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Merck
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重要文件

SML0788

Sigma-Aldrich

A 83-01

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

同義詞:

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

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About This Item

經驗公式(希爾表示法):
C25H19N5S
CAS號碼:
分子量::
421.52
分類程式碼代碼:
12352200
NACRES:
NA.77

產品名稱

A 83-01, ≥98% (HPLC)

品質等級

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

SMILES 字串

S=C([n]2nc(c(c2)c4c5c(ncc4)cccc5)c3nc(ccc3)C)Nc1ccccc1

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

一般說明

A-83-01可有效抑制烧伤创面收缩而不影响创面愈合,因为它可抑制转化生长因子-β (TGF-β)诱导的肌成纤维细胞群增加。此外,还可通过抑制动物的上皮间质转化(EMT)来阻止TGF-β1-依赖的癌症转移。

應用

A 83-01已用于:
  • 加入培养基用于分离肿瘤细胞的类器官形成
  • 加入杜氏改良Eagle培养基/F-12营养混合物(DMEM/F12)中以培养人表皮干细胞(EpSCs)

A 83-01已被用作转化生长因子β激酶1型受体的抑制剂。

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。
A-83-01是一种TGFβ激酶/激活素受体样激酶(ALK 5)抑制剂。

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3


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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)
Steven A Saenz et al.
PloS one, 16(11), e0248034-e0248034 (2021-11-10)
Retinoic acid receptor-related orphan nuclear receptor (ROR) γt is a member of the RORC nuclear hormone receptor family of transcription factors. RORγt functions as a critical regulator of thymopoiesis and immune responses. RORγt is expressed in multiple immune cell populations
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)
Eugenia Girda et al.
International journal of gynecological cancer : official journal of the International Gynecological Cancer Society, 27(8), 1701-1707 (2017-07-07)
Patient-derived organoids (PDOs), used in multiple tumor types, have allowed evaluation of tumor characteristics from individual patients. This study aimed to assess the feasibility of applying PDO in vitro culture for endocrine-based and drug sensitivity testing in endometrial cancer. Endometrial
Ling Leng et al.
Stem cell research & therapy, 11(1), 415-415 (2020-09-25)
Millions suffer from skin diseases. Functional interfollicular epidermal stem cells are needed in skin therapy or drug screening in vitro. We obtained functional interfollicular epidermal stem cells with intact stemness and cell junctions by treating them with Wnt3a. Moreover, epidermal

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