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SML0788

Sigma-Aldrich

A 83-01

≥98% (HPLC)

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Synonym(s):
3-(6-Methyl-2-pyridinyl)-N-phenyl-4-(4-quinolinyl)-1H-pyrazole-1-carbothioamide, A-83-01, A83-01
Empirical Formula (Hill Notation):
C25H19N5S
CAS Number:
Molecular Weight:
421.52
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

storage temp.

−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

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This Item
616454SML1962SML2384
A 83-01 ≥98% (HPLC)

Sigma-Aldrich

SML0788

A 83-01

Sigma-Aldrich

Sigma-Aldrich

SML1962

IWP-O1

BAY 87-2243 ≥98% (HPLC)

Sigma-Aldrich

SML2384

BAY 87-2243

form

powder

form

solid

form

powder

form

powder

color

white to beige

color

pale yellow

color

white to beige

color

white to beige

solubility

DMSO: 5 mg/mL, clear (warmed)

solubility

DMSO: 20 mg/mL

solubility

DMSO: 25 mg/mL, clear

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

storage temp.

2-8°C

storage temp.

2-8°C

storage temp.

2-8°C

Quality Level

100

Quality Level

200

Quality Level

100

Quality Level

-

Application

A 83-01 has been used as an inhibitor of transforming growth factor β kinase type 1 receptor.

Biochem/physiol Actions

A 83-01 is a TGFβ kinase/activin receptor-like kinase (ALK 5) inhibitor (IC50=12 nM) that prevents phosphorylation of Smad2/3 and inhibits growth induced by TGFβ. A 83-01 blocks phosphorylation of Smad2 and inhibits TGF-β-induced epithelial-to-mesenchymal transition. Also, A 83-01 inhibits the transcriptional activity induced by TGFβ type I receptor ALK-5, activin type IB receptor ALK-4 and nodal type I receptor ALK-7. A-83-01 induces an expansion of neonatal Nkx2.5-eGFP (+) cells.

Storage Class Code

11 - Combustible Solids

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)
First-line treatment selection with organoids of an EGFRm + TP53m stage IA1 patient with early metastatic recurrence after radical surgery and follow-up.
Ziqi Jia et al.
Journal of thoracic disease, 12(7), 3764-3773 (2020-08-18)
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
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
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)

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