945526-43-2
945526-43-2 structure
- Name: ISCK03
- Chemical Name: 4-tert-butyl-N-(4-imidazol-1-ylphenyl)benzenesulfonamide
- CAS Number: 945526-43-2
- Molecular Formula: C19H21N3O2S
- Molecular Weight: 355.454
- Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK c-Kit
- Create Date: 2017-11-01 13:43:16
- Modify Date: 2024-01-04 22:44:46
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ISCK03 is a specific SCF/c-Kit inhibitor.
| Name | 4-tert-butyl-N-(4-imidazol-1-ylphenyl)benzenesulfonamide |
|---|---|
| Synonyms |
4-t-butylphenyl-N-(4-imidazol-1-ylphenyl)sulfonamide
N-[4-(1H-Imidazol-1-yl)phenyl]-4-(2-methyl-2-propanyl)benzenesulfonamide UNII-3028H7W568 Whiteplex-IN ISCK03 t-Butylphenyl imidazolylphenyl sulfonamide Benzenesulfonamide, 4-(1,1-dimethylethyl)-N-[4-(1H-imidazol-1-yl)phenyl]- HMS3229P07 |
| Description | ISCK03 is a specific SCF/c-Kit inhibitor. |
|---|---|
| Related Catalog | |
| In Vitro | Pretreatment of 501mel cells with ISCK03 inhibits SCF-induced c-kit phosphorylation dose dependently. ISCK03 also inhibits p44/42 ERK mitogen-activated protein kinase (MAPK) phosphorylation, which is known to be involved in SCF/c-kit downstream signaling. However ISCK03 does not inhibit hepatocyte growth factor (HGF)-induced phosphorylation of p44/42 ERK proteins[1]. ISCK03, a tyrosine kinase inhibitor specific to KIT, prevents survival of CCDC26-KD cells under low-serum conditions. All treated cells exhibits sensitivity to ISCK03 in a dose-dependent manner. After ISCK03 treatment, the survival of KD cells is suppressed to the same level as that of non-KD cells. Conversely, ISCK03 treatment has limited effects on the growth of control K562 and KD clone 3–4 cells under high-serum concentration conditions[2]. |
| In Vivo | Oral administration of ISCK03 induces the dose-dependent depigmentation of newly regrown hair, and this is reversed with cessation of ISCK03 treatment. The topical application of ISCK03 promotes the depigmentation of UV-induced hyperpigmented spots. Fontana-Masson staining analysis shows epidermal melanin is diminished in spots 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 Assay | 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]. |
| Animal Admin | Mice: To induce the hair cycle, depilation of skin on the back of the female C57BL/6 mice is performed. Briefly, the hair is removed from anesthetized mice. The rat antimouse c-kit-neutralizing monoclonal antibody ACK2 is administered intraperitoneally (50 mg) every day. ISCK03 is administered orally once a day. On days 21–28, animals are sacrificed or analyzed for repigmentation of the newly regrown hair shaft. Skin is harvested and fixed in paraffin or frozen for immunohistochemical analyses[1]. |
| References |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Boiling Point | 520.0±60.0 °C at 760 mmHg |
| Molecular Formula | C19H21N3O2S |
| Molecular Weight | 355.454 |
| Flash Point | 268.3±32.9 °C |
| Exact Mass | 355.135437 |
| PSA | 72.37000 |
| LogP | 4.03 |
| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
| Index of Refraction | 1.607 |
| Storage condition | 2-8℃ |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Gloves |
|---|---|
| Hazard Codes | Xi |
| RIDADR | NONH for all modes of transport |