UNC0642
Based on 27 publication(s) in Google Scholar
UNC0642, a chemical probe, is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC50 of <2.5 nM for G9a.
For research use only. We do not sell to patients.
- Purity: 99.42%
- CAS No.: 1481677-78-4
- Formula: C29H44F2N6O2
- Molecular Weight:546.70
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) UNC0642
More- Nat Cell Biol. 2023 Jul;25(7):1017-1032. [Abstract]
- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]
- Proc Natl Acad Sci U S A. 2019 Feb 19;116(8):2961-2966. [Abstract]
- Acta Pharmacol Sin. 2019 Aug;40(8):1076-1084. [Abstract]
- Genomics Proteomics Bioinformatics. 2025 Apr 29:qzaf035. [Abstract]
- Oncogene. 2021 Apr;40(15):2711-2724. [Abstract]
- Cell Chem Biol. 2022 Jul 21;29(7):1153-1161.e5. [Abstract]
- J Med Chem. 2024 Sep 12;67(17):15098-15117. [Abstract]
- Clin Transl Med. 2024 Jun;14(6):e1692. [Abstract]
- Ecotoxicol Environ Saf. 2024 Jul 5:282:116686. [Abstract]
- J Invest Dermatol. 2024 Jun 20:S0022-202X(24)01860-8. [Abstract]
- Cell Prolif. 2021 Jul;54(7):e13072. [Abstract]
- Int J Mol Sci. 2022 Apr 1;23(7):3911. [Abstract]
- Cancers (Basel). 2026 Apr 15;18(8):1250. [Abstract]
- iScience. 2024 Jul 8;27(8):110475. [Abstract]
- Hum Pathol. 2018 Feb:72:117-126. [Abstract]
- Res Sq. 2026 Jun 10.
- bioRxiv. 2026 May 1.
- bioRxiv. 2026 Feb 18:2026.02.16.706212. [Abstract]
- bioRxiv. 2026 Jan 23:2026.01.22.701139. [Abstract]
- bioRxiv. 2025 January 18.
- bioRxiv. 2024 September 15.
- McGill University. 2023 Jul.
- bioRxiv. 2023 Nov 9.
- bioRxiv. 2023 Nov 17.
- bioRxiv. 2023 Feb 23:2023.02.23.529773. [Abstract]
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Gel Electrophoresis
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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WB
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WB
All Histone Methyltransferase Isoforms
More
Biological Activity
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EHMT2/G9a/KMT1C |
EHMT1/GLP/KMT1D |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| 4T1 | IC50 |
1.55 %
Compound: UNC0642
|
Antiproliferative activity against mouse 4T1 cells incubated for 3 to 5 days by MTT assay
Antiproliferative activity against mouse 4T1 cells incubated for 3 to 5 days by MTT assay
|
[PMID: 37788550] |
| A-375 | IC50 |
3.062 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human A-375 cells assessed as reduction in cell viability by CCK-8 assay
Cytotoxicity against human A-375 cells assessed as reduction in cell viability by CCK-8 assay
|
[PMID: 32015216] |
| A-431 | IC50 |
3.38 μM
Compound: UNC0642
|
Antiproliferative activity against human A-431 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human A-431 cells measured after 72 hrs by MTT assay
|
[PMID: 34847495] |
| CWR22R | GI50 |
>10 μM
Compound: UNC0642
|
Cytotoxicity against human 22Rv1 cells assessed as growth inhibition measured for 7 days
Cytotoxicity against human 22Rv1 cells assessed as growth inhibition measured for 7 days
|
[PMID: 38602846] |
| HCT-116 | IC50 |
5.01 μM
Compound: UNC0642
|
Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay
|
[PMID: 34847495] |
| HeLa | IC50 |
1.74 μM
Compound: UNC0642
|
Antiproliferative activity against human HeLa cells measured after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells measured after 72 hrs by MTT assay
|
[PMID: 34847495] |
| HepG2 | IC50 |
2.69 μM
Compound: UNC0642
|
Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells measured after 72 hrs by MTT assay
|
[PMID: 34847495] |
| HT-29 | IC50 |
1.35 μM
Compound: UNC0642
|
Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay
|
[PMID: 34847495] |
| JJN-3 | IC50 |
17.77 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human JJN-3 cells expressing shG9a assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
Cytotoxicity against human JJN-3 cells expressing shG9a assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
|
[PMID: 32477831] |
| JJN-3 | IC50 |
18.995 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human JJN-3 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
Cytotoxicity against human JJN-3 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
|
[PMID: 32477831] |
| JJN-3 | IC50 |
5.85 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human JJN-3 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
Cytotoxicity against human JJN-3 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
|
[PMID: 32477831] |
| JJN-3 | IC50 |
6.807 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human JJN-3 cells expressing shNT assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
