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Antiviral API
- Arenavirus
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- Endogenous Metabolite
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- Antiviral intermediates
UNC-0638
Category | Influenza Virus |
CAS | 1255580-76-7 |
Description | UNC0638 is an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 treatment of a variety of cell lines resulted in lower global H3K9me2 levels, equivalent to levels observed for small hairpin RNA knockdown of G9a and GLP with the functional potency of UNC0638 being well separated from its toxicity. UNC0638 markedly reduced the clonogenicity of MCF7 cells, reduced the abundance of H3K9me2 marks at promoters of known G9a-regulated endogenous genes and disproportionately affected several genomic loci encoding microRNAs. |
Product Information
Synonyms | UNC0638, UNC-0638, UNC 0638 |
Molecular Weight | 509.739 |
Molecular Formula | C30H47N5O2 |
Canonical SMILES | CC(C)N1CCC(CC1)NC2=NC(=NC3=CC(=C(C=C32)OC)OCCCN4CCCC4)C5CCCCC5 |
InChI | InChI=1S/C30H47N5O2/c1-22(2)35-17-12-24(13-18-35)31-30-25-20-27(36-3)28(37-19-9-16-34-14-7-8-15-34)21-26(25)32-29(33-30)23-10-5-4-6-11-23/h20-24H,4-19H2,1-3H3,(H,31,32,33) |
InChIKey | QOECJCJVIMVJGX-UHFFFAOYSA-N |
Boiling Point | 563.9±50.0 °C at 760 mmHg |
Melting Point | 93-94 °C |
Flash Point | 294.8±30.1 °C |
Purity | 0.98 |
Density | 1.1±0.1 g/cm3 |
Solubility | In Vitro: DMSO : ≥ 30 mg/mL (58.85 mM) |
Appearance | white solid powder |
Storage | Powder: -20°C: 3 years 4°C: 2 years In solvent: -80°C: 6 months -20°C: 1 month |
Complexity | 660 |
Exact Mass | 509.37297576 |
Index Of Refraction | 1.587 |
In Vitro | UNC0638, an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.The Ki of UNC0638 is determined to be 3.0±0.05 nM (n=2). Consistent with this, the Morrison Ki for UNC0638 is 3.7±0.2 nM (n=3). The selectivity of UNC0638 over a wide range of epigenetic targets is evaluated. Notably, UNC0638 is inactive against other H3K9 (SUV39H1 and SUV39H2), H3K27 (EZH2), H3K4 (SETD7, MLL and SMYD3), H3K79 (DOT1L) and H4K20 (SETD8) methyltransferases, as well as PRDM1, PRDM10 and PRDM12. In addition, UNC0638 is inactive against protein arginine methyltransferases PRMT1 and PRMT3, and HTATIP, a histone acetyltransferase. Of note, UNC0638 has weak but measurable activity against JMJD2E (IC50=4,500±1,100 nM), a Jumonji protein demethylase and DNA methyltransferase DNMT1 (IC50=107,000±6,000 nM). Nevertheless, the selectivity of UNC0638 for G9a and GLP over JMJD2E is >200-fold, and selectivity for G9a and GLP over DNMT1 is >5,000-fold. UNC0638 is a type of small molecule that can specifically inhibit the enzyme activity of histone methyltransferase EHMT and reduce the H3K9 dimethylation (H3K9me2) levels in cells. |
PSA | 62.75000 |
Target | IC50: <15 nM (G9a), 19±1 nM (GLP) |
Vapor Pressure | 0.0±1.5 mmHg at 25°C |
XLogP3-AA | 6.3 |