IM-93
目录号 : GC45793
A dual inhibitor of ferroptosis and NETosis
Cas No.:1173657-73-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IM-93 is a dual inhibitor of ferroptosis and NETosis.1 It inhibits tert-butyl hydroperoxide- and erastin-induced ferroptosis in NIH3T3 cells (IC50s =1.8 and 1.9 nM, respectively), as well as decreases NETosis induced by phorbol 12-myristate 13-acetate in isolated human peripheral blood neutrophils when used at concentrations ranging from 1.6 to 25 μM. IM-93 also inhibits hydrogen peroxide-induced necrosis in HL-60 cells (IC50 = 0.45 μM), but has no effect on necroptosis induced by Fas ligand in combination with Z-VAD-FMK and cycloheximide in Jurkat cells or pyroptosis induced by S. aureus and P. aeruginosa in THP-1 cells when used at a concentration of 25 μM.
|1. Dodo, K., Kuboki, E., Shimizu, T., et al. Development of a water-soluble indolylmaleimide derivative IM-93 showing dual inhibition of ferroptosis and NETosis. ACS Med. Chem. Lett. 10(9), 1272-1278 (2019).
| Cas No. | 1173657-73-2 | SDF | |
| Canonical SMILES | O=C(C(C1=CN(C)C2=C1C=CC=C2)=C3NCCCN(C)C)N(C(C)C)C3=O | ||
| 分子式 | C21H28N4O2 | 分子量 | 368.5 |
| 溶解度 | DMF: 20mg/mL,DMSO: 20mg/mL,DMSO:PBS (pH 7.2) (1:2): 0.3mg/mL,Ethanol: 1mg/mL | 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 | 2.7137 mL | 13.5685 mL | 27.137 mL |
| 5 mM | 0.5427 mL | 2.7137 mL | 5.4274 mL |
| 10 mM | 0.2714 mL | 1.3569 mL | 2.7137 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。
Development of a Water-Soluble Indolylmaleimide Derivative IM-93 Showing Dual Inhibition of Ferroptosis and NETosis
ACS Med Chem Lett 2019 Jul 30;10(9):1272-1278.PMID:31531196DOI:PMC6746101
The indolylmaleimide (IM) derivative IM-17 shows inhibitory activity against oxidative-stress-induced necrotic cell death and cardioprotective activity in rat ischemia-reperfusion injury models. In order to develop a more potent derivative, we conducted a detailed structure-activity relationship study of IM derivatives and identified IM-93 as the most potent derivative with good water solubility. IM-93 inhibited ferroptosis and NETosis, but not necroptosis or pyroptosis. In contrast, ferrostatin-1 (Fer-1), a ferroptosis inhibitor, did not inhibit NETosis, although the accompanying lipid peroxidation was partially inhibited by Fer-1, as well as by IM-93. Thus, IM derivatives have a unique activity profile and appear to be promising candidates for in vivo application.