Cytotoxicity against human JJN-3 cells expressing shNT assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
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[PMID: 32477831] |
| K562 | IC50 |
0.92 μM
Compound: UNC0642
|
Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells measured after 72 hrs by MTT assay
|
[PMID: 34847495] |
| K562 | IC50 |
>10 μM
Compound: UNC0642
|
Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 8 days
Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 8 days
|
[PMID: 38602846] |
| KMS-12-BM | IC50 |
10.8 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human KMS-12-BM cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
Cytotoxicity against human KMS-12-BM cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
|
[PMID: 32477831] |
| KMS-12-BM | IC50 |
20.255 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human KMS-12-BM cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
Cytotoxicity against human KMS-12-BM cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
|
[PMID: 32477831] |
| KMS-12-BM | IC50 |
23.725 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human KMS-12-BM cells expressing shNT assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
Cytotoxicity against human KMS-12-BM cells expressing shNT assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
|
[PMID: 32477831] |
| KMS-12-BM | IC50 |
58.67 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human KMS-12-BM cells expressing shG9a assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
Cytotoxicity against human KMS-12-BM cells expressing shG9a assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
|
[PMID: 32477831] |
| L02 | IC50 |
3.23 μM
Compound: UNC0642
|
Cytotoxicity against human HL7702 cells measured after 72 hrs by MTT assay
Cytotoxicity against human HL7702 cells measured after 72 hrs by MTT assay
|
[PMID: 34847495] |
| L02 | IC50 |
6.99 μM
Compound: UNC0642
|
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 2 days by MTT assay
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[PMID: 37788550] |
| MDA-MB-231 | EC50 |
16700 nM
Compound: 7, UNC0642
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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
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[PMID: 24102134] |
| MDA-MB-231 | IC50 |
110 nM
Compound: 7, UNC0642
|
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 | IC50 |
3.23 μM
Compound: UNC0642
|
Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells measured after 72 hrs by MTT assay
|
[PMID: 34847495] |
| MDA-MB-231 | IC50 |
0.99 μM
Compound: UNC0642
|
Antiproliferative activity against human MDA-MB-231 cells incubated for 3 to 5 days by MTT assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 3 to 5 days by MTT assay
|
[PMID: 37788550] |
| MDA-MB-231 | IC50 |
1.003 μM
Compound: UNC0642
|
Antiproliferative activity against human MDA-MB-231 cells after 5 days by MTT assay
Antiproliferative activity against human MDA-MB-231 cells after 5 days by MTT assay
|
[PMID: 37788550] |
| MDA-MB-231 | IC50 |
3.31 μM
Compound: 3; UNC0642
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 96 hrs by CCK-8 cell viability assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 96 hrs by CCK-8 cell viability assay
|
[PMID: 39008565] |
| NCI-H1299 | GI50 |
>10 μM
Compound: UNC0642
|
Cytotoxicity against human NCI-H1299 cells assessed as growth inhibition incubated for 8 days
Cytotoxicity against human NCI-H1299 cells assessed as growth inhibition incubated for 8 days
|
[PMID: 38602846] |
| PANC-1 | EC50 |
3500 nM
Compound: 7, UNC0642
|
Cytotoxicity against human PANC1 cells after 48 hrs by Alamar Blue assay
Cytotoxicity against human PANC1 cells after 48 hrs by Alamar Blue assay
|
[PMID: 24102134] |
| PANC-1 | IC50 |
40 nM
Compound: 7, UNC0642
|
Inhibition of lysine methyltransferase G9a in human PANC1 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
Inhibition of lysine methyltransferase G9a in human PANC1 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
|
[PMID: 24102134] |
| PANC-1 | IC50 |
5.74 μM
Compound: 3; UNC0642
|
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 96 hrs by CCK-8 cell viability assay
Antiproliferative activity against human PANC-1 cells assessed as inhibition of cell growth incubated for 96 hrs by CCK-8 cell viability assay
|
[PMID: 39008565] |
| PC-3 | EC50 |
8900 nM
Compound: 7, UNC0642
|
Cytotoxicity against human PC3 cells after 48 hrs by Alamar Blue assay
