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compound 3i (666-15)

Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.

compound 3i (666-15)化学構造

CAS No. 1433286-70-4

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫なし(納期7~10日)
JPY 22000 国内在庫なし(納期7~10日)
JPY 82000 国内在庫なし(納期7~10日)
JPY 145500 国内在庫なし(納期7~10日)
JPY 598500 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（13）

製品安全説明書

現在のバッチを見る： S884601 DMSO] 100 mg/mL] false] Ethanol] 3 mg/mL] false] Water] Insoluble] false 純度： 99.85%
99.85

compound 3i (666-15)関連製品

シグナル伝達経路

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domainシグナル伝達経路

Epigenetic Reader Domain阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
HEK293T Function assay 50 nM 1 hr Inhibition of CREB-mediated gene transcription in human HEK293T cells assessed as inhibition of forskolin-stimulated Nurr1/NR4A2 transcription at 50 nM after 1 hr by qRT-PCT analysis 26023867
HEK293T Function assay > 1 uM 30 mins Inhibition of VP16/CREB (unknown origin) interaction in human HEK293T cells assessed as inhibition of forskolin-stimulated gene transcription at > 1 uM after 30 mins by CRE-RLuc complementation assay 26023867
HEK293T Function assay > 1 uM 30 mins Inhibition of P53 (unknown origin) transfected in human HEK293T cells assessed as inhibition of forskolin-stimulated gene transcription at > 1 uM after 30 mins by CRE-RLuc complementation assay 26023867
MDA-MB-468 Antitumor assay 10 mg/kg 5 weeks Antitumor activity against human MDA-MB-468 cells xenografted in BALB/c mouse assessed as reduction in tumor volume at 10 mg/kg, ip once a day, 5 days per week for 5 weeks relative to control 26023867
HEK293T Function assay 100 nM 1 hr Inhibition of CREB in HEK293T cells assessed as inhibition of Fsk-induced NR4A2 gene expression at 100 nM pre-incubated for 1 hr before Fsk stimulation for 45 mins by qRT-PCR analysis 31765143
MDA-MB-468 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, GI50=0.046μM 26023867
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, GI50=0.073μM 26023867
HEK293T Function assay 30 mins Inhibition of CREB (unknown origin) expressed in HEK293T cells assessed as inhibition of forskolin-induced CREB transcription activity incubated for 30 mins by luciferase reporter gene assay, IC50=0.081μM 31765143
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, GI50=0.31μM 26023867
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay, GI50=0.47μM 26023867
HEK293T Function assay 30 mins Inhibition of NFkappaB (unknown origin)-mediated gene transcription in human HEK293T cells transfected with an NFkappaB firefly luciferase reporter gene assessed as inhibition of TNFalpha-stimulated gene transcription pretreated for 30 mins measured after, IC50=5.29μM 26023867
HEK293T Function assay Inhibition of CREB-mediated gene transcription in human HEK293T cells transfected with pCRE-RLuc by renilla luciferase reporter assay, IC50=0.081μM 26023867
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生物活性

製品説明 Compound 3i (666-15) is a potent and selective inhibitor of CREB-mediated gene transcription (IC50 = 0.081 ± 0.04 μM) and also potently inhibits cancer cell growth without harming normal cells.
Targets
CREB [1]
81 nM
In Vitro
In vitro

666-15 could potently inhibit cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI50 for 666-15 is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibit robust activity as well with GI50 of 0.47 and 0.31 μM. 666-15 inhibits CREB’s transcription activity in living cells independent of direct CREB or CBP binding interaction[1].
細胞実験 細胞株 HEK 293T cells
濃度 0.05, 0.1, 0.5 μM
反応時間 --
実験の流れ

HEK 293T cells are treated with different concentrations of 666-15 followed by treatment with forskolin. Then the relative mRNA level of Nurr1/NR4A2 is determined by qRT-PCR analysis.
In Vivo
In Vivo

In an in vivo MDA-MB-468 xenograft model, 666-15 completely suppresses the tumor growth without overt toxicity. Preliminary toxicity studies show that intraperitoneal (ip) injection of 10 mg/kg of 666-15 is well tolerated in mice[1].
動物実験 動物モデル 6- to 8-week old BALB/c nude mouse inoculated subcutaneously at the right flank with MDA-MB-468 cells
投与量 10 mg/kg
投与経路 IP

化学情報

分子量 620.52 化学式

C33H31Cl2N3O5
CAS No. 1433286-70-4 SDF --
Smiles C1=CC=C2C=C(C(=CC2=C1)C(=O)NCCOC3=CC4=CC=CC=C4C=C3C(=O)NC5=C(C=C(C=C5)Cl)O)OCCCN.Cl
保管 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (161.15 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。)

Ethanol : 3 mg/mL

Water : 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

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）

mg/kg g μL 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。

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Handling Instructions

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