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 M1:5cGZ2dmO2aX;uJIF{e2G7 MmTxTY5pcWKrdHnvckBw\iCJOXGgbY4hcHWvYX6gNlJTfjFiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJGg{UzmvZUKgZYZ1\XJiNEigbJJ{KGK7IFnuMWNmdGxiV3XzeIVzdiCjc4PhfUwhUUN3ME2wMlA1QCEQvF2= NGXDRmozOTd6MEe5NC=>
PC3 cells MX\GeY5kfGmxbjDhd5NigQ>? MXXJcohq[mm2aX;uJI9nKEd7YTDpckBpfW2jbjDQR|Mh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFizT|lu\TJiYX\0[ZIhPDhiaILzJIJ6KEmwLVPlcIwhX2W|dHXyckBie3OjeTygTWM2OD1yLkC1PUDPxE1? NGLYPGkzOTd6MEe5NC=>
MCF7 cells NF7qbFNHfW6ldHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKEd7YTDpckBpfW2jbjDNR2Y4KGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDIN2s6dWV{IHHmeIVzKDR6IHjyd{BjgSCLbj3D[YxtKFenc4Tldo4h[XO|YYmsJGlEPTB;MD6wO{DPxE1? NEiwTmUzOTd6MEe5NC=>
MDA-MB-231 cells Mn3USpVv[3Srb36gZZN{[Xl? MkXBOFghcA>? NWPVdZJFUW6qaXLpeIlwdiCxZjDHPYEhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bi\nSncjC0PEBpenNiYomgZ4xwdm:pZX7pZ{Bie3OjeTygTWM2OD1yLkC4NUDPxE1? M3Kyc|IzQTd3NUmz
IMR90 cells Mlm0SpVv[3Srb36gZZN{[Xl? M4HjfGlvcGmkaYTpc44hd2ZiR{nhJIlvKGi3bXHuJGlOWjlyIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBJO0t7bXWyJIFnfGW{IES4JIhzeyCkeTDJck1E\WyuIGfld5Rmem5iYYPzZZktKEmFNUC9NE4yOiEQvF2= M4j0elIyPzhyN{mw
HCT116 cells MVrGeY5kfGmxbjDhd5NigQ>? MnzMTY5pcWKrdHnvckBw\iCJOXGgbY4hcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBJO0t7bXWyJIFnfGW{IES4JIhzeyCkeTDJck1E\WyuIGfld5Rmem5iYYPzZZktKEmFNUC9NE4zOSEQvF2= M1qyNlIyPzhyN{mw
H1299 cells MX\GeY5kfGmxbjDhd5NigQ>? M2XkbFAvOjVidV2= MknQNlQhcA>? MWTJcohq[mm2aX;uJI9nKEd7YTDlfJBz\XO|ZXSgbY4hUDF{OUmgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCmaX3leIh6dGG2aX;uJI9nKHB3MzDheEBtgXNiM{ezJIF1KDBwMkWgeW0h[W[2ZYKgNlQhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? M4DqR|IyPzhyN{mw

... Click to View More Cell Line Experimental Data

Protocol

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
Synonyms

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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Molecular Weight Calculator

Molecular Weight Calculator

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Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Tech Support

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID