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 29000 国内在庫なし(納期7~10日)
JPY 23100 国内在庫あり
JPY 80700 国内在庫あり

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(12)

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

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
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 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

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。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください
Tags: compound 3i (666-15)を買う | compound 3i (666-15) ic50 | compound 3i (666-15)供給者 | compound 3i (666-15)を購入する | compound 3i (666-15)費用 | compound 3i (666-15)生産者 | オーダーcompound 3i (666-15) | compound 3i (666-15)化学構造 | compound 3i (666-15)分子量 | compound 3i (666-15)代理店