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UNC0631

Cat. No. M3103
UNC0631 Structure
Size Price Availability
5mg USD 133  USD133 Out of stock
10mg USD 232  USD232 Out of stock
50mg USD 787  USD787 Out of stock
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Quality Control & Documentation
Biological Activity

UNC0631 is a selective histone lysine methyltransferase (HMTase) inhibitor for G9a and GLP with IC50 of 6 nM and 15 nM, respectively, with excellent potency in a variety of cell lines and excellent separation of functional potency versus cell toxicity.

Protocol (for reference only)
Cell Experiment
Cell lines MDA-MB-231, PC3, HCT116, 22RV1, MCF7 and IMR90 cells
Preparation method Culturing MDA-MB-231, PC3, HCT116 cells in RPMI with 10% FBS, 22RV1 cells in alphaMEM and 10% FBS, MCF7 and IMR90 cells in DMEM with 10% FBS. Treating cells with inhibitors for 48 h. The media is removed and replaced with DMEM 10% FBS without phenol red supplemented with 1mg/mL of MTT and incubated for 1–2 h. Live cells reduce yellow MTT to purple formazan. The resulting formazanis solubilized in acidified isopropanol and 1% Triton. Formazan signal absorbance is measured at 570 nm and corrected for the 650 nm background. IC50s are calculated using GraphPad Prizm statistical package with sigmoidal variable slope dose response curve fit
Concentrations ~10 μM
Incubation time 48 hours
Animal Experiment
Animal models
Formulation
Dosages
Administration
Chemical Information
Molecular Weight 635.93
Formula C37H61N7O2
CAS Number 1320288-19-4
Form Solid
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Varvara Maksimova, et al. HeLa TI cell-based assay as a new approach to screen for chemicals able to reactivate the expression of epigenetically silenced genes

[2] Wenbo Ma, et al. The Histone Methyltransferase G9a Promotes Cholangiocarcinogenesis Through Regulation of the Hippo Pathway Kinase LATS2 and YAP Signaling Pathway

[3] Zichao Zhao, et al. Expression of G9a in breast cancer and its effect on proliferation of breast cancer cells in vitro

[4] Feng Liu, et al. Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines

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  Catalog
Abmole Inhibitor Catalog




Keywords: UNC0631 supplier, Histone Methyltransferase, inhibitors, activators


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