Art. -Nr.: HY-15273

UNC0638

12 Cited Publications

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UNC0638, a chemical probe, selectively inhibits G9a and GLP histone methyltransferases with IC₅₀ of 15 nM and 19 nM, respectively. UNC0638 inhibits TNBC cell invasion and migration in vitro. UNC0638 is also an inhibitor of EHMT1/2 and induces fetal hemoglobin (HbF) expression in human erythroid progenitor cell culture. In addition, UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities, with excellent potency and selectivity against multiple epigenetic and non-epigenetic targets.

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Reinheit: 99.84%
CAS. Nr.: 1255580-76-7
Formel: C₃₀H₄₇N₅O₂
Molecular Weight:509.73

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

UNC0638 Chemical Structure

CAS. Nr.: 1255580-76-7

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (12)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
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Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

EHMT2/G9a/KMT1C

EHMT1/GLP/KMT1D

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Calu-1	EC₅₀	1.3 μM Compound: Chemical probe: UNC0638	Antiproliferative against human Calu-1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human Calu-1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Calu-6	EC₅₀	1.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human Calu-6 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human Calu-6 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
CWR22R	EC₅₀	4.5 μM Compound: 5, UNC0638	Cytotoxicity against human 22Rv1 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human 22Rv1 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
CWR22R	IC₅₀	0.048 μM Compound: 5, UNC0638	Inhibition of G9a in human 22Rv1 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human 22Rv1 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
CWR22R	EC₅₀	0.2 μM Compound: Chemical probe: UNC0638	Antiproliferative against human 22RV1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human 22RV1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Daoy	EC₅₀	0.1 μM Compound: Chemical probe: UNC0638	Antiproliferative against human Daoy cells after 7 days by Cell-Titer Glo assay Antiproliferative against human Daoy cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
DU-145	EC₅₀	0.7 μM Compound: Chemical probe: UNC0638	Antiproliferative against human DU-145 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human DU-145 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
G-401	EC₅₀	0.4 μM Compound: Chemical probe: UNC0638	Antiproliferative against human G-401 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human G-401 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
HCT-116	EC₅₀	11 μM Compound: 5, UNC0638	Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
HCT-116	EC₅₀	11 μM Compound: 5, UNC0638	Cytotoxicity against p53-deficient human HCT116 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against p53-deficient human HCT116 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
HCT-116	IC₅₀	0.21 μM Compound: 5, UNC0638	Inhibition of G9a in human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
HCT-116	IC₅₀	0.24 μM Compound: 5, UNC0638	Inhibition of G9a in p53-deficient human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in p53-deficient human HCT116 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
HCT-116	IC₅₀	3.35 μM Compound: UNC0638	Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells assessed as inhibition of cell viability after 72 hrs by MTT assay	[PMID: 27720557]
HepG2	IC₅₀	3.7 μM Compound: UNC0638	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell viability after 72 hrs by MTT assay	[PMID: 27720557]
HFF	IC₅₀	2286 nM Compound: 19; UNC0638	Cytotoxicity against HFF Cytotoxicity against HFF	[PMID: 30366254]
HL-60	IC₅₀	23.75 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay	[PMID: 25978433]
HL-60	IC₅₀	27.38 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human HL-60 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay	[PMID: 25978433]
HL-60	EC₅₀	6.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human HL-60 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human HL-60 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
