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INDY
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
INDY图片
CAS NO:1169755-45-6
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
INDY 是一种有效的 ATP 竞争性 Dyrk1A 和 Dyrk1B 抑制剂，IC50 分别为 0.24 μM 和 0.23 μM。 INDY 与酶的 ATP 口袋结合，对 Dyrk1A 的 Ki 值为 0.18 μM。 INDY 大幅降低原发性胶质母细胞瘤 (GBM) 细胞系和神经祖细胞中正常和致瘤细胞的自我更新能力。
Cas No.1169755-45-6
化学名(Z)-1-(3-ethyl-5-hydroxybenzo[d]thiazol-2(3H)-ylidene)propan-2-one
Canonical SMILESCCN(/C1=C([H])/C(C)=O)C2=C(S1)C=CC(O)=C2
分子式C12H13NO2S
分子量235.3
溶解度DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml,Ethanol: slightly soluble
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

INDY is a selective inhibitor of Dyrk1A and Dyrk1B with IC50 values of 0.23 and 0.24 μM, respectively [1].

Dual-specificity tyrosine-(Y) -phosphorylation-regulated kinase 1A (Dyrk1A) is a serine/threonine kinase expressed in adult brains as well as fetal and phosphorylates myriad proteins. DYRK1B regulates nuclear functions mainly expressed in muscle and testis [1].

INDY is a selective Dyrk1A and Dyrk1B inhibitor. INDY inhibited Dyrk1A against ATP with Km and Ki of 37 and 0.18 μM, respectively. INDY (10 μM) exhibited > 90% inhibition on CLK1, CLK4, DYRK2, DYRK3, casein kinase 1 (CSNK1D) and PIM1. In COS7 cells, INDY (3 μM) inhibited tau-phosphorylation induced by Dyrk1A. In HEK293 cells, Dyrk1A inhibited the nuclear accumulation of NFATc1, while INDY relocated NFATc1 into the nucleus [1]. In EGFR-expressing glioblastomas tumor-initiating cells (GBM-TICs), INDY impaired cells self-renewal capacity and inhibited tumor growth and survival [2].

In X. laevis embryo overexpressed xDyrk1A, deformity was observed in the head and the eye of stage 40/41 tadpoles. While proINDY rescued the morphological abnormalities [1].

References:
[1]. Ogawa Y, Nonaka Y, Goto T, et al. Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A. Nat Commun, 2010, 1: 86.
[2]. Pozo N, Zahonero C, Fernández P, et al. Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastoma growth. J Clin Invest, 2013, 123(6): 2475-2487.