Catalog No.S7230

For research use only.

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.

UNC0642 Chemical Structure

CAS No. 1481677-78-4

Selleck's UNC0642 has been cited by 7 Publications

Purity & Quality Control

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 NXPpTGNNTnWwY4Tpc44h[XO|YYm= M3m2UGlvcGmkaYTpc44hd2ZibInzbY5mKG2ndHj5cJRz[W6|ZnXyZZNmKEd7YTDpckBpfW2jbjDQRW5EOSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gTFNMQW2nMjDj[YxtfWyjcjDs[ZZmdCCkeTDpcY12dm:obIXvdoV{[2WwY3WgbY4u[2WubDDX[ZN1\XKwIHHzd4F6NCCLQ{WwJF0hOC5yNDFOwG0v M1voVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUCyNVM1Lz5{NEGwNlE{PDxxYU6=
MDA-MB-231 MXjGeY5kfGmxbjDhd5NigQ>? NV7ZVmxCUW6qaXLpeIlwdiCxZjDsfZNqdmVibXX0bJltfHKjboPm[ZJie2ViR{nhJIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFizT|lu\TJiY3XscJVt[XJibHX2[Ywh[nliaX3teY5w\my3b4Lld4NmdmOnIHnuMYNmdGxiV3XzeIVzdiCjc4PhfUwhUUN3MDC9JFAvOTFizszNMi=> MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFyMkGzOEc,OjRzMEKxN|Q9N2F-
PC3 NITnbYJHfW6ldHnvckBie3OjeR?= NYrRPJdtUW6qaXLpeIlwdiCxZjDsfZNqdmVibXX0bJltfHKjboPm[ZJie2ViR{nhJIlvKGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25ib3[gTFNMQW2nMjDj[YxtfWyjcjDs[ZZmdCCkeTDpcY12dm:obIXvdoV{[2WwY3WgbY4u[2WubDDX[ZN1\XKwIHHzd4F6NCCLQ{WwJF0hOC5zMzFOwG0v MnznQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMEKxN|QoRjJ2MUCyNVM1RC:jPh?=
U2OS MX;GeY5kfGmxbjDhd5NigQ>? MoDCTY5pcWKrdHnvckBw\iCueYPpcoUhdWW2aInseJJidnOoZYLhd4UhTzmjIHnuJIh2dWGwIGWyU3Mh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIFizT|lu\TJiY3XscJVt[XJibHX2[Ywh[nliaX3teY5w\my3b4Lld4NmdmOnIHnuMYNmdGxiV3XzeIVzdiCjc4PhfUwhUUN3MDC9JFAvOTNizszNMi=> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFyMkGzOEc,OjRzMEKxN|Q9N2F-
PANC1 NH6weplEgXSxdH;4bYNqfHliYYPzZZk> M17CTFQ5KGi{cx?= MUHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDQRW5EOSClZXzsd{Bi\nSncjC0PEBpenNiYomgRYxidWG{IFLseYUh[XO|YYmsJGVEPTBiPTCzMlUh|ryPLh?= NXPOTJZYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNFIyOzRpPkK0NVAzOTN2PD;hQi=>
U2OS NHXEUIVEgXSxdH;4bYNqfHliYYPzZZk> MUi0PEBpenN? M2XqWGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHUzV1NiY3XscJMh[W[2ZYKgOFghcHK|IHL5JGFt[W2jcjDCcJVmKGG|c3H5MEBGSzVyIE2gOkDPxE1w MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDFyMkGzOEc,OjRzMEKxN|Q9N2F-
PC3 M3;WO2N6fG:2b4jpZ4l1gSCjc4PhfS=> M4jSXVQ5KGi{cx?= NUHCWZRXS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWEN|IHPlcIx{KGGodHXyJFQ5KGi{czDifUBCdGGvYYKgRox2\SCjc4PhfUwhTUN3MDC9JFgvQSEQvF2u MkLzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjRzMEKxN|QoRjJ2MUCyNVM1RC:jPh?=
MDA-MB-231 MmKxR5l1d3SxeHnjbZR6KGG|c3H5 NIDRc4o1QCCqcoO= MkDTR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDh[pRmeiB2ODDodpMh[nliQXzhcYFzKEKudXWgZZN{[XluIFXDOVAhRSBzNj63JO69VS5? NY\CSndiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNFIyOzRpPkK0NVAzOTN2PD;hQi=>
Methods Test Index PMID
Growth inhibition assay Cell viability 28630300
Western blot G9A / di-mH3K9 / ERBB3 31619200
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].

Protocol (from reference)

Cell Research:


  • 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.

Animal Research:


  • Animal Models: male Swiss Albino mice
  • Dosages: 5 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 546.7


CAS No. 1481677-78-4
Storage 3 years -20°C powder
2 years -80°C in solvent

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