INDY |
| Katalog-Nr.GC16126 |
INDY ist ein potenter und ATP-kompetitiver Dyrk1A- und Dyrk1B-Inhibitor mit IC50-Werten von 0,24 μM bzw. 0,23 μM. INDY bindet in die ATP-Tasche des Enzyms und hat einen Ki-Wert von 0,18 μM fÜr Dyrk1A. INDY reduziert die SelbsterneuerungskapazitÄt normaler und tumorigener Zellen in primÄren Glioblastom (GBM)-Zelllinien und neuralen VorlÄuferzellen stark.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1169755-45-6
Sample solution is provided at 25 µL, 10mM.
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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.
| Cas No. | 1169755-45-6 | 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 |
| Löslichkeit | DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:20): 0.05 mg/ml,Ethanol: slightly soluble | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.2499 mL | 21.2495 mL | 42.4989 mL |
| 5 mM | 0.85 mL | 4.2499 mL | 8.4998 mL |
| 10 mM | 0.425 mL | 2.1249 mL | 4.2499 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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