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- IDR1101-0005MG 產(chǎn)品型號(hào)
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KU-55933,≥99%
【英文同義名】:KU55933, KU 55933.
【中文同義名】:
訂購(gòu)信息:(*,常備現(xiàn)貨)
品 牌 | 產(chǎn)品名稱(chēng) | 產(chǎn)品貨號(hào) | 規(guī) 格 | 目錄價(jià)(元) |
Gene Operation | KU-55933 | IDR1101-0005MG | 5 mg | ¥549.00 |
IDR1101-0010MG | 10 mg | ¥929.00 | ||
IDR1101-0050MG | 50 mg | ¥3,249.00 | ||
IDR1101-0100MG | 100 mg | ¥5,519.00 |
產(chǎn)品描述
是一種高效的,特異的ATM抑制劑,IC50為12.9nM,Ki 值為2.2nM[1]。與作用于DNA-PK, PI3K/PI4K, ATR和mTOR相比,對(duì)ATM具有高度選擇性。通過(guò)誘導(dǎo)G1周期細(xì)胞停滯來(lái)抑制細(xì)胞增殖,還可以*消除雷帕霉素誘導(dǎo)AKT的反饋激活 [2]。此外,抑制ATM依賴(lài)的STAT3激活,是通過(guò)上調(diào)DR5表達(dá)使TRAIL誘導(dǎo)的凋亡增強(qiáng), 然而STAT3和NF-κB活性的抑制都和下調(diào)cFLIP有關(guān),并伴隨著凋亡水平上升[3]。
靶點(diǎn)
Targets | ATM kinase | ATM kinase |
IC50 | 12.9 nM | Ki 2.2 nM[1] |
化學(xué)特性
Cas No.: 587871-26-9 | M. Wt.: 395.49 |
Formula: C21H17NO3S2 | Purity: ≥99% |
Synonym: KU55933, KU 55933. | |
Chemical Name: 2-morpholino-6-(thianthren-1-yl)-4H-pyran-4-one | |
Appearance: White to off-white solid powder | |
Solubility: Soluble in DMSO (33 mg/ml) | |
Storage:Store powder at -20 ºC for the stability of three years. |
結(jié)構(gòu)式
Reference
[1] Hickson I,et al. Identification and characterization of a novel and specific inhibitor of the ataxia-angiectasia mutated kinase ATM. Cancer Res. 64(24):9152-9(2004).
[2] Yan Li,et al. The ATM Inhibitor Suppresses Cell Proliferation and Induces Apoptosis by Blocking Akt In Cancer Cells with Overactivated Akt. Cancer Research. 9(1):113-25(2010).
[3] Ivanov VN, et al. Inhibition of ataxia angiectasia mutated kinase activity enhances TRAIL-mediated apoptosis in human melanoma cells. 69(8):3510-9(2009).