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Merck
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Key Documents

SML0788

Sigma-Aldrich

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

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About This Item

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

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

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。

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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