INDY is a potent, ATP-competitive inhibitor of Dyrk1A and Dyrk1B with IC50 of 0.24 μM and 0.23 μM, respectively. INDY binds in the ATP pocket of the enzyme and has Ki of 0.18 μM for Dyrk1A. INDY greatly reduces the self-renewal capacity of normal and tumorigenic cells in primary glioblastoma (GBM) cell lines and neural progenitor cells.

Physicochemical Properties

Molecular Formula	C12H13NO2S
Molecular Weight	235.302
Exact Mass	235.067
CAS #	1169755-45-6
Related CAS #	1169755-45-6;
PubChem CID	44136031
Appearance	Off-white to light yellow solid powder
LogP	2.078
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	2
Heavy Atom Count	16
Complexity	316
Defined Atom Stereocenter Count	0
SMILES	CCN\1C2=C(C=CC(=C2)O)S/C1=C\C(=O)C
InChi Key	GCSZJMUFYOAHFY-SDQBBNPISA-N
InChi Code	InChI=1S/C12H13NO2S/c1-3-13-10-7-9(15)4-5-11(10)16-12(13)6-8(2)14/h4-7,15H,3H2,1-2H3/b12-6-
Chemical Name	(1Z)-1-(3-ethyl-5-hydroxy-1,3-benzothiazol-2-ylidene)propan-2-one
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vitro	At 3 μM and 30 μM, INDY (0.3-30 μM; 20 hours) virtually totally blocks tau phosphorylation [1]. Nuclear factor of activated T cells, or NFAT, signaling is blocked when acid-(Y)-phosphorylation regulator 1A is overexpressed [1].
ln Vivo	ProINDY (2.5 μM) significantly restores synchronized normal development in Xenopus laevis [1].
Cell Assay	Western Blot Analysis[1] Cell Types: COS7 cells transfected with EGFP-Dyrk1A and EGFP-tau Tested Concentrations: 0.3, 1, 3, 10, 30 μM Incubation Duration: 20 hrs (hours) Experimental Results: Mild inhibition of tau phosphorylation at 3 μM , almost complete inhibition at 30 μM.
References	[1]. Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A. Nat Commun. 2010 Oct 5;1:86. [2]. Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastomagrowth. J Clin Invest. 2013 Jun;123(6):2475-87.
Additional Infomation	INDY is a member of the class of benzothiazoles that is 2,3-dihydro-1,3-benzothiazole substituted by 2-oxopropylidene, ethyl, and hydroxy groups at positions 2, 3 and 5, respectively. It is an ATP-competitive inhibitor of Dyrk1A and Dyrk1B (IC50 of 0.24 muM and 0.23 muM, respectively). It has a role as an antineoplastic agent, a drug metabolite and an EC 2.7.12.1 (dual-specificity kinase) inhibitor. It is a member of benzothiazoles, an organic hydroxy compound and an enone.

Solubility Data

Solubility (In Vitro)

DMSO : ≥ 33.33 mg/mL (~141.65 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (10.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	4.2499 mL	21.2495 mL	42.4989 mL
	5 mM	0.8500 mL	4.2499 mL	8.4998 mL
	10 mM	0.4250 mL	2.1249 mL	4.2499 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.