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Description: DYRK1A/B inhibitor
Chemical Name: (1Z)-1-(3-Ethyl-5-hydroxy-2(3H)-benzothiazolylidene)-2-propanone
Purity: ≥98% (HPLC)
Biological Activity for INDY
INDY is a DYRK1A/B inhibitor (IC50 values are 0.23 and 0.24 μM, for DYRK1B and DYRKA respectively). Binds at the ATP-binding cleft of the enzyme. Reverses aberrant tau-phosphorylation and rescues repressed calcineurin/NFAT signaling. Impairs the self-renewal capacity of subventricular zone neural stem cells. Also available as a prodrug, proINDY (Cat. No. 4998).
Compound Libraries for INDY
INDY is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Stem Cell Library. Find out more about compound libraries available from Tocris.
Technical Data for INDY
| M. Wt | 235.3 |
| Formula | C12H13NO2S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1169755-45-6 |
| PubChem ID | 69538603 |
| InChI Key | GCSZJMUFYOAHFY-UHFFFAOYSA-N |
| Smiles | O=C(C)/C=C1SC2=CC=C(O)C=C2N\1CC |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for INDY
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.53 | 100 |
Preparing Stock Solutions for INDY
The following data is based on the product molecular weight 235.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4.25 mL | 21.25 mL | 42.5 mL |
| 5 mM | 0.85 mL | 4.25 mL | 8.5 mL |
| 10 mM | 0.42 mL | 2.12 mL | 4.25 mL |
| 50 mM | 0.08 mL | 0.42 mL | 0.85 mL |
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Product Datasheets for INDY
References for INDY
References are publications that support the biological activity of the product.
Pozo et al (2013) Inhibition of DYRK1A destabilizes EGFR and reduces EGFR-dependent glioblastoma growth. J.Clin.Invest. 123 2475 PMID: 23635774
Ogawa et al (2010) Development of a novel selective inhibitor of the Down syndrome-related kinase Dyrk1A. Nat.Commun. 1 86 PMID: 20981014
If you know of a relevant reference for INDY, please let us know.
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Keywords: INDY, INDY supplier, INDY, downs, syndrome-related, kinase, Dyrk1A/B, inhibitors, inhibits, tau, phosphorylation, hyperphosphorylation, calcineurin, NFAT, signalling, self-renewal, neural, stem, cells, NSCs, Microtubules, Stem, Cell, Proliferation, DYRK, 4997, Tocris Bioscience
5 Citations for INDY
Citations are publications that use Tocris products. Selected citations for INDY include:
Wahl et al (2018) Transcriptome analysis of Xenopus orofacial tissues deficient in retinoic acid receptor function. BMC Genomics 19 795 PMID: 30390632
Kim et al (2016) A chemical with proven clinical safety rescues Down-syndrome-related phenotypes in through DYRK1A inhibition. Dis Model Mech 9 839 PMID: 27483355
Peng et al (2020) Pharmacologic and genetic approaches define human pancreatic β cell mitogenic targets of DYRK1A inhibitors. JCI Insight 5 PMID: 31821176
Seu et al (2015) Stable Phenotypic Changes of the Host T Cells Are Essential to the Long-Term Stability of Latent HIV-1 Infection. J Virol 89 6656 PMID: 25878110
Wang et al (2015) A high-throughput chemical screen reveals that harmine-mediated inhibition of DYRK1A increases human pancreatic beta cell replication. Nat Med 21 383 PMID: 25751815
Do you know of a great paper that uses INDY from Tocris? Please let us know.
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Literature in this Area
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