HT-1080	EC₅₀	0.5 nM Compound: Chemical probe: UNC0638	Antiproliferative activity against human HT-1080 cells after 5 days by Cell-Titer-Glo assay Antiproliferative activity against human HT-1080 cells after 5 days by Cell-Titer-Glo assay	[PMID: 26147105]
HT-1080	EC₅₀	0.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human HT-1080 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human HT-1080 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
HT-1080	EC₅₀	1.2 nM Compound: Chemical probe: UNC0638	Antiproliferative activity against human HT-1080 cells after 2 days by Cell-Titer-Glo assay Antiproliferative activity against human HT-1080 cells after 2 days by Cell-Titer-Glo assay	[PMID: 26147105]
IMR-32	EC₅₀	>10 μM Compound: Chemical probe: UNC0638	Antiproliferative against human IMR-32 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human IMR-32 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
IMR-90	EC₅₀	2.3 μM Compound: 5, UNC0638	Cytotoxicity against human IMR90 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human IMR90 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
IMR-90	IC₅₀	0.12 μM Compound: 5, UNC0638	Inhibition of G9a in human IMR90 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human IMR90 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
K562	EC₅₀	5.3 μM Compound: Chemical probe: UNC0638	Antiproliferative against human K562 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human K562 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Kasumi 1	EC₅₀	1.1 μM Compound: Chemical probe: UNC0638	Antiproliferative against human Kasumi-1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human Kasumi-1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
KG-1a	IC₅₀	22.36 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 48 hrs by MTT assay	[PMID: 25978433]
KG-1a	IC₅₀	26.53 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human KG-1a cells assessed as decrease in cell viability measured after 24 hrs by MTT assay	[PMID: 25978433]
KMS-11	EC₅₀	4 μM Compound: Chemical probe: UNC0638	Antiproliferative against human KMS-11 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human KMS-11 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
KMS-12-BM	EC₅₀	4.4 μM Compound: Chemical probe: UNC0638	Antiproliferative against human KMS-12-BM cells after 5 days by Cell-Titer Glo assay Antiproliferative against human KMS-12-BM cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
L-363	EC₅₀	3.9 μM Compound: Chemical probe: UNC0638	Antiproliferative against human L-363 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human L-363 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
LN-229	EC₅₀	0.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human LN-229 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human LN-229 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
LNCaP	EC₅₀	0.3 μM Compound: Chemical probe: UNC0638	Antiproliferative against human LNCaP cells after 5 days by Cell-Titer Glo assay Antiproliferative against human LNCaP cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
MCF7	IC₅₀	0.07 μM Compound: 5, UNC0638	Inhibition of G9a in human MCF7 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human MCF7 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
MCF7	IC₅₀	81 nM Compound: 11, UNC0638	Inhibition of G9a in human MCF7 cells after 48 hrs by clonogenic assay Inhibition of G9a in human MCF7 cells after 48 hrs by clonogenic assay	[PMID: 22975593]
MCF7	IC₅₀	6.99 μM Compound: UNC0638	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability after 72 hrs by MTT assay	[PMID: 27720557]
MDA-MB-231	EC₅₀	11 μM Compound: 5, UNC0638	Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
MDA-MB-231	IC₅₀	0.081 μM Compound: 5, UNC0638	Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
MDA-MB-231	IC₅₀	81 nM Compound: 11, UNC0638	Inhibition of G9a in human MDA-MB-231 cells after 48 hrs by clonogenic assay Inhibition of G9a in human MDA-MB-231 cells after 48 hrs by clonogenic assay	[PMID: 22975593]
MDA-MB-231	IC₅₀	81 nM Compound: 5, UNC0638	Inhibition of lysine methyltransferase G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay Inhibition of lysine methyltransferase G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay	[PMID: 24102134]
MDA-MB-231	EC₅₀	11 μM Compound: 5, UNC0638	Cytotoxicity against human MDA-MB-231 cells after 48 hrs by Alamar Blue assay Cytotoxicity against human MDA-MB-231 cells after 48 hrs by Alamar Blue assay	[PMID: 24102134]
