MARK4 inhibitor 1是微管亲和力调节激酶4（MARK4）的强效抑制剂，对MARK4的IC50值为1.54±0.22μM。
Cas No.:2271081-58-2
Sample solution is provided at 25 µL, 10mM.
_1-3.$$$39978408@51.jpg');)
_1-9.$$$38538795@65.jpg');)
_1-9.$$$39112701@51.jpg');)
_1-7.$$$37316672@70.jpg');)
_366-372.$$$36198801@70.jpg');)
.$$$38565142@65.jpg');)
_1867-1883.$$$33248023@67.jpg');)
_eads6055.$$$39977546@45.jpg');)
_eadm9805.$$$40080571@45.jpg');)
_eadj3020.$$$39666821@45.jpg');)
_1-20.$$$39757301@28.jpg');)
_1-24.$$$38898113@28.jpg');)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
_1-19.$$$37460805@44.jpg');)
_1291-1307.$$$34518654@46.jpg');)
MARK4 inhibitor 1 is a potent inhibitor of microtubule affinity-regulated kinase 4 (MARK4) with an IC50 value of 1.54±0.22μM against MARK4. MARK4 has been found to be overexpressed in multiple cancer types, making it a potential target for cancer prevention or treatment interventions. MARK4 inhibitor 1 can bind to the active site residues of MARK4, inhibiting cell migration, promoting apoptosis and enhancing ROS generation. In vitro experiments, MARK4 inhibitor 1 was not toxic to wild-type HEK293 cells, but its IC50 values against MARK4-overexpressing HepG2, MDA-MB-435s and MCF-7 cells were 6.22±1.11μM, 9.94±1.12μM, and 8.14±1.10μM, respectively[1].
References:
[1] Aneja B, Khan NS, Khan P, et al. Design and development of Isatin-triazole hydrazones as potential inhibitors of microtubule affinity-regulating kinase 4 for the therapeutic management of cell proliferation and metastasis. Eur J Med Chem. 2019;163:840-852.
MARK4 inhibitor 1是微管亲和力调节激酶4（MARK4）的强效抑制剂，对MARK4的IC50值为1.54±0.22μM。MARK4在多种癌症类型中过度表达，是癌症预防或治疗干预措施的潜在靶点。MARK4 inhibitor 1能够与MARK4的活性位点残基结合，抑制细胞迁移，促进细胞凋亡，增强ROS生成。体外实验中，MARK4 inhibitor 1对野生型HEK293细胞无毒性，但对过表达MARK4的HepG2、MDA-MB-435s和MCF-7细胞的IC50值分别为6.22±1.11μM、9.94±1.12μM和8.14±1.10μM[1]。
| Cell experiment [1]: | |
Cell lines | HepG2, MDA-MB-435s, MCF-7, HEK293 |
Preparation Method | MARK4 inhibitor 1 was evaluated for cytotoxicity on HepG2, MDA-MB-435s, MCF-7 cells and HEK293 cells by MTT assay using the concentration range of 0-200μM for 24 and 48h. |
Reaction Conditions | 0-200μM; 24-48h |
Applications | MARK4 inhibitor 1was found to be non-toxic to HEK293 cells, while inhibit the proliferation of HepG2, MDA-MB-435s and MCF-7 cells in a dose-dependent manner. |
References: | |
| Cas No. | 2271081-58-2 | SDF | |
| Canonical SMILES | COC1=CC=C(CN2N=NC(C(N/N=C3C(NC4=C\3C=CC=C4C)=O)=O)=C2)C=C1 | ||
| 分子式 | C20H18N6O3 | 分子量 | 390.4 |
| 溶解度 | DMSO: 5 mg/mL (12.81 mM; ultrasonic and adjust pH to 2 with HCl) | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5615 mL | 12.8074 mL | 25.6148 mL |
| 5 mM | 512.3 μL | 2.5615 mL | 5.123 mL |
| 10 mM | 256.1 μL | 1.2807 mL | 2.5615 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet