| INDYDyrk1A and Dyrk1B inhibitor, selective |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
INDY Dilution Calculator
calculate
INDY Molarity Calculator
calculate
| 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.
ebiomall.com
>
>
我要提问
您的问题将推送给已购用户，TA们将会为你解答。