MDA-MB-231	IC₅₀	3.56 μM Compound: 47; UNC0638	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth measured after 72 hrs by MTT assay	[PMID: 35525212]
MDA-MB-231	IC₅₀	81 nM Compound: 38; UNC0638	Reduction in H3K9me2 level in human MDA-MB-231 cells incubated for 48 hrs by ChIP assay Reduction in H3K9me2 level in human MDA-MB-231 cells incubated for 48 hrs by ChIP assay	[PMID: 36528996]
MDA-MB-231	EC₅₀	11000 nM Compound: 4	Antiproliferative activity against human MDA-MB-231 cells by MTT assay Antiproliferative activity against human MDA-MB-231 cells by MTT assay	[PMID: 38799223]
MDA-MB-231	IC₅₀	81 nM Compound: 4	Downregulation of H3K9me2 level in human MDA-MB-231 cells measured after 48 hrs by Western blot analysis Downregulation of H3K9me2 level in human MDA-MB-231 cells measured after 48 hrs by Western blot analysis	[PMID: 38799223]
MDA-MB-231	EC₅₀	11 μM Compound: 126, UNC0638	Cytotoxicity against human MDA-MB-231 cells by MTT assay Cytotoxicity against human MDA-MB-231 cells by MTT assay	10.1039/C1MD00199J
MDA-MB-231	IC₅₀	81 nM Compound: 126, UNC0638	Inhibition of G9a/GLP in human MDA-MB-231 cells assessed as reduction of H3K9me2 level after 48 hrs by flow cytometric analysis Inhibition of G9a/GLP in human MDA-MB-231 cells assessed as reduction of H3K9me2 level after 48 hrs by flow cytometric analysis	10.1039/C1MD00199J
MOLT-16	EC₅₀	0.2 μM Compound: Chemical probe: UNC0638	Antiproliferative against human MOLT-16 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human MOLT-16 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
MOLT-4	GI₅₀	188 nM Compound: 5; UNC0638	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 and measured after 12 days by ATPlite assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 and measured after 12 days by ATPlite assay	[PMID: 36882960]
MOLT-4	GI₅₀	188 nM Compound: 5; UNC0638	Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 by ATPlite assay Antiproliferative activity against human MOLT-4 cells assessed as inhibition of cell growth with replenishment of medium with compound on day 4 and 7 by ATPlite assay	[PMID: 36882960]
MV4-11	EC₅₀	1.7 μM Compound: Chemical probe: UNC0638	Antiproliferative against human MV4-11 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human MV4-11 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H1975	EC₅₀	>10 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H1975 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H1975 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H2009	EC₅₀	3.9 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H2009 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H2009 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H358	EC₅₀	4.3 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H358 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H358 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H441	EC₅₀	8.7 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H441 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H441 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H522	EC₅₀	1.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H522 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H522 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H661	EC₅₀	4.9 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H661 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H661 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
NCI-H929	EC₅₀	4.6 μM Compound: Chemical probe: UNC0638	Antiproliferative against human NCI-H929 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human NCI-H929 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
OPM-2	EC₅₀	5.6 μM Compound: Chemical probe: UNC0638	Antiproliferative against human OPM-2 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human OPM-2 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
PA-1	EC₅₀	0.2 μM Compound: Chemical probe: UNC0638	Antiproliferative against human PA-1 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human PA-1 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
PC-3	EC₅₀	14 μM Compound: 5, UNC0638	Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 21780790]
PC-3	IC₅₀	0.059 μM Compound: 5, UNC0638	Inhibition of G9a in human PC3 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay Inhibition of G9a in human PC3 cells assessed as reduction of H3K9me2 after 48 hrs by In-Cell Western assay	[PMID: 21780790]
