| Bioactivity | ER-27319 (maleate), an acridone derivative, is a potent and selective SKY inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 (maleate) inhibits the release of antigen-induced allergic mediators from human and rat mast cells with an IC50 of 10 μM and can be used for study in allergic diseases[1] [2] . |
| Target | 10 μM (Syk) in human and rat mast cells |
| Invitro | ER-27319 (maleate) (24 h) 抑制 RBL-2H3 细胞、大鼠腹膜和人培养肥大细胞中抗原诱导的肌醇磷酸的生成、花生四烯酸的释放、组胺和肿瘤坏死因子 α 的分泌，且IC50 值约为10 μM[1]。ER-27319 (maleate) (10-30 μM, 10 min) 选择性抑制 FcεRI γ 磷酸化的免疫受体酪氨酸激活基序诱导的 SYK 的酪氨酸磷酸化[1]。ER-27319 (maleate) (高达100 μM, 60 min) 不抑制Jurkat 细胞中 CD3 刺激引起的 ZAP-70 的酪氨酸磷酸化[1]。ER-27319 (maleate) (100 μM, 10 min) 在抗 IgG 刺激的犬皮肤瘤源性肥大细胞中抑制两种蛋白 (38, 70 kD) 的酪氨酸磷酸化，降低另外两种蛋白 (62, 80 kD) 的酪氨酸磷酸化[2]。 Western Blot Analysis[1] Cell Line: |
| Name | ER-27319 maleate |
| CAS | 1204480-26-1 |
| Formula | C22H24N2O5 |
| Molar Mass | 396.44 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Katsuhiro Moriya, et al. ER-27319, an acridone-related compound, inhibits release of antigen-induced allergic mediators from mast cells by selective inhibition of Fcɛ receptor I-mediated activation of Syk. Proc Natl Acad Sci U S A. 1997 Nov 11; 94(23): 12539–12544. [2]. Yoshitaka Sato, et al. IgG-mediated signal transduction in canine mastocytoma-derived cells. Int Arch Allergy Immunol. 2002 Dec;129(4):305-13. |
ER-27319 maleate
CAS: 1204480-26-1 F: C22H24N2O5 W: 396.44
ER-27319 (maleate), an acridone derivative, is a potent and selective SKY inhibitor, and inhibits the tyrosine phos
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