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Description: Potent and highly selective ROCK inhibitor; orally active
Alternative Names: Azaindole-1,BAY-549
Chemical Name: 6-Chloro-N4-[3,5-difluoro-4-[(3-methyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy]phenyl]-2,4-pyrimidinediamine
Purity: ≥98% (HPLC)
Biological Activity for TC-S 7001
TC-S 7001 (also known as BAY-549) is a potent and highly selective ROCK inhibitor (IC50 values are 0.6 and 1.1 nM for human ROCK1 and ROCK2, respectively), which exhibits >200-fold selectivity over TRK and FLT3 receptors, and >900-fold selectivity over a panel of other kinases and cardiovascular relevent enzymes and receptors. TC-S 7001 reduces blood pressure in normotensive and hypertensive rats, and is orally active.
External Portal Information for TC-S 7001
Chemicalprobes.org and the Chemical Probes webpages of the Structural Genomics Consortium are portals that offer independent guidance on the selection and/or application of small molecules for research. The use of TC-S 7001 (BAY 549) is reviewed on chemicalprobes.org and the SGC website.
Technical Data for TC-S 7001
| M. Wt | 402.79 |
| Formula | C18H13ClF2N6O |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 867017-68-3 |
| PubChem ID | 11524200 |
| InChI Key | NRSGWEVTVGZDFC-UHFFFAOYSA-N |
| Smiles | ClC1=CC(NC2=CC(F)=C(OC3=C(C(C)=CN4)C4=NC=C3)C(F)=C2)=NC(N)=N1 |
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 TC-S 7001
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.28 | 100 | |
| ethanol | 40.28 | 100 |
Preparing Stock Solutions for TC-S 7001
The following data is based on the product molecular weight 402.79. 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 | 2.48 mL | 12.41 mL | 24.83 mL |
| 5 mM | 0.5 mL | 2.48 mL | 4.97 mL |
| 10 mM | 0.25 mL | 1.24 mL | 2.48 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets for TC-S 7001
References for TC-S 7001
References are publications that support the biological activity of the product.
Kast et al (2007) Cardiovascular effects of a novel potent and highly selective azaindole-based inhibitor of Rho-kinase. Br.J.Pharmacol. 152 1070 PMID: 17934515
Dahal et al (2010) Therapeutic efficacy of azaindole-1 in experimental pulmonary hypertension. Eur.Resp.J. 36 808 PMID: 20530035
If you know of a relevant reference for TC-S 7001, please let us know.
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Keywords: TC-S 7001, TC-S 7001 supplier, TC-S7001, Azaindole-1, potent, selective, rho-kinase, inhibitors, inhibits, ROCK1, ROCK2, BAY-549, Rho-kinases, 4961, Tocris Bioscience
Citations for TC-S 7001
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Stem Cells Scientific Review
Written by Kirsty E. Clarke, Victoria B. Christie, Andy Whiting and Stefan A. Przyborski, this review provides an overview of the use of small molecules in the control of stem cell growth and differentiation. Key signaling pathways are highlighted, and the regulation of ES cell self-renewal and somatic cell reprogramming is discussed. Compounds available from Tocris are listed.
Stem Cell Workflow Poster
Stem cells have potential as a source of cells and tissues for research and treatment of disease. This poster summarizes some key protocols demonstrating the use of small molecules across the stem cell workflow, from reprogramming, through self-renewal, storage and differentiation to verification. Advantages of using small molecules are also highlighted.
Stem Cells Poster
Written by Rebecca Quelch and Stefan Przyborski from Durham University (UK), this poster describes the isolation of pluripotent stem cells, their maintenance in culture, differentiation, and the generation and potential uses of organoids.