A-83-01

Catalog No.S7692 Batch:S769202

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Technical Data

Formula

C25H19N5S
Molecular Weight 421.52 CAS No. 909910-43-6
Solubility (25°C)* In vitro DMSO 21 mg/mL (49.81 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 57 publications

Loss of Kmt2c or Kmt2d primes urothelium for tumorigenesis and redistributes KMT2A-menin to bivalent promoters [ Nat Genet, 2025, 57(1):165-179] PubMed: 39806204
Microbial metabolites control self-renewal and precancerous progression of human cervical stem cells [ Nat Commun, 2025, 16(1):2327] PubMed: 40057497
RSAD2: A pathogenic interferon-stimulated gene at the maternal-fetal interface of patients with systemic lupus erythematosus [ Cell Rep Med, 2025, S2666-3791(25)00047-3] PubMed: 39983716
A pancreatic cancer organoid incorporating macrophages reveals the correlation between the diversity of tumor-associated macrophages and cancer cell survival [ Biomaterials, 2025, 314:122838] PubMed: 39348736
NLRP7 maintains the genomic stability during early human embryogenesis via mediating alternative splicing [ Commun Biol, 2025, 8(1):125] PubMed: 39865169
Establishing Pancreatic Cancer Organoids from EUS-Guided Fine-Needle Biopsy Specimens [ Cancers (Basel), 2025, 17(4)692] PubMed: 40002285
Protocol for generating a pancreatic cancer organoid associated with heterogeneous tumor microenvironment [ STAR Protoc, 2025, 6(1):103539] PubMed: 39772386
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

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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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