A-83-01

Catalog No.S7692 Batch:S769201

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Technical Data

Formula

C25H19N5S
Molecular Weight 421.52 CAS No. 909910-43-6
Solubility (25°C)* In vitro DMSO 23 mg/mL (54.56 mM)
Water ˂1 mg/mL
Ethanol ˂1 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description A-83-01 is a potent inhibitor of TGF-β type I receptor (ALK5-TD) with IC50 of 12 nM. A-83-01 also inhibits the transcription induced by activin/nodal type I receptor (ALK4-TD) and nodal type I receptor (ALK7-TD) with IC50 of 45 nM and 7.5 nM, respectively.Solutions are unstable and should be fresh-prepared.
Targets
ALK7 [1]
(Cell-free assay)		 ALK5 [1]
(Cell-free assay)		 ALK4 [1]
(Cell-free assay)
7.5 nM 12 nM 45 nM
In vitro

A-83-01 inhibits the transcriptional activity induced by TGF-β type I receptor ALK-5 and that by activin type IB receptor ALK-4 and nodal type I receptor ALK-7, the kinase domains of which are structurally highly related to those of ALK-5. A-83-01 is potent in the inhibition of ALK5 and also prevents phosphorylation of Smad2/3 and the growth inhibition induced by TGF-β.[1]
In vivo

A83-01 treatment significantly increases the number of Nkx2.5+ cardiomyoblasts at baseline and after myocardial injury, resulting in an increase in newly formed cardiomyocytes. A83-01 treatment significantly improves ventricular elastance and stroke work, leading to improved contractility after injury.[2]

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    Wild-type mink lung epithelial (Mv1Lu) cells, R mutant of Mv1Lu (R4-2) cells, HaCaT cells, C2C12 cells, NMuMG cells

  • Concentrations

    1 μM

  • Incubation Time

    1 h

  • Method

    Cell proliferation assay: Mv1Lu cells are seeded in duplicate at a density of 2.5 × 104 cells/well in 24-well plates. The following day, cells are pretreated for 1 h with 1 μM A-83-01 and then cultured with TGF-β (1 ng/mL) for 24 h, 48 h, or 72 h. Cells are trypsinized and counted with a Coulter counter. To explore whether A-83-01 reduces the growth-inhibitory effects of TGF-β in concentration-dependent fashion, Mv1Lu cells are seeded as above and pretreated for 1 h with various concentrations of A-83-01. After pretreatment, cells are cultured with TGF-β (1 ng/mL) for 48 h and counted.
Animal Study:

[2]
  • Animal Models

    8–10 week old Nkx2.5 enhancer-eGFP transgenic mice

  • Dosages

    10 mg/kg

  • Administration

    IP

Selleck's A-83-01 has been cited by 48 publications

Restoring sweat gland function in mice using regenerative sweat gland cells derived from chemically reprogrammed human epidermal keratinocytes [ Sci Bull (Beijing), 2024, S2095-9273(24)00799-0] PubMed: 39550273
Jag1/2 maintain esophageal homeostasis and suppress foregut tumorigenesis by restricting the basal progenitor cell pool [ Nat Commun, 2024, 15(1):4124] PubMed: 38750026
Jag1/2 maintain esophageal homeostasis and suppress foregut tumorigenesis by restricting the basal progenitor cell pool [ Nat Commun, 2024, 15(1):4124] PubMed: 38750026
Self-renewing human naïve pluripotent stem cells dedifferentiate in 3D culture and form blastoids spontaneously [ Nat Commun, 2024, 15(1):668] PubMed: 38253551
VGLL1 cooperates with TEAD4 to control human trophectoderm lineage specification [ Nat Commun, 2024, 15(1):583] PubMed: 38233381
Inhibition of HDAC activity directly reprograms murine embryonic stem cells to trophoblast stem cells [ Dev Cell, 2024, S1534-5807(24)00326-5] PubMed: 38823394
CALB2 drives pancreatic cancer metastasis through inflammatory reprogramming of the tumor microenvironment [ J Exp Clin Cancer Res, 2024, 43(1):277] PubMed: 39358777
Dual inhibition of SUMOylation and MEK conquers MYC-expressing KRAS-mutant cancers by accumulating DNA damage [ J Biomed Sci, 2024, 31(1):68] PubMed: 38992694
FOXA3 regulates cholesterol metabolism to compensate for low uptake during the progression of lung adenocarcinoma [ PLoS Biol, 2024, 22(5):e3002621] PubMed: 38805565
Extraembryonic mesoderm cells derived from human embryonic stem cells rely on Wnt pathway activation [ Cell Prolif, 2024, 10.1111/cpr.13761] PubMed: 39385268

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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