UNC0638

Catalog No.S8071

UNC0638 Chemical Structure

Molecular Weight(MW): 509.73

UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets.

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Purity & Quality Control

Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets.
Targets
G9a [1]
(Cell-free assay)
GLP [1]
(Cell-free assay)
<15 nM 19 nM
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
22Rv1 cells MXzGeY5kfGmxbjDhd5NigQ>? MY\Jcohq[mm2aX;uJI9nKEd7YTDpckBpfW2jbjCyNnJ3OSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gTFNMQW2nMjDh[pRmeiB2ODDodpMh[nliSX6tR4VtdCCZZYP0[ZJvKGG|c3H5MEBKSzVyPUCuNFQ5KM7:TR?= M3r5U|IyPzhyN{mw
PC3 cells NHHrS3FHfW6ldHnvckBie3OjeR?= MXXJcohq[mm2aX;uJI9nKEd7YTDpckBpfW2jbjDQR|Mh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFizT|lu\TJiYX\0[ZIhPDhiaILzJIJ6KEmwLVPlcIwhX2W|dHXyckBie3OjeTygTWM2OD1yLkC1PUDPxE1? NWPOO2k{OjF5OEC3PVA>
MCF7 cells MkWwSpVv[3Srb36gZZN{[Xl? NUnhVGl3UW6qaXLpeIlwdiCxZjDHPYEhcW5iaIXtZY4hVUOINzDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhUDONOX3lNkBi\nSncjC0PEBpenNiYomgTY4uS2WubDDX[ZN1\XKwIHHzd4F6NCCLQ{WwQVAvODdizszN NY\SXGxVOjF5OEC3PVA>
MDA-MB-231 cells M4nPPGZ2dmO2aX;uJIF{e2G7 M3W0c|Q5KGh? NYXmdYwxUW6qaXLpeIlwdiCxZjDHPYEhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjC0PEBpenNiYomgZ4xwdm:pZX7pZ{Bie3OjeTygTWM2OD1yLkC4NUDPxE1? NEDLWJUzOjl5NUW5Ny=>
IMR90 cells NHTC[ZpHfW6ldHnvckBie3OjeR?= M3\Kc2lvcGmkaYTpc44hd2ZiR{nhJIlvKGi3bXHuJGlOWjlyIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBJO0t7bXWyJIFnfGW{IES4JIhzeyCkeTDJck1E\WyuIGfld5Rmem5iYYPzZZktKEmFNUC9NE4yOiEQvF2= NH\2clYzOTd6MEe5NC=>
HCT116 cells MmroSpVv[3Srb36gZZN{[Xl? M2S4SmlvcGmkaYTpc44hd2ZiR{nhJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhUDONOX3lNkBi\nSncjC0PEBpenNiYomgTY4uS2WubDDX[ZN1\XKwIHHzd4F6NCCLQ{WwQVAvOjFizszN MWWyNVc5ODd7MB?=
H1299 cells M1r2dWZ2dmO2aX;uJIF{e2G7 M{fZ[VAvOjVidV2= NXnJN3NVOjRiaB?= MnfRTY5pcWKrdHnvckBw\iCJOXGg[ZhxemW|c3XkJIlvKEhzMkm5JINmdGy|IHHzd4V{e2WmIHHzJIlvcGmkaYTpc44hd2ZiZHnt[ZRpgWyjdHnvckBw\iCyNUOgZZQhdHm|IEO3N{BifCByLkK1JJVOKGGodHXyJFI1KGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? MYSyNVc5ODd7MB?=

... Click to View More Cell Line Experimental Data

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[1].

Protocol

Kinase Assay:

[1]

+ Expand

SAHH-coupled assays:

This assay utilizes SAHH to hydrolyze the methyltransfer product S-adenosylhomocysteine to homocysteine and adenosine in the presence of adenosine deaminase which converts adenosine to inosine. The homocysteine concentration is then determined through conjugation of its free sulfhydryl moiety to a thiol-sensitive fluorophore, ThioGlo. For IC50 determinations, assay mixtures are prepared in 25 mM Potassium Phosphate buffer pH 7.5, 1 mM EDTA, 2 mM MgCl2, 0.01% Triton X 100 with 5 μM SAHH , 0.3 U/mL of adenosine deaminase, 25 μM SAM, and 15 μM ThioGlo. G9a, EHMT1, SETD7, SETD8, PRMT3 and SUV39H2 are assayed at 25 nM, 100 nM, 200 nM, 250 nM, 1 μM and 100 nM, respectively. UNC0638 is added at concentrations ranging from 4 nM to 16 μM. After 2 min incubation, reactions are initiated by addition of the histone peptides: 10 μM H3(1-25) for G9a, 20 μM H3(1-25) for EHMT1, 100 μM H3(1-25) for SETD7, 500 μM H4(1-24) for SETD8, 10 μM H4(1-24) for PRMT3 and 200 μM H3K9Me1 (1-15) for SUV39H2. The methylation reaction is followed by monitoring the increase in fluorescence using Biotek Synergy2 plate reader with 360/40 nm excitation filter and 528/20 nm emission filter for 20 min in 384 well-plate format. Activity values are corrected by subtracting background caused by the peptide or the protein. IC50 values are calculated using Sigmaplot. Standard deviations are calculated from two independent experiments.
Cell Research:

[1]

+ Expand
  • Cell lines: MCF7, U2OS, H1299 cell lines
  • Concentrations: 3 μM
  • Incubation Time: 65 h
  • Method:

    Approximately 5×105 cells were plated onto 75 cm2 flasks. MCF7 and U2OS cells were grown in Minimal Essential Media (MEM) without phenol red supplemented with Earl's salts, 10% FBS, 1 mM Pyruvate, 2 mM Glutamine, and 1×non-essential amino acids. H1299 cells were grown in Dulbecco's Modified Eagle's Medium (DMEM) with phenol red supplemented with 10% FBS and 1×Anti-Anti. At the time of cell plating, media was supplemented with 3 μM UNC638A or the equivalent DMSO vehicle. The media with 3 μM UNC638A but without any cells was also used as a control. All flasks were incubated at 37℃/5% CO2. After 65 hours, media was collected from the cells and centrifuged to remove any cell debris. The media (10 to 15 mL) from each of study groups was mixed with HPLC grade chloroform (7 to 12 mL). After the mixture was gently shaken, it was allowed to sit until the organic layer and the aqueous layer separated. The organic layer was collected, dried over anhydrous Na2SO4, and concentrated in vacuo. The resulting residue was dissolved in 100 μL of methanol and the solution was analyzed using an Agilent 6110 LC/MS Series system with UV detector set to at 254 nm. Samples were injected (10 μL) onto a Phenomenex Kinetex 2.1 x 100 nm, 2.6 μM, C18 column at room temperature and eluted with 72% B (MeCN) with A being H2O + 0.1% formic acid. The flow rate was 0.3 mL/min. No degradation products of UNC0638 were observed for any of treatment groups.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Swiss albino mice
  • Formulation: --
  • Dosages: IV, 1 mg/kg; PO, 3 mg/kg; IP, 2.5 mg/kg
  • Administration: i.v./i.p./oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (196.18 mM)
Ethanol 100 mg/mL (196.18 mM)
Water 6 mg/mL (11.77 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 509.73
Formula

C30H47N5O2

CAS No. 1255580-76-7
Storage powder
in solvent
Synonyms

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID