INDY

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

INDY 

INDY 是一种有效，ATP 竞争性的 Dyrk1A 和 Dyrk1B 抑制剂，IC50 分别为 0.24 μM 和 0.23 μM。INDY 结合在酶的 ATP 口袋中，对 Dyrk1A 的 Ki 值为 0.18 μM。INDY 大大降低了原代胶质母细胞瘤 (GBM) 细胞系和神经祖细胞中正常细胞和致瘤细胞的自我更新能力。

INDY

INDY Chemical Structure

CAS No. : 1169755-45-6

规格 价格 是否有货
5 mg ￥2700 询问价格 & 货期
10 mg ￥4500 询问价格 & 货期

* Please select Quantity before adding items.

生物活性

INDY is a potent and ATP-competitive Dyrk1A and Dyrk1B inhibitor with IC50s of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has a Ki value of 0.18 μM for Dyrk1A. INDY sharply reduces the self-renewal capacity of normal and tumorigenic cells in primary Glioblastoma (GBM) cell lines and neural progenitor cells[1][2].

IC50 & Target

IC50: 0.24 μM (Dyrk1A) and 0.23 μM (Dyrk1B)[1]
Ki: 0.18 μM (Dyrk1A)[1]
体外研究
(In Vitro)

INDY (0.3-30 μM; 20 hours) mildly inhibits tau-phosphorylation at 3 μM, and nearly completely inhibits at 30 μM[1].
INDY effectively reverses the aberrant tau-phosphorylation and rescues the repressed NFAT (nuclear factor of activated T cell) signalling induced by Dyrk1A (dual-specificity tyrosine-(Y)-phosphorylation-regulated kinase 1A) overexpression[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: COS7 cells transfected with either EGFP-Dyrk1A and EGFP-tau
Concentration: 0.3, 1, 3, 10, 30 μM
Incubation Time: 20 hours
Result: Mildly inhibited tau-phosphorylation at 3 μM, and nearly completely inhibited at 30 μM.

体内研究
(In Vivo)

ProINDY (2.5 μM) recoveres apparently normal development of the Xenopus embryo[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

235.30

Formula

C12H13NO2S
CAS 号

1169755-45-6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Ogawa Y, et al. Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A. Nat Commun. 2010 Oct 5;1:86.

    [2]. Pozo N, et al. Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastomagrowth. J Clin Invest. 2013 Jun;123(6):2475-87.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务