Seclidemstat (Synonyms: SP-2577)
目录号: PL15117 纯度: ≥99%
CAS No. :1423715-37-0
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中文名称
Seclidemstat
英文名称
Seclidemstat
英文别名
Seclidemstat;TYH386V3WJ;SP2577;s6722;Benzoic acid, 3-((4-methyl-1-piperazinyl)sulfonyl)-, (2E)-2-(1-(5-chloro-2-hydroxyphenyl)ethylidene)hydrazide;SP-2577
Cas No.
1423715-37-0
分子式
C20H23ClN4O4S
分子量
450.94
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Seclidemstat 是一种有效的非竞争性可逆 KDM1A (LSD1) 抑制剂 (Ki=31 nM, IC50)。Seclidemstat 促进 SWI/SNF 复合物突变卵巢癌的抗肿瘤免疫,并抑制病毒产生、病毒 DNA 复制和晚期基因表达。Seclidemstat 可用于尤文肉瘤的研究。
生物活性
Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (K i =31 nM, IC 50 =13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma.
性状
Solid
IC50 & Target[1][2]
Ki: 31 nM (LSD1)
IC50: 13 nM (LSD1)
体外研究(In Vitro)
Seclidemstat (72 hours) inhibits SWI/SNF-mutation-dependent tumor cell proliferation with IC50 ranging from 0.013 to 2.819 μM (COV434, BIN67, SCCOHT-1, TOV21G, SKOV3, A427, H522, A549, H1299, G401, G402, HCC15 cells).
Seclidemstat (72 hours) promotes endogenous retroviruses (ERVs) expression and activation of IFNβ pathway in SCCOHT cell lines (SCCOHT-1, BIN67, and COV434 cells).
Seclidemstat (3 μM) promotes PD-L1 expression in SCCOHT COV 434 pIND 20 BRG1-2.7 cell line. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Dai XJ, et al. Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1 [published correction appears in J Med Chem. 2021 May 13;64(9):6410-6411]. J Med Chem. 2021;64(5):2466-2488.
[2]. Soldi R, et al. The novel reversible LSD1 inhibitor SP-2577 promotes anti-tumor immunity in SWItch/Sucrose-NonFermentable (SWI/SNF) complex mutated ovarian cancer. PLoS One. 2020;15(7):e0235705. Published 2020 Jul 10.
溶解度数据
In Vitro: DMSO : 50 mg/mL (110.88 mM; ultrasonic and warming and heat to 80°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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