For research use only.

Catalog No.S7230

1 publication

UNC0642 Chemical Structure

CAS No. 1481677-78-4

UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.

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Selleck's UNC0642 has been cited by 1 publication

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Choose Selective Histone Methyltransferase Inhibitors

Biological Activity

Description UNC0642 is a potent, selective inhibitor of histone methyltransferases G9a/GLP with IC50s less than 2.5 nM for G9a and GLP and shows more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels.
G9a [1]
(Cell-free assay)
GLP [1]
(Cell-free assay)
<2.5 nM <2.5 nM
In vitro

UNC0642 is competitive with the peptide substrate and non-competitive with the cofactor SAM. The Ki of UNC0642 is determined to be 3.7 ± 1 nM. It is more than 20,000-fold selective for G9a and GLP over 13 other methyltransferases (IC50 > 50,000 nM) and more than 2,000-fold selective over PRC2-EZH2 (IC50 > 5,000 nM). UNC0642 displays high potency (IC50 < 150 nM) in reducing cellular levels of H3K9me2, low cell toxicity (EC50 > 3,000 nM), resulting in a good separation of functional potency and cell toxicity with a tox/function ratio (which is determined by dividing the EC50 value of the observed toxicity by the IC50 value of the functional potency) of > 45 in U2OS, PC3, and PANC-1 cells. UNC0642 reduces clonogenicity in PANC-1 cells in a concentration-dependent manner while it has no effect on clonogenicity in MDA-MB-231 cells[1].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
PANC1 NG[3ephHfW6ldHnvckBie3OjeR?= Ml3MTY5pcWKrdHnvckBw\iCueYPpcoUhdWW2aInseJJidnOoZYLhd4UhTzmjIHnuJIh2dWGwIGDBUmMyKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCxZjDIN2s6dWV{IHPlcIx2dGG{IHzleoVtKGK7IHntcZVvd2[udX;y[ZNk\W6lZTDpck1k\WyuIGfld5Rmem5iYYPzZZktKEmFNUCgQUAxNjB2IN88UU4> M2LXdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUCyNVM1Lz5{NEGwNlE{PDxxYU6=
MDA-MB-231 MnuxSpVv[3Srb36gZZN{[Xl? MmHVTY5pcWKrdHnvckBw\iCueYPpcoUhdWW2aInseJJidnOoZYLhd4UhTzmjIHnuJIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKEh|S{nt[VIh[2WubIXsZZIhdGW4ZXygZpkhcW2vdX7v[ox2d3Knc3PlcoNmKGmwLXPlcIwhX2W|dHXyckBie3OjeTygTWM2OCB;IECuNVEh|ryPLh?= M4PWTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUCyNVM1Lz5{NEGwNlE{PDxxYU6=
PC3 NFqwO3VHfW6ldHnvckBie3OjeR?= MmPpTY5pcWKrdHnvckBw\iCueYPpcoUhdWW2aInseJJidnOoZYLhd4UhTzmjIHnuJIh2dWGwIGDDN{Bk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiSEPLPY1mOiClZXzseYxieiCuZY\lcEBjgSCrbX31co9ndHWxcnXzZ4Vv[2ViaX6tZ4VtdCCZZYP0[ZJvKGG|c3H5MEBKSzVyIE2gNE4yOyEQvF2u NYPQdnpDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNFIyOzRpPkK0NVAzOTN2PD;hQi=>
U2OS NVHFZ2VrTnWwY4Tpc44h[XO|YYm= NV;HSFdCUW6qaXLpeIlwdiCxZjDsfZNqdmVibXX0bJltfHKjboPm[ZJie2ViR{nhJIlvKGi3bXHuJHUzV1NiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJGg{UzmvZUKgZ4VtdHWuYYKgcIV3\WxiYomgbY1ufW6xZnz1c5Jme2OnbnPlJIlvNWOnbHygW4V{fGW{bjDhd5NigSxiSVO1NEA:KDBwMUOg{txONg>? NYDtZYFSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNFIyOzRpPkK0NVAzOTN2PD;hQi=>
PANC1 M2\VcmN6fG:2b4jpZ4l1gSCjc4PhfS=> MoLKOFghcHK| NIXEeHZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSU6FMTDj[YxteyCjZoTldkA1QCCqcoOgZpkhSWyjbXHyJGJtfWViYYPzZZktKEWFNUCgQUA{NjVizszNMi=> NFzEbGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGwNlE{PCd-MkSxNFIyOzR:L3G+
U2OS MYXDfZRwfG:6aXPpeJkh[XO|YYm= NFX6N2E1QCCqcoO= MUDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDVNm9UKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDBcIFu[XJiQnz1[UBie3OjeTygSWM2OCB;IE[g{txONg>? M4nENFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUCyNVM1Lz5{NEGwNlE{PDxxYU6=
PC3 MkTQR5l1d3SxeHnjbZR6KGG|c3H5 MmrFOFghcHK| NGjzeXFEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[W[2ZYKgOFghcHK|IHL5JGFt[W2jcjDCcJVmKGG|c3H5MEBGSzVyIE2gPE46KM7:TT6= Mn;LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMEKxN|QoRjJ2MUCyNVM1RC:jPh?=
MDA-MB-231 NGXkTYNEgXSxdH;4bYNqfHliYYPzZZk> MUi0PEBpenN? MUfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNSGEuVUJvMkOxJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCDbHHtZZIhSmy3ZTDhd5NigSxiRVO1NEA:KDF4Lkeg{txONg>? NGDa[HU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGwNlE{PCd-MkSxNFIyOzR:L3G+

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Growth inhibition assay
Cell viability ; 

PubMed: 28630300     

Cell survival was analyzed by performing MTT assay on cells following vehicle or UNC0642 (96 h). Immunoblotting analysis of G9a in nuclear extracts from various breast epithelial cells. 

Western blot
G9A / di-mH3K9 / ERBB3 ; 

PubMed: 31619200     

G9a inhibitors, UNC0642 and BIX01294, significantly blocked G9a-mediated di-mH3K9 activity and reduced ERBB3 expression in EGFR-autophosphorylated lung cancer H1975 cells.

In vivo For evaluation in vivo PK properties in male Swiss Albino mice, a single intraperitoneal (IP) injection (5 mg/kg) of UNC0642 results in a plasma Cmax (maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL. It displays modest brain penetration with a brain/plasma ratio of 0.33[1]. A single intraperitoneal (i.p.) injection dose of 5 mg/kg of UNC0642 is sufficient to inhibit G9a activity in adult mice. UNC0642 improves the life span and weight gain of m+/pΔS−U pups, produces long-lasting activation of PWS-associated genes, is apparently well tolerated and produces no notable acute toxicity, and does not interfere with the expression of the AS-associated Ube3a gene[2].


Cell Research:


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  • Cell lines: MDA-MB-231, PC3, and U2OS cells
  • Concentrations: --
  • Incubation Time: 48 h
  • Method:

    MDA-MB-231, PC3, and U2OS cells are cultured in RPMI with 10% FBS, PANC-1 cells in DMEM with 10% FBS. Cells are treated with inhibitors for 48 h. Cell viability assays are performed by incubating cells with 0.1 mg/mL of resazurin for 3-4 h. Resazurin reduction is monitored with 544 nm excitation, measuring fluorescence at 590 nm.

    (Only for Reference)
Animal Research:


- Collapse
  • Animal Models: male Swiss Albino mice
  • Dosages: 5 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (182.91 mM)
Ethanol 100 mg/mL (182.91 mM)
Water Insoluble

* 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 546.7


CAS No. 1481677-78-4
Storage powder
in solvent
Synonyms N/A

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Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID