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120615-25-0

中文名稱 CKI-7
英文名稱 CKI-7
CAS 120615-25-0
分子式 C11H12ClN3O2S
分子量 285.75
MOL 文件 120615-25-0.mol
更新日期 2023/03/20 15:41:27
120615-25-0 結(jié)構(gòu)式 120615-25-0 結(jié)構(gòu)式

基本信息

中文別名
化合物 T10829
化合物 CKI-7 FREE BASE
英文別名
CKI-7 free base
CKI 7 free base,CKI7 free base
N-(2-Aminoethyl)-5-chloro-8-isoquinolinesulfonamide
N-(2-AMinoethyl)-5-chloro-isoquinolin-8-sulphonaMide
8-Isoquinolinesulfonamide, N-(2-aminoethyl)-5-chloro-
8-[N-(2-Aminoethyl)sulphamoyl]-5-chloroisoquinoline, CKI-7
8-Isoquinolinesulfonamide, N-(2-aminoethyl)-5-chloro- Dihydrochloride

物理化學(xué)性質(zhì)

熔點(diǎn)188-190°C
沸點(diǎn)499.7±55.0 °C(Predicted)
密度1.432±0.06 g/cm3(Predicted)
儲(chǔ)存條件−20°C
溶解度H2O: 9 mg/mL
酸度系數(shù)(pKa)7.80±0.50(Predicted)
形態(tài)solid
顏色white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS06
警示詞危險(xiǎn)
危險(xiǎn)性描述H301
危險(xiǎn)品標(biāo)志T
危險(xiǎn)類別碼25
安全說明45
危險(xiǎn)品運(yùn)輸編號(hào)UN 2811 6.1/PG 3
WGK Germany3
海關(guān)編碼2933499090
CKI-7價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱CAS號(hào)包裝價(jià)格
2024/11/08HY-133028CKI-7
CKI-7 free base
120615-25-05mg850元
2024/11/08HY-133028CKI-7
CKI-7 free base
120615-25-010mg1500元
2024/11/08HY-133028CKI-7
CKI-7 free base
120615-25-010mM * 1mLin DMSO1572元

常見問題列表

生物活性
CKI-7 free base 是一種有效且 ATP 競爭性的酪蛋白激酶 1 (CK1) 抑制劑,IC50 為 6 μM,Ki 為 8.5 μM。CKI-7 free base 選擇性抑制 Cdc7 激酶,還抑制 SGK,S6K1 以及 MSK1。CKI-7 free base 對酪蛋白激酶 II 和其他蛋白激酶的作用弱得多。
靶點(diǎn)

CK1

6 μM (IC 50 )

CK1

8.5 μM (Ki)

Cdc7

SGK

S6K1

MSK1

體外研究

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.
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.

RT-PCR

Cell Line: Mouse ES cells
Concentration: 0.1-10 μM
Incubation Time: 5 days
Result: Significantly increased 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.

Western Blot Analysis

Cell Line: Mouse ES cells
Concentration: 5 μM
Incubation Time: 5 days
Result: Suppressed SFEB-induced β-catenin stabilization on day 5.
體內(nèi)研究

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.

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