| INDYDyrk1A and Dyrk1B inhibitor, selective |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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| Cas No. | 1169755-45-6 | SDF | Download SDF |
| Chemical Name | (Z)-1-(3-ethyl-5-hydroxybenzo[d]thiazol-2(3H)-ylidene)propan-2-one | ||
| Canonical SMILES | CCN(/C1=C([H])/C(C)=O)C2=C(S1)C=CC(O)=C2 | ||
| Formula | C12H13NO2S | M.Wt | 235.3 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | Pale yellow solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
