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CKI-7

カタログ番号GC38755

CKI-7 は、6 μM の IC50 と 8.5 μM の Ki を持つ強力な ATP 競合カゼインキナーゼ 1 (CK1) 阻害剤です。 CKI-7 は選択的 Cdc7 キナーゼ阻害剤です。 CKI-7 は、SGK、リボソーム S6 キナーゼ 1 (S6K1)、マイトジェンおよびストレス活性化プロテイン キナーゼ 1 (MSK1) も阻害します。 CKI-7 は、カゼイン キナーゼ II および他のプロテイン キナーゼに対してはるかに弱い影響を及ぼします。

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CKI-7 化学構造

Cas No.: 120615-25-0

サイズ 価格 在庫数 個数
1mg
$46.00
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5mg
$79.00
在庫あり
10mg
$139.00
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25mg
$348.00
在庫あり
50mg
$580.00
在庫あり
100mg
$1,038.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases[1][2][3][4].

CKI-7 (0.1-10 μM; 5 days; ES cells) treatment significantly increases the expression of the early neuroectodermal marker Sox1 and the number of cells positive for the neural markers nestin and βIII-tubulin, in a concentration-dependent manner[1].CKI-7 (5 μM; 5 days; ES cells) treatment suppresses SFEB-induced β-catenin stabilization on day 5, indicating that CKI-7 inhibits Wnt signaling[1]. RT-PCR[1] Cell Line: Mouse ES cells

In vivo dose-dependent anti-tumor activity of CKI-7 is demonstrated in a SCID-Beige mouse systemic tumor model utilzing a recently isolated Philadelphia chromosome positive acute lymphoblastic leukemia cell line. Standard cell cycle synchronization studies established that exposure to CKI-7 results in cell cycle dependent caspase 3 activation and apoptotic cell death[2].

[1]. Osakada F, et al. In vitro differentiation of retinal cells from human pluripotent stem cells by small-molecule induction. J Cell Sci. 2009 Sep 1;122(Pt 17):3169-79. [2]. Mark G. Frattini, et al. Small Molecule Inhibition of Cdc7, a Key Cell Cycle Regulator and Novel Therapeutic Target, Successfully Inhibits Leukemia Cell Growth in Vitro and in Vivo. Blood (2008) 112 (11): 2668. [3]. Chijiwa T, et al. A newly synthesized selective casein kinase I inhibitor, N-(2-aminoethyl)-5-chloroisoquinoline-8-sulfonamide, and affinity purification of casein kinase I from bovine testis. J Biol Chem. 1989 Mar 25;264(9):4924-7. [4]. Rena G, et al. D4476, a cell-permeant inhibitor of CK1, suppresses the site-specific phosphorylation and nuclear exclusion of FOXO1a. EMBO Rep. 2004 Jan;5(1):60-5.

Chemical Properties

Cas No. 120615-25-0 SDF
Canonical SMILES O=S(C1=CC=C(Cl)C2=C1C=NC=C2)(NCCN)=O
Formula C11H12ClN3O2S M.Wt 285.75
溶解度 DMSO: 25 mg/mL (87.49 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.4996 mL 17.4978 mL 34.9956 mL
5 mM 0.6999 mL 3.4996 mL 6.9991 mL
10 mM 0.35 mL 1.7498 mL 3.4996 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 11 reference(s) in Google Scholar.)

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