1. GPCR/G Protein
    Epigenetics
  2. Sigma Receptor
    Histone Methyltransferase

UNC0642 

Cat. No.: HY-13980 Purity: 99.89%
Handling Instructions

UNC0642 is a potent and selective G9a/GLP inhibitor, inhibits G9a/GLP with an IC50 of less than 2.5 nM.

For research use only. We do not sell to patients.
UNC0642 Chemical Structure

UNC0642 Chemical Structure

CAS No. : 1481677-78-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 130 In-stock
5 mg USD 108 In-stock
10 mg USD 180 In-stock
50 mg USD 540 In-stock
100 mg USD 1020 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

    UNC0642 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.

    The effects of treatment with the indicated epigenetic inhibitors on cleaved PARP (Clv-PARP) expression in both PC9/ER and HCC827/ER cells. β-actin is used as a loading control.

    UNC0642 purchased from MCE. Usage Cited in: Cell Death Dis. 2018 Jan 26;9(2):129.

    H3K9Me2, PTEN, p-AKT, and AKT expression levels are measured in PC9/ER xenograft tumor tissues. β-actin is used as a loading control.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    UNC0642 is a potent and selective G9a/GLP inhibitor, inhibits G9a/GLP with an IC50 of less than 2.5 nM.

    IC50 & Target

    IC50: less than 2.5 nM (G9a, GLP)[1]

    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 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].

    In Vivo

    A single intraperitoneal (IP) injection (5 mg/kg) of UNC0642results in a plasma Cmax (maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL[1].

    References
    Preparing Stock Solutions
    Concentration Volume 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
    Please refer to the solubility information to select the appropriate solvent.
    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
    Molecular Weight

    546.7

    Formula

    C₂₉H₄₄F₂N₆O₂

    CAS No.

    1481677-78-4

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 295 mg/mL (Need ultrasonic and warming)

    UNC0642 is prepared in vehicle (saline)[2].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    Product Name:
    UNC0642
    Cat. No.:
    HY-13980
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