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[CAS NO. 1255580-76-7] UNC0638
| Ships within | Stock | Price | Qty | Total |
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| Catalog: | HY-15273 |
| Brand: | MCE |
| CAS: | 1255580-76-7 |
Overview
| MDL | MFCD22208587 |
|---|---|
| Molecular Weight | 509.73 |
| Molecular Formula | C30H47N5O2 |
| SMILES | CC(N1CCC(NC2=C3C=C(OC)C(OCCCN4CCCC4)=CC3=NC(C5CCCCC5)=N2)CC1)C |
6 Publications Citing Use of MCE
Summary
UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC 50 s of less than 15 nM and 19 nM, respectively. UNC0638 has anti- FMDV (foot-and-mouth disease virus) and anti- VSV (vesicular stomatitis virus) activities.
IC50 & Target
IC50: <15 nM (G9a), 19±1 nM (GLP) [1]
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 K i of UNC0638 is determined to be 3.0±0.05 nM (n=2). Consistent with this, the Morrison K i 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 (IC 50 =4,500±1,100 nM), a Jumonji protein demethylase and DNA methyltransferase DNMT1 (IC 50 =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 [1] . 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 [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
1M HCl : 100 mg/mL ( 196.18 mM ; ultrasonic and adjust pH to 1 with HCl)
DMSO : ≥ 30 mg/mL ( 58.85 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9618 mL | 9.8091 mL | 19.6182 mL |
| 5 mM | 0.3924 mL | 1.9618 mL | 3.9236 mL |
| 10 mM | 0.1962 mL | 0.9809 mL | 1.9618 mL |
References
- [1] Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74.
- [2] Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5.
- [3] Singh N, et al. Inhibition of EHMT2 Induces a Robust Antiviral Response Against Foot-and-Mouth Disease and Vesicular Stomatitis Virus Infections in Bovine Cells. J Interferon Cytokine Res. 2016 Jan;36(1):37-47.
Synonyms
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