| 產(chǎn)品編號 | 5.09703 |
| 品牌 | Sigma |
| 形式 | solid |
| 警告 | Toxicity: Standard Handling (A) |
| 測定 | ≥98% (HPLC) |
| 顏色 | off-white |
| 分子量 | 437.90 |
| 溶解性 | DMSO: 100?mg/mL |
| 質(zhì)量水平 | 100 |
| 儲存條件 | OK to freeze
protect from light |
| 儲存溫度 | 2-8°C |
別名
LSD1 Inhibitor VII, SP-2509 - CAS 1423715-09-6 - Calbiochem,BHC110 Inhibitor VII, Histone Lysine Demethylase Inhibitor XIV, KIAA1718 Inhibitor VII, LSD Inhibitor VII, SP-2509
一般描述
A cell-permeable phenethylidene-benzohydrazide compound that acts as a potent, selective, reversible, and non-competitive inhibitor of Lysine-Specific Demethylase 1 (LSD1; IC50 = 13 nM; Ki = 31 nM). Exhibits excellent selectivity over monoamine oxidases A and B (IC50 >300 μM), lactate dehydrogenase, glucose oxidase, hERG, CYP1A2, CYP2D6 (IC50 ≥ 10 μM), CYP2C9 (IC50 = 8.04 μM) and CYP2C19 (IC50 = 9.76 μM). Inhibits CYP3A4 only at >200-fold higher concentration. Reduces the proliferation of several cancer cell lines, including AN3 Ca, BT-20, MCF-7, T-47D, HT29, MIA PaCa-2 and SK-N-MC (IC50 = 356, 489, 637, 649, 429, 468 and 329 nM, respectively).
A cell-permeable, lysine-specific demethylase 1 (LSD1) active site-targeting phenethylidene-benzohydrazide that inhibits LSD1 activity (IC50 = 13 nM) in a reversible and substrate non-competitive (Ki = 34 nM) manner, while inhibiting CYP3A4 only at much higher concentrations (IC50 = 2.61 μM) and displaying little or no potency towards CYP1A2/2C9/2C19/2D6. MAO-A/B, D-lactate dehydrogenase, glucose oxidase, and hERG (IC50 ≥8.0 μM). Shown to enhance histone H3 Lys9 dimethylation (H3K9me2) in androgen-dependent prostate cancer VCaP cultures (1 to 10 μM) and effectively inhibits LSD1-dependent cancer growth (IC50 in nM = 329/SK-N-MC, 356/AN3 Ca, 429/HT29, 468/MIA PaCa-2, 489/BT-20, 612/HER218, 614/HCT 116, 637/MCF-7, 649/T-47D; 96 h).
生化/生理作用
Cell permeable: yes
Primary Target
LSD1
Reversible: yes
重懸
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他說明
Fiskus, W., et al. 2014. Leukemia28, 2155.
Sorna, V., et al. 2013. J. Med. Chem.56, 9496.
關(guān)鍵字： LSD1 Inhibitor VII, SP-2509 - CAS 1423715-09-6 - Calbiochem;LSD1 Inhibitor VII, SP-2509 - CAS 1423715-09-6 - Calbiochem價(jià)格;LSD1 Inhibitor VII, SP-2509 - CAS 1423715-09-6 - Calbiochem廠家;1423715-09-6;Sigma
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我們擁有廣泛的高質(zhì)量產(chǎn)品組合和解決方案，致力于推動科學(xué)研究，提高藥物研發(fā)和生物制藥生產(chǎn)的質(zhì)量和效率，并為獲取準(zhǔn)確可靠的診斷和檢測結(jié)果提供安全的保障。我們的愿景是使全球各地的人們能夠更快地獲得提升人類健康水平的解決方案。我們的共同目標(biāo)是通過與全球科學(xué)界合作，解決生命科學(xué)中棘手的問題。
30萬個(gè)廣泛產(chǎn)品組合，其中包括業(yè)內(nèi)許多知名的品牌，Sigma-Alrdich?、Milli-Q?、 Supelco?、Millipore?、SAFC?和BioReliance?。
關(guān)于默克
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科學(xué)探索和負(fù)責(zé)任的企業(yè)精神一直是默克科技進(jìn)步的關(guān)鍵，也是默克自1668年以來永葆活力的秘訣。默克家族作為公司的創(chuàng)始者至今仍持有默克大部分的股份，我們在全球都叫“默克”，僅美國和加拿大例外。默克的三大領(lǐng)域：醫(yī)藥健康、生命科學(xué)及電子科技在這兩個(gè)國家分別稱之為“EMD Serono”、“MilliporeSigma”和“EMD Electronics”。
默克在中國已經(jīng)有87年發(fā)展歷史，目前有超過4100名員工，在