HSP27 inhibitor J2 (Synonyms: J2) |
| Catalog No.GC38503 |
HSP27 inhibitor J2 est un inhibiteur de HSP27 qui induit de manière significative la formation anormale de dimères de HSP27 et inhibe la production de macropolymères de HSP27.
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Cas No.: 2133499-85-9
Sample solution is provided at 25 µL, 10mM.
HSP27 inhibitor J2 est un inhibiteur de HSP27 qui induit de manière significative la formation anormale de dimères de HSP27 et inhibe la production de macropolymères de HSP27[1-3].
Le traitement par J2 (10 µM J2 ; 12 heures) a montré une activité de réticulation de HSP27 plus forte dans les cellules de cancer du poumon à forte expression de HSP27, avec une cytotoxicité relativement faible[4].
Le traitement par J2 (15 mg/kg ; i.p ; tous les deux jours après irradiation pendant 14 jours) a significativement inhibé l'infiltration des cellules immunitaires dans le tissu pulmonaire. Les souris traitées par J2 ont vu leurs symptômes de détresse respiratoire induite par irradiation se renverser. J2 a également inhibé la fibrose pulmonaire induite par l'IR chez les souris[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.
| Expériences cellulaires [1]: | |
Lignées cellulaires | NCI-H460 |
Méthode de préparation | Les cellules ont été traitées avec J2 à 10 µM pendant 12 heures. |
Conditions de réaction | 10 µM de J2 pendant 12 heures |
Domaines d'application | Le J2 a montré une activité de réticulation de HSP27 plus forte dans les cellules de cancer du poumon exprimant fortement HSP27. |
| Expériences animales [2]: | |
Modèles animaux | Souris mâles C57BL/6 |
Méthode de préparation | Les souris ont été exposées à une dose unique de 75 Gy délivrée au poumon gauche en une seule fraction. Le J2 a été administré par voie intrapéritonéale à 15 mg/kg tous les deux jours après l'irradiation. |
Forme de dosage | 15 mg/kg, i.p., tous les deux jours après l'irradiation pendant 14 jours |
Domaines d'application | Le traitement par J2 a significativement inhibé l'infiltration des cellules immunitaires dans le tissu pulmonaire. |
Références : [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. [2]. 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. | |
| Cas No. | 2133499-85-9 | SDF | |
| Synonymes | J2 | ||
| Canonical SMILES | O=C1C=C(C)OC2=C1C(O)=CC(OCC3SC3)=C2 | ||
| Formula | C13H12O4S | M.Wt | 264.3 |
| Solubility | DMSO: 25 mg/mL (94.59 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.7836 mL | 18.9179 mL | 37.8358 mL |
| 5 mM | 0.7567 mL | 3.7836 mL | 7.5672 mL |
| 10 mM | 0.3784 mL | 1.8918 mL | 3.7836 mL |
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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