产品介绍 SP2509 (HCI-2509)是一种选择性histone demethylase LSD1抑制剂，IC50为 13 nM，对MAO-A，MAO-B，乳酸脱氢酶和葡萄糖氧化酶没有活性。SP2509 可诱导凋亡并促进自噬。参考 产品说明 “高效，选择性和可逆的组蛋白脱甲基酶LSD1抑制剂 “改为 “有效的，选择性的和可逆的组蛋白脱甲基酶LSD1拮抗剂” 添加产品介绍SP2509是一种新型的赖氨酸特异性去甲基化酶1（LSD1）拮抗剂，IC50值为13 nM，对MAO-A和MAO-B不起作用。 LSD1对组蛋白H3上的单/二甲基化赖氨酸4进行去甲基化。LSD1的高表达与癌症的预后不良相关。在培养的人急性髓细胞性白血病（AML）细胞中，SP2590抑制LSD1的活性，抑制集落生长，诱导细胞凋亡。SP2590也可以抑制LSD1与CoREST的结合，增加启动子特异性的H3K4Me3，诱导p53、p21和C/EBPα。而且，SP2590还可以促进培养的和原代的AML细胞的分化。 在AML异种移植小鼠中，SP2590单独治疗显著提高了小鼠的存活率，与HDAC的抑制剂panobinostat (PS)共同治疗时具有很好的体内活性。 product description： 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). 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).
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
SP-2509
CAS number：1423715-09-6 molecular formula：C19H20ClN3O5S
overview
compound introduction
Specs
| Chinese alias | N-[(E)-1-(5-氯-2-羟苯基)亚乙基氨基]-3-吗啉-4-基磺酰基苯甲酰胺 | ||
| English alias | - | ||
| CAS number | 1423715-09-6 | molecular formula | C19H20ClN3O5S |
| molecular weight | 437.9 g/mol | Exact mass | 10mM in DMSO |
| PSA | 117.000 Ų | logp | 2.1 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
