476496 Sigma-AldrichProtein Lysine Methyltransferase Inhibitor, UNC0321 - Calbiochem
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Overview
Key Spec Table
| Empirical Formula |
|---|
| C₂₇H₄₅N₇O₃ |
Products
| Catalogue Number | Packaging | Qty/Pack | |
|---|---|---|---|
| 476496-5MG | Glass bottle | 5 mg |
| Description | |
|---|---|
| Overview | A cell-permeable, quinazoline analog that potently and selectively inhibits PKMT G9a (IC50 = 6 nM and 9 nM in two biochemical assays for CLOT and ECSD, respectively, and Ki = 63 pM, which is approximately 250-fold more potent than a closely-related analog, BIX01294 (Cat. No. 382190)). It inhibits GLP with reduced potency (15 nM) and is found to be inactive (IC50 > 40 µM) toward other protein lysine and arginine methyltransferases, such as SET7/9 (aH3K4 PKMT), SET8/PreSET7 (aH4K20 PKMT), and PRMT3, as well as JMJD2E (> 1000-fold selectivity) in ECSD enzymatic assays. It also inhibits H3K9me2 accumulation (IC50 = 11,000 nM) in MDA-MB-231 cells, in comparison to BIX01294 (IC50 = 500 nM). Please note that the molecular weight for this compound is batch-specific due to variable water content. |
| Catalogue Number | 476496 |
| Brand Family | Calbiochem® |
| Synonyms | 7-(2-(2-(Dimethylamino)ethoxy)ethoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine |
| References | |
|---|---|
| References | Liu, F., et al. 2010. J. Med. Chem. 53, 5844. |
| Product Information | |
|---|---|
| Form | Light tan solid |
| Hill Formula | C₂₇H₄₅N₇O₃ |
| Chemical formula | C₂₇H₄₅N₇O₃ |
| Structure formula Image | |
| Quality Level | MQ100 |
| Biological Information | |
|---|---|
| Purity | >98% by HPLC |
| Packaging Information | |
|---|---|
| Packaged under inert gas | Packaged under inert gas |
| Global Trade Item Number | |
|---|---|
| Catalogue Number | GTIN |
| 476496-5MG | 04055977183856 |