SP2509
别名: HCI-2509
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。
SP2509 Chemical Structure
CAS: 1423715-09-6
客户使用Selleck的SP2509发表文献25篇
客户使用该产品的1个实验数据
产品质控
SP2509相关产品
| 相关靶点 | KDM1 KDM2 KDM3 KDM4 KDM5 KDM6 | 点击展开 |
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| 相关产品 | GSK J4 HCl CPI-455 HCl Iadademstat (ORY-1001) 2HCl GSK-LSD1 2HCl JIB-04 OG-L002 ML324 IOX1 GSK J1 CP2 CPI-455 L-2-Hydroxyglutaric acid disodium | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 FDA药物库 天然产物库 已知活性药物库-I 生物活性库Ⅱ | 点击展开 |
相关信号通路图
Histone Demethylase抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| HT-29 | Growth inhibition assay | 96 h | Growth inhibition of human HT-29 cells after 96 hrs by ATPlite luminescence assay IC50=0.429 μM | 24237195 | |
| MCF7 | Growth inhibition assay | 96 h | Growth inhibition of human MCF7 cells after 96 hrs by ATPlite luminescence assay IC50=0.637 μM | 24237195 | |
| MDA-MB-231 | Growth inhibition assay | 96 h | Growth inhibition of human MDA-MB-231 cells after 96 hrs by ATPlite luminescence assay IC50=1.04 μM | 24237195 | |
| MDA-MB-435 | Growth inhibition assay | 96 h | Growth inhibition of human MDA-MB-435 cells after 96 hrs by ATPlite luminescence assay IC50=1.44 μM | 24237195 | |
| MDA-MB-468 | Growth inhibition assay | 96 h | Growth inhibition of human MDA-MB-468 cells after 96 hrs by ATPlite luminescence assay IC50=2.73 μM | 24237195 | |
| MIAPaCa2 | Growth inhibition assay | 96 h | Growth inhibition of human MIAPaCa2 cells after 96 hrs by ATPlite luminescence assay IC50=0.468 μM | 24237195 | |
| PANC1 | Growth inhibition assay | 96 h | Growth inhibition of human PANC1 cells after 96 hrs by ATPlite luminescence assay IC50=1.104 μM | 24237195 | |
| PC3 | Growth inhibition assay | 96 h | Growth inhibition of human PC3 cells after 96 hrs by ATPlite luminescence assay IC50=2.16 μM | 24237195 | |
| T47D | Growth inhibition assay | 96 h | Growth inhibition of human T47D cells after 96 hrs by ATPlite luminescence assay IC50=0.649 μM | 24237195 | |
| SK-N-MC | Growth inhibition assay | 96 h | Growth inhibition of human SK-N-MC cells after 96 hrs by ATPlite luminescence assay IC50=0.329 μM | 24237195 | |
| U87 | Growth inhibition assay | 96 h | Growth inhibition of human U87 cells after 96 hrs by ATPlite luminescence assay IC50=1.16 μM | 24237195 | |
| Hs | Growth inhibition assay | 96 h | Growth inhibition of human Hs 578T cells after 96 hrs by ATPlite luminescence assay IC50=1.7 μM | 24237195 | |
| HER218 | Growth inhibition assay | 96 h | Growth inhibition of human HER218 cells after 96 hrs by ATPlite luminescence assay IC50=0.612 μM | 24237195 | |
| HCT116 | Growth inhibition assay | 96 h | Growth inhibition of human HCT116 cells after 96 hrs by ATPlite luminescence assay IC50=0.614 μM | 24237195 | |
| BT20 | Growth inhibition assay | 96 h | Growth inhibition of human BT20 cells after 96 hrs by ATPlite luminescence assay IC50=0.489 μM | 24237195 | |
| BT549 | Growth inhibition assay | 96 h | Growth inhibition of human BT549 cells after 96 hrs by ATPlite luminescence assay IC50=1.01 μM | 24237195 | |
| AN3CA | Growth inhibition assay | 96 h | Growth inhibition of human AN3CA cells after 96 hrs by ATPlite luminescence assay IC50=0.356 μM | 24237195 | |
| HCT116 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human HCT116 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.33 μM. | 27524309 | |
| MCF7 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MCF7 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 0.44 μM. | 27524309 | |
| DU145 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human DU145 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.62 μM. | 27524309 | |
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 0.65 μM. | 27524309 | |
| MDA-MB-231 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human MDA-MB-231 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.75 μM. | 27524309 | |