Cytotoxicity against human PC3 cells after 48 hrs by Alamar Blue assay
|
[PMID: 24102134] |
| PC-3 | IC50 |
130 nM
Compound: 7, UNC0642
|
Inhibition of lysine methyltransferase G9a in human PC3 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
Inhibition of lysine methyltransferase G9a in human PC3 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
|
[PMID: 24102134] |
| RPMI-8226 | IC50 |
22 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability measured after 72 hrs by Celltiter-glo luminescent cell viability assay
|
[PMID: 32477831] |
| RPMI-8226 | IC50 |
26.925 μM
Compound: Chemical Probe: UNC0642
|
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
Cytotoxicity against human RPMI-8226 cells assessed as reduction in cell viability measured after 72 hrs by MTS assay
|
[PMID: 32477831] |
| U2OS | IC50 |
130 nM
Compound: 7, UNC0642
|
Inhibition of lysine methyltransferase G9a in human U2OS cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
Inhibition of lysine methyltransferase G9a in human U2OS cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay
|
[PMID: 24102134] |
| U2OS | EC50 |
6 μM
Compound: 7, UNC0642
|
Cytotoxicity against human U2OS cells after 48 hrs by Alamar Blue assay
Cytotoxicity against human U2OS cells after 48 hrs by Alamar Blue assay
|
[PMID: 24102134] |
UNC0642 displays high in vitro and cellular potency, low cell toxicity, and excellent selectivity. 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. UNC0642 displays high in vitro potency for GLP (IC50< 2.5 nM), similar to G9a. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, GPCRs, transporters, and ion channels. UNC0642 exhibits high potency at reducing the H3K9me2 mark, low cell toxicity, and good separation of functional potency and cell toxicity in a number of cell lines. It reduces clonogenicity in PANC-1 cells, a pancreatic carcinoma cell line[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1481677-78-4
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Appearance Solid
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Molecular Weight 546.70
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Formula C29H44F2N6O2
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Color Off-white to light yellow
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SMILES
CC(N1CCC(NC2=C3C=C(OC)C(OCCCN4CCCC4)=CC3=NC(N5CCC(F)(F)CC5)=N2)CC1)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (27)
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Journal Impact Factor
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Most Recent
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Nat Cell Biol
Dynamic de novo heterochromatin assembly and disassembly at replication forks ensures fork stability. [Abstract]2023 Jul;25(7):1017-1032. PMID: 37414849
UNC0642 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Jul;25(7):1017-1032. [Abstract]
Immunoblot showed pCHK1 levels in wild type cells (WT), wild type where G9a activity was inhibited with UNC0642 (2 h) (WT + UNC0642), and a G9a knock out clone (G9a-/-), in the presence or in the absence of replication stress.
UNC0642 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Jul;25(7):1017-1032. [Abstract]
UNC0642 (1 μM; 2 h). Dynamics of H3K9me2 PTM at replication sites in the presence (UNC0642-) or in the absence of G9a activity (UNC0642+) at ongoing (UT) and stalled (HU) replication forks.
UNC0642 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2023 Jul;25(7):1017-1032. [Abstract]
UNC0642 (1 µM; 2 h) treatment caused TIG3 cells to restart replication more slowly (shorter IdU tracks) than untreated cells after release from HU.
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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
UNC0642 purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129. [Abstract]
H3K9Me2, PTEN, p-AKT, and AKT expression levels are measured in PC9/ER xenograft tumor tissues. β-actin is used as a loading control.
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Proc Natl Acad Sci U S A
2019 Feb 19;116(8):2961-2966. PMID: 30718431 -
Acta Pharmacol Sin
Inhibition of G9a by a small molecule inhibitor, UNC0642, induces apoptosis of human bladder cancer cells. [Abstract]2019 Aug;40(8):1076-1084. PMID: 30765842
UNC0642 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2019 Aug;40(8):1076-1084. [Abstract]
UNC0642 suppresses the activity of G9a protein according to detection of the level of H3K9me2. T24 and J82 cells are treated with UNC0642 for 24 h at the indicated concentration.
