ISCK03
Based on 6 publication(s) in Google Scholar
ISCK03 is a SCF/c-Kit and CD117-specific inhibitor. ISCK03 significantly inhibits c-Kit phosphorylation at 10 μM.
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- Pureté: 98.30%
- CAS No.: 945526-43-2
- Formule: C19H21N3O2S
- Masse moléculaire:355.45
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ISCK03
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Customer Validation & Images
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Activité biologique
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 945526-43-2
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Appearance Solid
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Masse moléculaire 355.45
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Formule C19H21N3O2S
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Color Off-white to light yellow
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SMILES
O=S(C1=CC=C(C(C)(C)C)C=C1)(NC2=CC=C(N3C=CN=C3)C=C2)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Cancer Lett
PGR-KITLG signaling drives a tumor-mast cell regulatory feedback to modulate apoptosis of breast cancer cells. [Abstract]2024 May 1:589:216795. PMID: 38556106 -
CNS Neurosci Ther
Metrnl/C-KIT Axis Attenuates Early Brain Injury Following Subarachnoid Hemorrhage by Inhibiting Neuronal Ferroptosis. [Abstract]2025 Feb;31(2):e70286. PMID: 39981761 -
Front Cell Dev Biol
Rheb1-Deficient Neutrophils Promote Hematopoietic Stem/Progenitor Cell Proliferation via Mesenchymal Stem Cells. [Abstract]2021 May 27:9:650599. PMID: 34124040 -
Cell Cycle
2020 Aug;19(16):2074-2080. PMID: 32658594
ISCK03 purchased from MedChemExpress. Usage Cited in: Cell Cycle. 2020 Aug;19(16):2074-2080. [Abstract]
The expressions of p-JAK/JAK and p-STAT3/STAT3 are examined by Western blot assay. SCF induces up-regulation of p-JAK/JAK and p-STAT3/STAT3, but this effect is effectively counteracted by the SCF/c-kit inhibitor ISCK03.
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Prostate
c-Kit-Mediated PI3K/AKT and Wnt/β-Catenin Signaling Drives Resistance to 5α-Reductase Inhibitors in Benign Prostatic Hyperplasia. [Abstract]2025 Sep 29. PMID: 41017279 -
Mol Reprod Dev
Mechanism of Bushen Shengjing Decoction on the Spermatogenic Function of in Rats With Oligoasthenospermia: Focus on SCF/c-Kit Signaling Pathway-Mediated Apoptosis. [Abstract]2025 Aug;92(8):e70044. PMID: 40788237
Solvant et solubilité
DMSO : ≥ 38 mg/mL (106.91 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Wintzell M, et al. Repeated cisplatin treatment can lead to a multiresistant tumor cell population with stem cell features and sensitivity to 3-bromopyruvate. Cancer Biol Ther. 2012 Dec;13(14):1454-62. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8133 mL | 14.0667 mL | 28.1334 mL | 70.3334 mL |
| 5 mM | 0.5627 mL | 2.8133 mL | 5.6267 mL | 14.0667 mL | |
| 10 mM | 0.2813 mL | 1.4067 mL | 2.8133 mL | 7.0333 mL | |
| 15 mM | 0.1876 mL | 0.9378 mL | 1.8756 mL | 4.6889 mL | |
| 20 mM | 0.1407 mL | 0.7033 mL | 1.4067 mL | 3.5167 mL | |
| 25 mM | 0.1125 mL | 0.5627 mL | 1.1253 mL | 2.8133 mL | |
| 30 mM | 0.0938 mL | 0.4689 mL | 0.9378 mL | 2.3444 mL | |
| 40 mM | 0.0703 mL | 0.3517 mL | 0.7033 mL | 1.7583 mL | |
| 50 mM | 0.0563 mL | 0.2813 mL | 0.5627 mL | 1.4067 mL | |
| 60 mM | 0.0469 mL | 0.2344 mL | 0.4689 mL | 1.1722 mL | |
| 80 mM | 0.0352 mL | 0.1758 mL | 0.3517 mL | 0.8792 mL | |
| 100 mM | 0.0281 mL | 0.1407 mL | 0.2813 mL | 0.7033 mL |
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