HSP27抑制剂J2 (J2)是HSP27的抑制剂,能显著诱导异常HSP27二聚体形成,抑制HSP27大聚合物的生成。
Cas No.:2133499-85-9
Sample solution is provided at 25 µL, 10mM.
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HSP27 inhibitor J2 (J2) is an inhibitor of HSP27, which significantly induces abnormal HSP27 dimer formation and inhibits HSP27 macropolymer production[1-3].
J2(10 µM J2;12 hr)showed stronger HSP27 cross linking activity in HSP27 high expressed lung cancer cells and relatively low cytoxicity[4].
J2(15 mg/kg; i.p; on every other day after irradiation for 14d) treatment significantly inhibited immune cell infiltration in lung tissue. J2-treated mice reversed radiation-induced respiratory distress. J2 inhibited IR-induced lung fibrosis in mice[5-6].
References:
[1]. Hwang SY, Kwak SY, et,al. Synthesis and biological effect of chrom-4-one derivatives as functional inhibitors of heat shock protein 27. Eur J Med Chem. 2017 Oct 20;139:892-900. doi: 10.1016/j.ejmech.2017.08.065. Epub 2017 Sep 1. PMID: 28869891.
[2]. Garrido C, Bruey JM, et,al. HSP27 inhibits cytochrome c-dependent activation of procaspase-9. FASEB J. 1999 Nov;13(14):2061-70. doi: 10.1096/fasebj.13.14.2061. PMID: 10544189.
[3]. Younghwa Na, et al. Methods for treating pulmonary fibrosis using chromenone derivatives.
[4]. Choi B, Choi SK, et,al. Sensitization of lung cancer cells by altered dimerization of HSP27. Oncotarget. 2017 Oct 31;8(62):105372-105382. doi: 10.18632/oncotarget.22192. PMID: 29285257; PMCID: PMC5739644.
[5]. Kim JY, An YM, et,al. HSP27 inhibitor attenuates radiation-induced pulmonary inflammation. Sci Rep. 2018 Mar 8;8(1):4189. doi: 10.1038/s41598-018-22635-9. PMID: 29520071; PMCID: PMC5843649.
[6]. Kim JY, Jeon S, et,al. The Hsp27-Mediated IkBα-NFκB Signaling Axis Promotes Radiation-Induced Lung Fibrosis. Clin Cancer Res. 2019 Sep 1;25(17):5364-5375. doi: 10.1158/1078-0432.CCR-18-3900. Epub 2019 May 24. PMID: 31126962.
HSP27抑制剂J2 (J2)是HSP27的抑制剂,能显著诱导异常HSP27二聚体形成,抑制HSP27大聚合物的生成[1-3]。
J2在高表达HSP27的肺癌细胞中表现出较强的HSP27交联活性,并且细胞毒性相对较低[4]。
J2(15 mg/kg; i.p; on every other day after irradiation for 14d)显著抑制肺组织免疫细胞浸润。j2治疗小鼠逆转了辐射引起的呼吸窘迫。J2抑制IR诱导的小鼠肺纤维化[5-6]。
| Cell experiment [1]: | |
|
Cell lines |
NCI-H460 cells |
|
Preparation Method |
Cells were treated with J2 at 10 µM for 12 hr. |
|
Reaction Conditions |
10 µM J2;12 hr |
|
Applications |
J2 showed stronger HSP27 cross linking activity in HSP27 high expressed lung cancer cells. |
| Animal experiment [2]: | |
|
Animal models |
Male C57BL/6 mice |
|
Preparation Method |
Mice were exposed to a single dose of 75 Gy delivered to the left lung in a single fraction,15 mg/kg of J2 was intraperitoneal administered on every other day after irradiation. |
|
Dosage form |
15 mg/kg; i.p; every other day after irradiation for 14d. |
|
Applications |
J2 treatment significantly inhibited immune cell infiltration in lung tissue. |
|
References: [1]. Choi B, Choi SK, et,al. Sensitization of lung cancer cells by altered dimerization of HSP27. Oncotarget. 2017 Oct 31;8(62):105372-105382. doi: 10.18632/oncotarget.22192. PMID: 29285257; PMCID: PMC5739644. |
|
| Cas No. | 2133499-85-9 | SDF | |
| 别名 | J2 | ||
| Canonical SMILES | O=C1C=C(C)OC2=C1C(O)=CC(OCC3SC3)=C2 | ||
| 分子式 | C13H12O4S | 分子量 | 264.3 |
| 溶解度 | DMSO: 25 mg/mL (94.59 mM) | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7836 mL | 18.9179 mL | 37.8358 mL |
| 5 mM | 756.7 μL | 3.7836 mL | 7.5672 mL |
| 10 mM | 378.4 μL | 1.8918 mL | 3.7836 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: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet