UNC0642

Name: UNC0642
Brand: MedChemExpress
SKU: HY-13980
Rating: 5.0 (20 reviews)

Cat. No.: HY-13980 Purity: 99.92%: FAQs
Data Sheet SDS COA Handling Instructions

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UNC0642 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.

UNC0642 Chemical Structure

CAS No. : 1481677-78-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 119	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 119	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 825	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 20 publication(s) in Google Scholar

18 Publications Citing Use of MCE UNC0642

: 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.

: 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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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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

UNC0642 is a potent and selective lysine methyltransferases G9a and GLP inhibitor, with an IC₅₀ of <2.5 nM for G9a.

IC₅₀ & Target

EHMT2/G9a/KMT1C

EHMT1/GLP/KMT1D

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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]
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]
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	EC₅₀	16700 nM Compound: 7, UNC0642	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	3.23 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]
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]
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]
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]
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	6000 nM 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]

In Vitro

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 K_i 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.

In Vivo

A single intraperitoneal (IP) injection (5 mg/kg) of UNC0642 results in a plasma C_max (maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL^[1].

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

Molecular Weight

546.70

Formula

C₂₉H₄₄F₂N₆O₂

CAS No.

1481677-78-4

Appearance

Solid

Color

Off-white to light yellow

SMILES

CC(N1CCC(NC2=C3C=C(OC)C(OCCCN4CCCC4)=CC3=NC(N5CCC(F)(F)CC5)=N2)CC1)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8292 mL	9.1458 mL	18.2916 mL
5 mM	0.3658 mL	1.8292 mL	3.6583 mL
10 mM	0.1829 mL	0.9146 mL	1.8292 mL

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.57 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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (275 KB) SDS (392 KB)

COA (248 KB) LCMS (270 KB)

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]

Cell Assay ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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

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

UNC0642 Related Classifications

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:

UNC06421481677-78-4UNC 0642UNC-0642Histone MethyltransferaseInhibitorinhibitorinhibit

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UNC0642

Customer Review

UNC0642 Related Antibodies

18 Publications Citing Use of MCE UNC0642

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View All Histone Methyltransferase Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

UNC0642 Related Antibodies

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Complete Stock Solution Preparation Table

UNC0642 Related Classifications

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