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In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Kinase selectivity assays
Selectivity of UNC 0642 against a panel of 50 kinases was conducted using a standard off-chip mobility shift assay technology.
Cell lines
PANC-1 and MDA-MB-231 cells
Preparation method
The solubility of this compound in DMSO is > 18.5 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.
Reacting condition
0, 0.5 or 1 μM; 2 weeks
Applications
UNC 0642 concentration-dependently reduced clonogenicity in PANC-1 cells but it showed no effect on clonogenicity in MDA-MB-231 cells. Besides, UNC 0642 potently reduced cellular levels of H3K9me2 with low cell toxicity, which resulted in a good separation of functional potency and cell toxicity with a tox/function ratio of 88 in PANC-1 cells.
Animal models
Male Swiss Albino mice
Dosage form
5 mg/kg; i.p.
A single intraperitoneal injection of 5 mg/kg UNC 0642 resulted in a plasma Cmax of 947 ng/mL and an AUC of 1265 h·ng/mL. However, UNC 0642 only displayed modest brain penetration, with a brain/plasma ratio of 0.33, which suggested that UNC 0642 might not be suitable for exploration of the role of G9a/GLP in the CNS.
Other notes
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
References:
[1]. Liu F, Barsyte-Lovejoy D, Li F, Xiong Y, Korboukh V, Huang XP, Allali-Hassani A, Janzen WP, Roth BL, Frye SV, Arrowsmith CH, Brown PJ, Vedadi M, Jin J. Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP. J Med Chem. 2013 Nov 14;56(21):8931-42.