2. Epigenetics Apoptosis
  3. Histone Methyltransferase Apoptosis
  4. DCG066

DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562.

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DCG066 Chemical Structure

DCG066 Chemical Structure

CAS No. : 494786-13-9

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DCG066 Related Antibodies

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View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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Description

DCG066 is an inhibitor of lysine methyltransferase G9a. DCG066 can bind directly to G9a and inhibit methyltransferase activity in vitro. DCG066 decreases di-methylation levels of histone H3 lysine 9 (H3K9Me2), inhibits cell proliferation and induces cell apoptosis. DCG066 displays low cytotoxicity in leukemia cell lines with high levels of G9a expression, including K562[1].

IC50 & Target

G9a

 

Cellular Effect
Cell Line Type Value Description References
A549 IC50
6.6 μM
Compound: DCG066
Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human A549 cells after 48 hrs by CCK8 assay
[PMID: 27393948]
HepG2 IC50
3.2 μM
Compound: DCG066
Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human HepG2 cells after 48 hrs by CCK8 assay
[PMID: 27393948]
HL-60 IC50
4.4 μM
Compound: DCG066
Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human HL60 cells after 48 hrs by CCK8 assay
[PMID: 27393948]
K562 IC50
1.7 μM
Compound: DCG066
Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
Antiproliferative activity against human K562 cells after 48 hrs by CCK8 assay
[PMID: 27393948]
Molecular Weight

579.58

Formula

C30H31F6N3O2
CAS No.
SMILES

O=C(N(C)C)NC1=CC=C(C=C1)CN2CCC(CC2)C(O)(C3=CC=C(C=C3)C(F)(F)F)C4=CC=C(C=C4)C(F)(F)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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DCG066 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DCG066494786-13-9DCG 066DCG-066Histone MethyltransferaseApoptosisInhibitorinhibitorinhibit

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