SP2509

别名: HCI-2509

目录号：S7680 Purity: 99.99%

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

规格	价格	库存
10mM (1mL in DMSO)	1367.73	现货
5mg	1204.84	现货
25mg	3883.86	现货
100mg	8155.08	现货
1g	12039.3	现货
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产品质控

批次：纯度： 99.99%

99.99

SP2509相关产品

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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 高选择性抑制剂库	点击展开

细胞实验数据示例

细胞系	实验类型	孵育时间	活性描述	文献信息(PMID)
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

靶点

LSD1 ^[1]
(Cell-free assay)

13 nM

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。
激酶实验	SP2509 活性检测
激酶实验	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。

参考文献
https://pubmed.ncbi.nlm.nih.gov/24699304/

参考文献

https://pubmed.ncbi.nlm.nih.gov/24699304/

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

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

DMSO : 38 mg/mL ( (86.77 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

体内溶解配方批次：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
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	7.000mg/ml (15.99mM)	以 1 mL 工作液为例,取50μL140mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!
均匀悬浊液	CMC-NA	≥5mg/ml	以 1 mL 工作液为例，取 5 mg该产品加到 1 ml CMC-NA 溶液中，混合均匀，即可得工作液浓度为 5 mg/ml的均匀悬浊液。
澄清溶液	10%DMSO 1 90%Corn oil 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	5.000mg/ml (11.42mM)	以 1 mL 工作液为例，取100μL50mg/ml的澄清DMSO储备液加到900μL玉米油中，混合均匀。工作液请现配现用！
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 该配方已经过Selleck实验室实测。如果上述溶解方案不能满足您的需求，可联系Selleck销售提供定制化测试。	3.500mg/ml (7.99mM)	以 1 mL 工作液为例,取50μL70mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

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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* 必填项

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