ISCK03
(Synonyms: STEM-CELLFACTOR/C-KIT抑制剂 ,c-Kit Inhibitor II,Stem-Cell Factor/c-Kit Inhibitor) 目录号 : GC13961
An inhibitor of SCF/c-kit signaling
Cas No.:945526-43-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Kinase experiment: | 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 experiment: | 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 experiment: | 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: [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. | |
ISCK03 is an inhibitor of SCF-mediated c-kit activation.
The signaling downstream of SCF/c-kit plays a key role in the development of various mammalian cells, such as mast cells, melanocytes, primordial germ cells, and hematopoietic progenitor cells.
In vitro: Previous study showed that the pretreatment of 501mel cells with ISCK03 could dose-dependently inhibit SCF-induced c-kit phosphorylation. ISCK03 could also inhibit the phosphorylation of p44/42 ERK mitogen-activated protein kinase that was known to be involved in SCF/c-kit downstream signaling. However, ISCK03 was not able to inhibit hepatocyte growth factor-induced phosphorylation of p44/42 ERK proteins [1].
In vivo: To determine the in vivo efficacy, ISCK03was orally administered to depilated C57BL/6 mice. Results showed that the oral administration of ISCK03 could induce the dose-dependent depigmentation of newly regrown hair, and this was reversed with cessation of ISCK03 treatment. In addition, the topical application of ISCK03 could promote the depigmentation of UV-induced hyperpigmented spots on n brownish guinea pig skin. Moreover, the Fontana–Masson staining analyses showed epidermal melanin was diminished in spots treated with ISCK03 [1].
Clinical trial: Up to now, ISCK03 is still in the preclinical development stage.
References:
[1] Y. J. Na, H. S. Baek, S. M. Ahn, 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. Biochemical Pharmacology 74(5), 780-786 (2007).
| Cas No. | 945526-43-2 | SDF | |
| 别名 | STEM-CELLFACTOR/C-KIT抑制剂 ,c-Kit Inhibitor II,Stem-Cell Factor/c-Kit Inhibitor | ||
| 化学名 | 4-(1,1-dimethylethyl)-N-[4-(1H-imidazol-1-yl)phenyl]-benzenesulfonamide | ||
| Canonical SMILES | O=S(NC1=CC=C(N2C=NC=C2)C=C1)(C3=CC=C(C(C)(C)C)C=C3)=O | ||
| 分子式 | C19H21N3O2S | 分子量 | 355.5 |
| 溶解度 | ≤2mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8129 mL | 14.0647 mL | 28.1294 mL |
| 5 mM | 0.5626 mL | 2.8129 mL | 5.6259 mL |
| 10 mM | 0.2813 mL | 1.4065 mL | 2.8129 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。