RD	IC₅₀	11.17 μM Compound: 47; UNC0638	Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 24 hrs Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 24 hrs	[PMID: 35525212]
RD	IC₅₀	2.91 μM Compound: 47; UNC0638	Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 144 hrs Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 144 hrs	[PMID: 35525212]
RD	IC₅₀	3.05 μM Compound: 47; UNC0638	Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against human RD cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 35525212]
RD	CC₅₀	34.2 μM Compound: UNC-0638	Cytotoxicity against human RD cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human RD cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37021456]
RPMI-8226	EC₅₀	5.1 μM Compound: Chemical probe: UNC0638	Antiproliferative against human RPMI-8226 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human RPMI-8226 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
RS4-11	EC₅₀	3.1 μM Compound: Chemical probe: UNC0638	Antiproliferative against human RS4-11 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human RS4-11 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
Sf9	IC₅₀	13 nM Compound: UNC0638	Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 m Inhibition of N-terminal GST tagged human recombinant EHMT1 (794 to 1294 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 m	[PMID: 31350126]
Sf9	IC₅₀	26 nM Compound: UNC0638	Inhibition of N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 m Inhibition of N-terminal GST tagged human recombinant EHMT2 (785 to 1210 residues) expressed in baculovirus infected Sf9 insect cells assessed as reduction in conversion of SAH to AMP using histone H3 as substrate and SAH as cosubstrate incubated for 30 m	[PMID: 31350126]
SJRH30	IC₅₀	2.48 μM Compound: 47; UNC0638	Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 144 hrs Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 144 hrs	[PMID: 35525212]
SJRH30	IC₅₀	2.64 μM Compound: 47; UNC0638	Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 72 hrs Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 72 hrs	[PMID: 35525212]
SJRH30	IC₅₀	5.01 μM Compound: 47; UNC0638	Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 24 hrs Antiproliferative activity against human Rh30 cells assessed as inhibition of cell growth incubated for 24 hrs	[PMID: 35525212]
SK-BR-3	EC₅₀	0.6 μM Compound: Chemical probe: UNC0638	Antiproliferative against human SK-BR-3 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human SK-BR-3 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
SK-N-MC	EC₅₀	0.2 μM Compound: Chemical probe: UNC0638	Antiproliferative against human SK-N-MC cells after 7 days by Cell-Titer Glo assay Antiproliferative against human SK-N-MC cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
SW982	CC₅₀	29.46 μM Compound: UNC-0638	Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 37021456]
THP-1	EC₅₀	4.9 μM Compound: Chemical probe: UNC0638	Antiproliferative against human THP-1 cells after 5 days by Cell-Titer Glo assay Antiproliferative against human THP-1 cells after 5 days by Cell-Titer Glo assay	[PMID: 26147105]
THP-1	IC₅₀	0.24 μM Compound: 47; UNC0638	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 144 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 144 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 35525212]
THP-1	IC₅₀	0.34 μM Compound: 47; UNC0638	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 35525212]
THP-1	IC₅₀	0.84 μM Compound: 47; UNC0638	Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human THP-1 cells assessed as inhibition of cell growth incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay	[PMID: 35525212]
U2OS	EC₅₀	0.5 μM Compound: Chemical probe: UNC0638	Antiproliferative against human U2OS cells after 7 days by Cell-Titer Glo assay Antiproliferative against human U2OS cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]
U-937	IC₅₀	19.72 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 48 hrs by MTT assay	[PMID: 25978433]
U-937	IC₅₀	21.4 μM Compound: Chemical Probe: UNC0638	Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay Cytotoxicity against human U-937 cells assessed as decrease in cell viability measured after 24 hrs by MTT assay	[PMID: 25978433]
ZR-75-30	EC₅₀	1.2 μM Compound: Chemical probe: UNC0638	Antiproliferative against human ZR-75-30 cells after 7 days by Cell-Titer Glo assay Antiproliferative against human ZR-75-30 cells after 7 days by Cell-Titer Glo assay	[PMID: 26147105]

