4-QuinazolinaMine, 7-[3-(diMethylaMino)propoxy]-2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6-Methoxy-N-(1-Methyl-4-piperidinyl)-
UNC0224
CAS: 1197196-48-7
Molecular Formula: C26H43N7O2
4-QuinazolinaMine, 7-[3-(diMethylaMino)propoxy]-2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6-Methoxy-N-(1-Methyl-4-piperidinyl)- - Names and Identifiers
4-QuinazolinaMine, 7-[3-(diMethylaMino)propoxy]-2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6-Methoxy-N-(1-Methyl-4-piperidinyl)- - Physico-chemical Properties
| Molecular Formula | C26H43N7O2 |
| Molar Mass | 485.67 |
| Density | 1.141±0.06 g/cm3(Predicted) |
| Boling Point | 641.0±65.0 °C(Predicted) |
| Solubility | Soluble in DMSO |
| pKa | 9.34±0.70(Predicted) |
| Storage Condition | 2-8°C |
| Use | NC0224 is a potent and selective G9a HMTase inhibitor, exhibiting an IC50 value of 15 nM.4 Isothermal titration calorimetry revealed UNC0224 binds to G9a with a Kd value of 29 nM. |
| In vitro study | In G9a ECSD and CLOT assays, the IC 50 values of 43 nM and 57 nM for UNC0224 (Compound 10), respectively. In GLP ECSD and CLOT assays, the IC 50 values of 50 nM and 58 nM for UNC0224, respectively. In ITC experiments, the K d value of UNC0224 to the G9a protein is 23 nM. |
4-QuinazolinaMine, 7-[3-(diMethylaMino)propoxy]-2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6-Methoxy-N-(1-Methyl-4-piperidinyl)- - Reference
| Reference Show more | 1: Liu F, Chen X, Allali-Hassani A, Quinn AM, Wigle TJ, Wasney GA, Dong A, Senisterra G, Chau I, Siarheyeva A, Norris JL, Kireev DB, Jadhav A, Herold JM, Janzen WP, Arrowsmith CH, Frye SV, Brown PJ, Simeonov A, Vedadi M, Jin J. Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2,4-diamino-7-aminoalkoxy-quinazolines. J Med Chem. 2010 Aug 12;53(15):5844-57. doi: 10.1021/jm100478y. PubMed PMID: 20614940; PubMed Central PMCID: PMC2920043. 2: Liu F, Chen X, Allali-Hassani A, Quinn AM, Wasney GA, Dong A, Barsyte D, Kozieradzki I, Senisterra G, Chau I, Siarheyeva A, Kireev DB, Jadhav A, Herold JM, Frye SV, Arrowsmith CH, Brown PJ, Simeonov A, Vedadi M, Jin J. Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a. J Med Chem. 2009 Dec 24;52(24):7950-3. doi: 10.1021/jm901543m. PubMed PMID: 19891491; PubMed Central PMCID: PMC2825141. |
4-QuinazolinaMine, 7-[3-(diMethylaMino)propoxy]-2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6-Methoxy-N-(1-Methyl-4-piperidinyl)- - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.059 ml | 10.295 ml | 20.59 ml |
| 5 mM | 0.412 ml | 2.059 ml | 4.118 ml |
| 10 mM | 0.206 ml | 1.03 ml | 2.059 ml |
| 5 mM | 0.041 ml | 0.206 ml | 0.412 ml |
Last Update：2024-01-02 23:10:35
4-QuinazolinaMine, 7-[3-(diMethylaMino)propoxy]-2-(hexahydro-4-Methyl-1H-1,4-diazepin-1-yl)-6-Methoxy-N-(1-Methyl-4-piperidinyl)- - Reference Information
| biological activity | UNC0224 is an effective selective histone methyltransferase G9a inhibitor, Ki is 2.6 nM,IC50 value is 15 nM,Kd is 23 nM. UNC0224 also effectively inhibited GLP with an IC50 value of 20-58 nM. UNC0224 was inactive for SET7/9,SET8/PreSET7,PRMT3 and JMJD2E. |
| target | G9a 15 nM (IC 50 ) G9a 2.6 nM (Ki) G9a 23 nM (Kd) GLP 20-58 nM (IC 50 ) |
| in vitro study | In G9a ECSD and CLOT assays, the IC 50 values of 43 nM and 57 nM for UNC0224 (Compound 10), respectively. In GLP ECSD and CLOT assays, the IC 50 values of 50 nM and 58 nM for UNC0224, respectively. In ITC experiments, the K d value of UNC0224 to the G9a protein is 23 nM. |
Last Update：2024-04-09 21:11:58
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CAS: 1197196-48-7
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CAS: 1197196-48-7
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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