
InChI
1S/C25H19N5S/c1-17-8-7-13-23(27-17)24-21(19-14-15-26-22-12-6-5-11-20(19)22)16-30(29-24)25(31)28-18-9-3-2-4-10-18/h2-16H,1H3,(H,28,31)
InChI key
HIJMSZGHKQPPJS-UHFFFAOYSA-N
一般描述
A-83-01 may effectively prevent burn wound contraction without impeding wound closure, due to its ability to inhibit the transforming growth factor-β (TGF-β)-induced rise in myofibroblast population. Additionally, it can hinder TGF-β1-dependent cancer metastasis by suppressing epithelial-mesenchymal transition (EMT) in animals.
应用
A 83-01已被用作转化生长因子β激酶1型受体的抑制剂。
A 83-01 has been used:
- in the culture medium for organoid formation from dissociated tumor cells,
- as a component in Dulbecco′s modified Eagle medium/nutrient mixture F-12 (DMEM/F12) for culturing human epidermal stem cells (EpSCs)
生化/生理作用
A 83-01是一种TGFβ激酶/激活素受体样激酶（ALK 5）的抑制剂（IC50= 12nM），可阻止Smad2/3的磷酸化并抑制TGFβ诱导的生长。 A 83-01可阻断Smad2的磷酸化并抑制TGF-β诱导的上皮-间质转化。 此外，A 83-01可抑制由TGFβI型受体ALK-5、活化素IB型受体ALK-4、和结节型I受体ALK-7诱导的转录活性。 A-83-01可诱导新生Nkx2.5-eGFP（+）细胞的扩增。
WGK
WGK 3
The Use of Endometrial Cancer Patient?Derived Organoid Culture for Drug Sensitivity Testing Is Feasible
Girda E, et al.
International Journal of Gynecological Cancer : Official Journal of the International Gynecological Cancer Society, 27(8), 1701-1701 (2017)
Topical application of ALK5 inhibitor A-83-01 reduces burn wound contraction in rats by suppressing myofibroblast population
Sun X, et al.
Bioscience, Biotechnology, and Biochemistry, 78, 1805-1812 (2014)
A83-01 inhibits TGF-Β-induced upregulation of Wnt3 and epithelial to mesenchymal transition in HER2-overexpressing breast cancer cells.
Wu Y, et al.
Breast Cancer Research and Treatment, 163(3), 449-460 (2017)
Personalized identification of optimal HIPEC perfusion protocol in patient-derived tumor organoid platform
Forsythe SD, et al.
Annals of Surgical Oncology, 27, 4950-4960 (2020)
Jin Seok et al.
Stem cell research & therapy, 11(1), 1-1 (2020-01-05)
Human placenta-derived mesenchymal stem cells (PD-MSCs) are powerful sources for cell therapy in regenerative medicine. However, a limited lifespan by senescence through mechanisms that are well unknown is the greatest obstacle. In the present study, we first demonstrated the characterization
商品
Human pancreatic cancer organoid biobank (PDAC organoids) with various KRAS mutations to aide in 3D cell culture and cancer research applications.
可生成组织和干细胞来源3D脑、胃肠道、肺和癌症肿瘤类器官模型的类器官培养产品。
Organoid culture products to generate tissue and stem cell derived 3D brain, intestinal, gut, lung and cancer tumor organoid models.
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