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Genomics Proteomics Bioinformatics
Integrated Computational and Functional Screening Identify G9a Inhibitors for SETD2-Mutant Leukemia. [Abstract]2025 Apr 29:qzaf035. PMID: 40300107 -
Oncogene
2021 Apr;40(15):2711-2724. PMID: 33712705 -
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 -
J Med Chem
Discovery of a Novel Benzimidazole Derivative Targeting Histone Deacetylase to Induce Ferroptosis and Trigger Immunogenic Cell Death. [Abstract]2024 Sep 12;67(17):15098-15117. PMID: 39145486 -
Clin Transl Med
Inhibition of HDAC2 sensitises antitumour therapy by promoting NLRP3/GSDMD-mediated pyroptosis in colorectal cancer. [Abstract]2024 Jun;14(6):e1692. PMID: 38804602 -
Ecotoxicol Environ Saf
The critical role of SETDB1-mediated CCND1/PI3K/AKT pathway via p53-RS di-methylation at K370 in the proliferation of WRL68 cells induced by nicotine. [Abstract]2024 Jul 5:282:116686. PMID: 38971100 -
J Invest Dermatol
DNA Damage Stress Control Is a Truncated Large T Antigen and Euchromatic Histone Lysine Methyltransferase 2-Dependent Central Feature of Merkel Cell Carcinoma. [Abstract]2024 Jun 20:S0022-202X(24)01860-8. PMID: 38908781 -
Cell Prolif
EZH2-mediated inhibition of KLF14 expression promotes HSCs activation and liver fibrosis by downregulating PPARγ. [Abstract]2021 Jul;54(7):e13072. PMID: 34031939
UNC0642 purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2021 Jul;54(7):e13072. [Abstract]
The HSCs shown were treated with DNMT inhibitors (5-azacytidine, 2 μmol/L), G9a inhibitors (UNC0642, 2 μmol/L), and pan-HDAC inhibitor Givinostat (ITF-2357, 100 nmol/L) for 48 hours, or with EZH2 inhibitors (EPZ-6438, 10 μmol/L) for 72 hours. KLF14 expression was detected by Western blotting.
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Int J Mol Sci
Dual Inhibition of H3K9me2 and H3K27me3 Promotes Tumor Cell Senescence without Triggering the Secretion of SASP. [Abstract]2022 Apr 1;23(7):3911. PMID: 35409271 -
Cancers (Basel)
Comparative Preclinical Evaluation of BIX-01294 and UNC0642 as EHMT2-Targeting Anticancer Agents. [Abstract]2026 Apr 15;18(8):1250. PMID: 42073575 -
iScience
Genome-scale CRISPR-Cas9 screen identifies host factors as potential therapeutic targets for SARS-CoV-2 infection. [Abstract]2024 Jul 8;27(8):110475. PMID: 39100693 -
Hum Pathol
2018 Feb:72:117-126. PMID: 29133140 -
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bioRxiv
Radiation synergizes with BET inhibition to stimulate durable, systemic anti-tumor immunity in murine cancer models. [Abstract]2026 Feb 18:2026.02.16.706212. PMID: 41757027 -
bioRxiv
2026 Jan 23:2026.01.22.701139. PMID: 41648188 -
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bioRxiv
Combinatory EHMT and PARP inhibition induces an interferon response and a CD8 T cell-dependent tumor regression in PARP inhibitor-resistant models. [Abstract]2023 Feb 23:2023.02.23.529773. PMID: 36865165
Solvent & Solubility
DMSO : 50 mg/mL (91.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.57 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.57 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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal 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.
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%+
-
+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
MDA-MB-231, PC3, and U2OS cells are treated with inhibitors (UNC0642) 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. In-cell western assay is performed as described previously[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice: Standard PK studies are performed using male Swiss albino mice. Plasma and brain concentrations are measured at 0.08, 0.25, 0.5, 1, 2, 4, 8, and 24 h following a single IP injection of UNC0642 at 5 mg/kg. The compound concentration at each time point in plasma or brain is the average value from 3 test animals[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (276 KB)
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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)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Liu F, et al. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-8942. [Content Brief]
[2]. Wang L, et al. Targeting EHMT2 reverses EGFR-TKI resistance in NSCLC by epigenetically regulating the PTEN/AKT signaling pathway. Cell Death Dis. 2018 Jan 26;9(2):129 [Content Brief]
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8292 mL | 9.1458 mL | 18.2916 mL | 45.7289 mL |
| 5 mM | 0.3658 mL | 1.8292 mL | 3.6583 mL | 9.1458 mL | |
| 10 mM | 0.1829 mL | 0.9146 mL | 1.8292 mL | 4.5729 mL | |
| 15 mM | 0.1219 mL | 0.6097 mL | 1.2194 mL | 3.0486 mL | |
| 20 mM | 0.0915 mL | 0.4573 mL | 0.9146 mL | 2.2864 mL | |
| 25 mM | 0.0732 mL | 0.3658 mL | 0.7317 mL | 1.8292 mL | |
| 30 mM | 0.0610 mL | 0.3049 mL | 0.6097 mL | 1.5243 mL | |
| 40 mM | 0.0457 mL | 0.2286 mL | 0.4573 mL | 1.1432 mL | |
| 50 mM | 0.0366 mL | 0.1829 mL | 0.3658 mL | 0.9146 mL | |
| 60 mM | 0.0305 mL | 0.1524 mL | 0.3049 mL | 0.7621 mL | |
| 80 mM | 0.0229 mL | 0.1143 mL | 0.2286 mL | 0.5716 mL |