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ISCK03

Catalog No. T3452   CAS 945526-43-2

ISCK03 is a selective SCF/c-Kit inhibitor.

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ISCK03 Chemical Structure
ISCK03, CAS 945526-43-2
Pack Size Availability Price/USD Quantity
2 mg In stock $ 33.00
5 mg In stock $ 52.00
10 mg In stock $ 85.00
25 mg In stock $ 182.00
50 mg In stock $ 312.00
100 mg In stock $ 531.00
1 mL * 10 mM (in DMSO) In stock $ 57.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ISCK03 is a selective SCF/c-Kit inhibitor.
In vitro Pretreatment with ISCK03 dose-dependently inhibits SCF-induced c-kit phosphorylation and p44/42 ERK (MAPK) phosphorylation, key components of SCF/c-kit signaling, without affecting HGF-induced phosphorylation of the same ERK proteins. As a specific tyrosine kinase inhibitor of KIT, ISCK03 effectively suppresses the survival of CCDC26-KD cells in low-serum environments, demonstrating dose-dependent sensitivity. While significantly impacting KD cells, reducing their survival to levels comparable with non-KD cells, ISCK03 shows minimal effects on the growth of control K562 and KD clone 3–4 cells in high-serum conditions.
In vivo Administering ISCK03 orally causes a dose-dependent depigmentation of newly regrown hair, a process that reverses upon discontinuing the treatment. Topically applying ISCK03 effectively depigments UV-induced hyperpigmented spots. Fontana-Masson staining analysis reveals a reduction in epidermal melanin in areas treated with ISCK03[1].
Kinase Assay ATP is dispensed into 384-well plates, chemical compounds (ISCK03: 2.5, 5, 10, 100 μM) are added by replicative plate, and recombinant human c-kit protein is added for the kinase reaction. Following a 45-min incubation at 37°C, the development reaction is carried out for 40 min at room temperature. After the reaction is stopped, the coumrain and fluorescein fluorescence-emission signals are detected[1].
Cell Research To determine any cytotoxic effects of ISCK03 on 501mel cells, MTT assays are performed with various doses of ISCK03 (1, 5, 10 μM). 501mel cells are cultured with SCF alone (50 ng/mL) or SCF with ISCK03 for 48 h[1].
Molecular Weight 355.45
Formula C19H21N3O2S
CAS No. 945526-43-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (140.66 mM)

TargetMolReferences and Literature

1. Na YJ, et al. [4-t-butylphenyl]-N-(4-imidazol-1-yl phenyl)sulfonamide (ISCK03) inhibits SCF/c-kit signaling in 501mel human melanoma cells and abolishes melanin production in mice and brownish guinea pigs. Biochem Pharmacol. 2007 Sep 1;74(5):780-6. 2. Hirano T, et al. Long noncoding RNA, CCDC26, controls myeloid leukemia cell growth through regulation of KIT expression. Mol Cancer. 2015 Apr 19;14:90. doi: 10.1186/s12943-015-0364-7.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library Stem Cell Differentiation Compound Library Bioactive Compound Library NO PAINS Compound Library Immunology/Inflammation Compound Library Target-Focused Phenotypic Screening Library Bioactive Compounds Library Max

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Keywords

ISCK03 945526-43-2 Tyrosine Kinase/Adaptors c-Kit inhibit SCFR CD117 Inhibitor ISCK-03 ISCK 03 inhibitor

 

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