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Submit ReviewMRK 740
Description: Potent PRDM9 inhibitor
Chemical Name: 3-(3,5-Dimethoxyphenyl)-5-(1-methyl-9-(2-methylpyridin-4-yl)-1,4,9-triazaspiro[5.5]undecan-4-yl)-1,2,4-oxadiazole
Purity: ≥98% (HPLC)
Biological Activity for MRK 740
MRK 740 is a potent PRDM9 histone methyltransferase inhibitor (IC50 = 85 nM for in vitro methylation of H3K4), which displays >100-fold selectivity over other histone methyltransferases. MRK 740 inhibits H3K4 methylation in cells (IC50 = 0.8 μM).
Licensing Information
This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the MRK-740 probe summary on the SGC website.
External Portal Information for MRK 740
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of MRK 740 is reviewed on the chemical probes website.
Compound Libraries for MRK 740
MRK 740 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for MRK 740
| M. Wt | 464.56 |
| Formula | C25H32N6O3 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 2387510-80-5 |
| PubChem ID | 137331596 |
| InChI Key | NZYTZRHHBAJPKN-UHFFFAOYSA-N |
| Smiles | CC1=CC(N2CCC3(CC2)CN(CCN3C)C4=NC(C5=CC(OC)=CC(OC)=C5)=NO4)=CC=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 MRK 740
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.46 | 100 | |
| 1eq. HCl | 46.46 | 100 |
Preparing Stock Solutions for MRK 740
The following data is based on the product molecular weight 464.56. 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 | 2.15 mL | 10.76 mL | 21.53 mL |
| 5 mM | 0.43 mL | 2.15 mL | 4.31 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.15 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets for MRK 740
References for MRK 740
References are publications that support the biological activity of the product.
Allali-Hassani et al (2019) Discovery of a chemical probe for PRDM9. Nat.Commun. 10 5759 PMID: 31848333
If you know of a relevant reference for MRK 740, please let us know.
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Keywords: MRK 740, MRK 740 supplier, MRK740, histone, lysine, methyltransferase, inhibitors, inhibits, potent, PRDM9, PR, domain, zinc, finger, protein, 9, Other, Lysine, Methyltransferases, 6803, Tocris Bioscience
Citations for MRK 740
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