In Vitro

UNC0638, an inhibitor of G9a and GLP with excellent potency and selectivity over a wide range of epigenetic and non-epigenetic targets.The K_i of UNC0638 is determined to be 3.0±0.05 nM (n=2). Consistent with this, the Morrison K_i for UNC0638 is 3.7±0.2 nM (n=3). The selectivity of UNC0638 over a wide range of epigenetic targets is evaluated. Notably, UNC0638 is inactive against other H3K9 (SUV39H1 and SUV39H2), H3K27 (EZH2), H3K4 (SETD7, MLL and SMYD3), H3K79 (DOT1L) and H4K20 (SETD8) methyltransferases, as well as PRDM1, PRDM10 and PRDM12. In addition, UNC0638 is inactive against protein arginine methyltransferases PRMT1 and PRMT3, and HTATIP, a histone acetyltransferase. Of note, UNC0638 has weak but measurable activity against JMJD2E (IC₅₀=4,500±1,100 nM), a Jumonji protein demethylase and DNA methyltransferase DNMT1 (IC₅₀=107,000±6,000 nM). Nevertheless, the selectivity of UNC0638 for G9a and GLP over JMJD2E is >200-fold, and selectivity for G9a and GLP over DNMT1 is >5,000-fold^[1]. UNC0638 is a type of small molecule that can specifically inhibit the enzyme activity of histone methyltransferase EHMT and reduce the H3K9 dimethylation (H3K9me2) levels in cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1255580-76-7
Appearance Solid
Molecular Weight 509.73
Formel C₃₀H₄₇N₅O₂
Color White to yellow
SMILES

CC(N1CCC(NC2=C3C=C(OC)C(OCCCN4CCCC4)=CC3=NC(C5CCCCC5)=N2)CC1)C
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (12)

All WBCell Proliferation/Viability AssayCell Migration/Invasion AssayRT-PCR

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Journal Impact Factor

Cancer Res

TNG917 is a Potent and Selective Inhibitor of Histone Lysine Methyltransferases EHMT1/2 that Enhances Anti-Tumor Immunity and Immunotherapy Efficacy. [Abstract]

2026 Jun 10. PMID: 42268285
Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Cell Death Dis

Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signaling pathway. [Abstract]

2018 Jan 26;9(2):129. PMID: 29374157

UNC0638 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]

The effects of treatment with UNC0638 (10 μM) on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

UNC0638 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]

The EHMT2 inhibitor UNC0638 (5-10 μM; 48 h) effectively inhibited cell growth in both PC9/ER and HCC827/ER cells.

UNC0638 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]

UNC0638 (100 nM; 48 h) suppressed cell migration in PC9 and PC9/ER cells.

UNC0638 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]

UNC0638 (100 nM; 48 h) pretreatment enhanced the sensitivity of PC9/ER cells to Erlotinib compared to non-pretreated cells.

UNC0638 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]

Treatment with UNC0638 (10 μM) resulted in the downregulation of Bcl-2 and VEGF in EGFR-TKI-resistant NSCLC cell lines.
Proc Natl Acad Sci U S A

MGMT-activated DUB3 stabilizes MCL1 and drives chemoresistance in ovarian cancer. [Abstract]

2019 Feb 19;116(8):2961-2966. PMID: 30718431
Acta Pharmacol Sin

DNMT inhibition epigenetically restores the cGAS-STING pathway and activates RIG-I/MDA5-MAVS to enhance antitumor immunity. [Abstract]

2025 Aug 19. PMID: 40830678
Acta Pharmacol Sin

P300/CBP inhibition sensitizes mantle cell lymphoma to PI3Kδ inhibitor idelalisib. [Abstract]

2022 Feb;43(2):457-469. PMID: 33850273
Cell Chem Biol

Visualization of the dynamic interaction between nucleosomal histone H3K9 tri-methylation and HP1α chromodomain in living cells. [Abstract]

2022 Jul 21;29(7):1153-1161.e5. PMID: 35728598
Cell Biosci

Activation of goblet cell Piezo1 alleviates mucus barrier damage in mice exposed to WAS by inhibiting H3K9me3 modification. [Abstract]

2023 Jan 12;13(1):7. PMID: 36631841
J Neurosci

Histone Methyltransferase G9a in Primary Sensory Neurons Promotes Inflammatory Pain and Transcription of Trpa1 and Trpv1 via Bivalent Histone Modifications. [Abstract]

