SML0788

A 83-01

≥98% (HPLC), powder, TGF-β RI kinase inhibitor

• 别名: 3-（6-甲基-2-吡啶基）-N-苯基-4-（4-喹啉基）-1H-吡唑-1-硫代甲酰胺, A-83-01, A83-01
• 经验公式（希尔记法）: C₂₅H₁₉N₅S
• CAS号: 909910-43-6
• 分子量: 421.52
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• product name: A 83-01, ≥98% (HPLC)
• 品質等級: 100
• 化驗: ≥98% (HPLC)
• 形狀: powder
• 顏色: white to beige
• 溶解度: DMSO: 5 mg/mL, clear (warmed)
• 儲存溫度: −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 密鑰: HIJMSZGHKQPPJS-UHFFFAOYSA-N

说明

一般說明

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.

應用

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。

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3