SP2509

SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.

CAS No. 1423715-09-6

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 71500	国内在庫あり
100mg	JPY 149500	国内在庫あり
1g	JPY 220500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（25）

カスタマーフィードバック1个实验数据

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

SP2509関連製品

関連ターゲット	KDM1 KDM2 KDM3 KDM4 KDM5 KDM6	もっと見る
関連製品	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	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ	もっと見る

シグナル伝達経路

Histone Demethylaseシグナル伝達経路

Histone Demethylase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

SP2509 (HCI-2509) is a selective histone demethylase LSD1 inhibitor with IC50 of 13 nM, showing no activity against MAO-A, MAO-B, lactate dehydrogenase and glucose oxidase. SP2509 induces apoptosis and promotes autophagy.

Targets

LSD1 ^[1]
(Cell-free assay)

13 nM

In Vitro
In vitro	In AML cells, SP2509 inhibits the association of LSD1 with CoREST, increases promoter-specific H3K4Me3 and induces p53, p21 and C/EBPα. SP2509 also significantly inhibits the colony growth and induces apoptosis of OCI-AML3. In addition, SP2509 induces differentiation of cultured and primary AML cells, and exerts synergistic lethal activity when used in combination with panobinostat. ^[1]
Kinase Assay	SP2509 activity assays
Kinase Assay	Test compounds are diluted to 20 × the desired test concentration in 100% DMSO and 2.5 μL of the diluted drug sampleis added to a black 384-well plate. The LSD1 enzyme stock is diluted 17-fold with assay buffer and 40 μL of the diluted LSD1 enzyme is added to the appropriate wells. Substrate, consisting of horseradish peroxidase, dimethyl K4 peptide corresponding to the first 21 amino acids of the N-terminal tail of histone H3, and 10-acetyl-3,7-dihydroxyphenoxazine is then added to wells. Resorufin is analyzed on an Envision plate reader with an excitation wavelength of 530 nm and an emission wavelength of 595 nm. The activity of SP2509 on the other oxidases is determined by using commercially available kits. The glucose oxidase activity (which also noncovalently binds FAD in an elongate conformation), is determined using the glucose oxidase kit. The MAO assays are performed using the MAO-glo kit with MAO-A and MAO-B.
細胞実験	細胞株	OCI-AML3, MV4-11 and MOLM13 cells
	濃度	~10 μM
	反応時間	96 hours
	実験の流れ	Cultured AML cells are treated with SP2509 and/or PS for 96 h. At the end of treatment, cells are washed free of the drugs and 500 cells per condition are plated in methylcellulose and incubated at 37 °C. Colony formation is measured 7–10 days after plating.

In Vivo
In Vivo	In mice bearing OCI-AML3 xenografts, SP2509 (25 mg/kg i.p.) significantly improved the survival of the mice, while co-treatment with SP2509 and panobinostat exerts superior in vivo activity.
動物実験	動物モデル	NOD/SCID mice bearing OCI-AML3 xenografts
	投与量	20% Cremaphor, 20% DMSO, 60% sterile water
	投与経路	i.p.

参考
[1] Fiskus W, et al. Leukemia. 2014, 28(11), 2155-2164.

参考

[1] Fiskus W, et al. Leukemia. 2014, 28(11), 2155-2164.

化学情報

分子量	437.90	化学式	C₁₉H₂₀ClN₃O₅S
CAS No.	1423715-09-6	SDF	Download SP2509 SDFをダウンロードする
Smiles	CC(=NNC(=O)C1=CC(=CC=C1)S(=O)(=O)N2CCOCC2)C3=C(C=CC(=C3)Cl)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 83 mg/mL ( (189.54 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):