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UNC0642

Catalog No. T4166 CAS 1481677-78-4

Synonyms: UNC-0642, UNC 0642

UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

UNC0642, CAS 1481677-78-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 34.00
2 mg	In stock	$ 48.00
5 mg	In stock	$ 79.00
10 mg	In stock	$ 133.00
25 mg	In stock	$ 243.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 597.00
200 mg	In stock	$ 868.00
1 mL * 10 mM (in DMSO)	In stock	$ 96.00

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Purity: 99.5%

Purity: 98.75%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	UNC0642 is an effective and specific G9a/GLP inhibitor (IC50< 2.5 nM).
Targets&IC50	G9a:<2.5 nM, GLP:<2.5 nM
In vitro	UNC0642 (Ki: 3.7±1 nM) is competitive with the peptide substrate and non-competitive with the cofactor SAM. UNC0642 is more than 300-fold selective for G9a and GLP over a broad range of kinases, transporters, GPCRs, and ion channels. UNC0642 exhibits high potency at low cell toxicity, reducing the H3K9me2 mark, and good separation of functional potency in a number of cell lines.
In vivo	UNC0642 (5 mg/kg, i.p.) results in a plasma Cmax of 947 ng/mL and an AUC of 1265 h·ng/ml.
Cell Research	MDA-MB-231, PC3, and U2OS cells are treated with 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.
Animal Research	Mouse: 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 UNC0642 (5 mg/kg, i.p.). The compound concentration at each time point in plasma or brain is the average value from 3 test animals[1].

Synonyms	UNC-0642, UNC 0642
Molecular Weight	546.7
Formula	C29H44F2N6O2
CAS No.	1481677-78-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (91.46 mM), Sonification and heating are recommended.

References and Literature

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):8931-42. doi: 10.1021/jm401480r. Epub 2013 Oct 31.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Anti-Diabetic Compound Library Histone Modification Compound Library Methylation Compound Library Glycometabolism Compound Library Fluorochemical Library Chromatin Modification Compound Library Epigenetics Compound Library Stem Cell Differentiation Compound Library

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You can also refer to dose conversion for different animals. More

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

UNC0642 1481677-78-4 Chromatin/Epigenetic Histone Methyltransferase inhibit UNC-0642 Inhibitor UNC 0642 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.