2025 Jan 17:e1790242024. PMID: 39824634
Mol Med Rep

UNC0638, a G9a inhibitor, suppresses epithelial‑mesenchymal transition‑mediated cellular migration and invasion in triple negative breast cancer. [Abstract]

2018 Feb;17(2):2239-2244. PMID: 29207160

UNC0638 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2018 Feb;17(2):2239-2244. [Abstract]

UNC0638 (0.5 and 1 µM; 24 h) suppressed triple negative breast cancer cell migration and invasion by regulating EMT-associated proteins. Western blots of EMT-associated proteins were performed.
Mol Carcinog

A novel high-risk model identified by epithelial-mesenchymal transition predicts prognosis and radioresistance in rectal cancer. [Abstract]

2024 Nov;63(11):2119-2132. PMID: 39056517
bioRxiv

2023 Nov 17.

Lösungsmittel & Löslichkeit

In Vitro:

1M HCl : 100 mg/mL (196.18 mM; ultrasonic and adjust pH to 1 with HCl)

DMSO : 33.33 mg/mL (65.39 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9618 mL

9.8091 mL

19.6182 mL

5 mM

0.3924 mL

1.9618 mL

3.9236 mL

10 mM

0.1962 mL

0.9809 mL

1.9618 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Vedadi M, et al. A chemical probe selectively inhibits G9a and GLP methyltransferase activity in cells. Nat Chem Biol. 2011 Jul 10;7(8):566-74. [Content Brief]

[2]. Fu L, et al. Effects of the Histone Methyltransferase Inhibitor UNC0638 on Histone H3K9 Dimethylation of Cultured Ovine Somatic Cells and Development of Resulting Early Cloned Embryos. Reprod Domest Anim. 2014 Apr;49(2):e21-5. [Content Brief]

[3]. Singh N, et al. Inhibition of EHMT2 Induces a Robust Antiviral Response Against Foot-and-Mouth Disease and Vesicular Stomatitis Virus Infections in Bovine Cells. J Interferon Cytokine Res. 2016 Jan;36(1):37-47. [Content Brief]

[4]. Nualkaew T, et al. UNC0638 induces high levels of fetal hemoglobin expression in β-thalassemia/HbE erythroid progenitor cells[J]. Annals of hematology, 2020, 99: 2027-2036. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / 1M HCl	1 mM	1.9618 mL	9.8091 mL	19.6182 mL	49.0456 mL
	5 mM	0.3924 mL	1.9618 mL	3.9236 mL	9.8091 mL
	10 mM	0.1962 mL	0.9809 mL	1.9618 mL	4.9046 mL
	15 mM	0.1308 mL	0.6539 mL	1.3079 mL	3.2697 mL
	20 mM	0.0981 mL	0.4905 mL	0.9809 mL	2.4523 mL
	25 mM	0.0785 mL	0.3924 mL	0.7847 mL	1.9618 mL
	30 mM	0.0654 mL	0.3270 mL	0.6539 mL	1.6349 mL
	40 mM	0.0490 mL	0.2452 mL	0.4905 mL	1.2261 mL
	50 mM	0.0392 mL	0.1962 mL	0.3924 mL	0.9809 mL
	60 mM	0.0327 mL	0.1635 mL	0.3270 mL	0.8174 mL
1M HCl	80 mM	0.0245 mL	0.1226 mL	0.2452 mL	0.6131 mL
1M HCl	100 mM	0.0196 mL	0.0981 mL	0.1962 mL	0.4905 mL

Keywords

UNC0638

12 Cited Publications

100 mg Angebot einholen

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UNC0638

Anti-Infection Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Antiviral Compound Library

Autophagy Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) UNC0638

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UNC0638

Anti-Infection Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Antiviral Compound Library

Autophagy Compound Library

Reprogramming Compound Library

Chemical Probe Library

Anti-Blood Cancer Compound Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Methylation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) UNC0638

Alle Histone Methyltransferase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (12)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UNC0638 Related Classifications

HY-15273 Related Classifications