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Description: ATP-competitive inhibitor of DAPK and ZIPK
Chemical Name: 2-[[1-(3-Chlorophenyl)-4,5-dihydro-4-oxo-1H-pyrazolo[3,4-d]pyrimidin-6-yl]thio]propanamide
Purity: ≥98% (HPLC)
Biological Activity
ATP-competitive inhibitor of DAPK (IC50 = 200 nM) and ZIPK (Kd = 280 nM). Also inhibits PIM3 kinase (IC50 = 200 nM) but exhibits no significant effect on Src or Abl kinases. Reduces phosphorylation of regulatory myosin light chain and myosin light chain phosphatase in mouse aortic and rabbit ileal tissues.
Technical Data
| M. Wt | 349.8 |
| Formula | C14H12CIN5O2S |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1030203-81-6 |
| PubChem ID | 42938883 |
| InChI Key | BDVPSWBRXLWRCV-UHFFFAOYSA-N |
| Smiles | O=C1NC(SC(C(N)=O)C)=NC2=C1C=NN2C3=CC=CC(Cl)=C3 |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 17.49 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 349.8. 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 |
|---|---|---|---|
| 0.5 mM | 5.72 mL | 28.59 mL | 57.18 mL |
| 2.5 mM | 1.14 mL | 5.72 mL | 11.44 mL |
| 5 mM | 0.57 mL | 2.86 mL | 5.72 mL |
| 25 mM | 0.11 mL | 0.57 mL | 1.14 mL |
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References
References are publications that support the biological activity of the product.
MacDonald et al (2016) A Small Molecule Pyrazolo[3,4-d]Pyrimidinone Inhibitor of Zipper-Interacting Protein Kinase Suppresses Calcium Sensitization of Vascular Smooth Muscle. Mol.Pharmacol. 89 105 PMID: 26464323
Carlson et al (2013) Fluorescence linked enzyme chemoproteomic strategy for discovery of a potent and selective DAPK1 and ZIPK inhibitor. ACS.Chem.Biol. 8 2715 PMID: 24070067
If you know of a relevant reference for HS 38, please let us know.
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Keywords: HS 38, HS 38 supplier, HS38, ATP-competitive, inhibitors, inhibits, DAPK, ZIPK, PIM3, kinase, regulatory, myosin, light, chain, llight, phosphatase, 5768, Tocris Bioscience
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Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
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