Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
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
50 mM
0.0392 mL
0.1962 mL
0.3924 mL
Description
UNC0638 is a potent, selective and cell-penetrant chemical probe for and histone methyltransferase with of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets. UNC0638 has anti-viral activities.
UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP, with a toxicity/function ratio of >100, compared to <6 for BIX01294. UNC0638 is a selectivite inhibitor of G9a and GLP over a wide range of epigenetic and non-epigenetic targets. UNC0638 is more than 10,000-fold selective against SET7/9 (a H3K4 HMTase), SET8 (a H4K20 HMTase), PRMT3, and SUV39H2. In MDA-MB-231 cells, UNC0638 (48 h exposure) reduces H3K9me2 levels in a concentration-dependent manner with an IC50 of 81 nM. UNC0638 treatment of a variety of cell lines results 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 reduces the clonogenicity of MCF7 cells, reduces the abundance of H3K9me2 marks at promoters of known G9a-regulated endogenous genes and disproportionately affected several genomic loci encoding microRNAs. In mouse embryonic stem cells, UNC0638 reactivates G9a-silenced genes and a retroviral reporter gene in a concentration-dependent manner without promoting differentiation.
In vivo
In mouse drug metabolism and pharmacokinetic studies, UNC0638 had high clearance, short half-life, high volume distribution and low exposure after intravenous, oral or intraperitoneal administration. Thus, although UNC0638 is probably not suitable for in vivo animal studies owing to low exposure levels, its high stability under cellular assay conditions, in combination with high potency and selectivity, makes UNC0638 an ideal chemical tool for cell-based studies.