| A2780 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human A2780 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.77 μM. | 27524309 | |
| A549 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human A549 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 0.83 μM. | 27524309 | |
| MDA-MB-231 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MDA-MB-231 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 1.4 μM. | 27524309 | |
| NCI-H1299 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human NCI-H1299 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 1.73 μM. | 27524309 | |
| A2780 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A2780 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 2.14 μM. | 27524309 | |
| A549 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human A549 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 2.69 μM. | 27524309 | |
| NCI-H1299 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human NCI-H1299 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 3.01 μM. | 27524309 | |
| PC3 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human PC3 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 4.45 μM. | 27524309 | |
| SMMC7721 | Antiproliferative assay | 96 hrs | Antiproliferative activity against human SMMC7721 cells over-expressing LSD1 assessed as reduction in cell viability measured after 96 hrs by MTT assay, IC50 = 5.36 μM. | 27524309 | |
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 13.08 μM. | 27524309 | |
| LSD1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SMMC7721 over-expressing LSD1 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 15.75 μM. | 27524309 | |
| PC3 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human PC3 cells over-expressing LSD1 assessed as reduction in cell viability measured after 72 hrs by MTT assay, IC50 = 19.72 μM. | 27524309 | |
| H460 | Antiproliferative assay | 48 to 72 hrs | Antiproliferative activity against human H460 cells after 48 to 72 hrs by MTT assay, IC50 = 0.47 μM. | 29754076 | |
| MCF7 | Antiproliferative assay | 48 to 72 hrs | Antiproliferative activity against human MCF7 cells after 48 to 72 hrs by MTT assay, IC50 = 0.62 μM. | 29754076 | |
| Raji | Antiproliferative assay | 48 to 72 hrs | Antiproliferative activity against human Raji cells after 48 to 72 hrs by MTT assay, IC50 = 0.98 μM. | 29754076 | |
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | 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。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在AML细胞中，SP2509抑制LSD1与CoREST联合，增加启动子特异性H3K4Me3，并诱导p53，p21和C/EBPα。SP250也显著抑制菌落生长，并诱导OCI-AML3的细胞凋亡。此外，SP2509诱导培养的和原代AML细胞的增殖，并且与panobinostat结合使用时，发挥协同致死性。[1] | |||
|---|---|---|---|---|
| 激酶实验 | SP2509 活性检测 | |||
| 测试化合物在100% DMSO中稀释至20 ×所需的测试浓度，并将2.5 μL稀释的药物样品加入到黑色384孔板。LSD1酶储液用测试缓冲液稀释17倍，将40 μL稀释的LSD1酶加入到适当的孔中。然后将由辣根过氧化物酶，二甲基K4肽相应的组蛋白H3 N端尾部的前21个氨基酸，和10-乙酰基-3,7-二羟吩恶嗪组成的底物加入孔中。Resorufin在Envision平板阅读器上以530 nm的激发波长和595 nm的发射波长进行分析。SP2509对其他氧化酶的活性使用市售试剂盒测定。葡萄糖氧化酶活性(其在扩张的构象中非共价结合FAD)，使用葡萄糖氧化酶试剂盒测定。MAO测定使用MAO-glo试剂盒与MAO-A 和 MAO-B进行。 | ||||
| 细胞实验 | 细胞系 | OCI-AML3，MV4-11 和 MOLM13 细胞 | ||
| 浓度 | ~10 μM | |||
| 孵育时间 | 96小时 | |||
| 方法 | 培养的AML细胞用SP2509 和/或PS处理96小时。在处理结束时，细胞用游离药物清洗3遍，每种条件下的500个细胞接种于甲基纤维素，并在37 °C下培养。菌落形成在接种7–10天后测量。 | |||
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在负荷OCI-AML3异种移植物的小鼠体内，SP2509 (25 mg/kg i.p.)显著提高小鼠的存活率，与SP2509和panobinostat联合治疗发挥出优良的体内活性。 | |
|---|---|---|
| 动物实验 | Animal Models | 负荷 OCI-AML3 异种移植物的NOD/SCID小鼠 |
| Dosages | 20% Cremaphor，20% DMSO，60% 无菌水 | |
| Administration | i.p. | |
化学信息&溶解度
| 分子量 | 437.90 | 分子式 | C19H20ClN3O5S |
| CAS号 | 1423715-09-6 | SDF | Download SP2509 SDF |
| Smiles | CC(=NNC(=O)C1=CC(=CC=C1)S(=O)(=O)N2CCOCC2)C3=C(C=CC(=C3)Cl)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 83 mg/mL ( (189.54 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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