2. Epigenetics
  3. Histone Methyltransferase
  4. UNC0642

UNC0642 

Cat. No.: HY-13980 Purity: 99.92%
COA Handling Instructions

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

UNC0642 Chemical Structure

CAS No. : 1481677-78-4

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 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 11 publication(s) in Google Scholar

Top Publications Citing Use of Products

    UNC0642 purchased from MCE. 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 MCE. 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.

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 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

    IC50: <2.5 nM (G9a)[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].

    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 Cmax (maximum concentration) of 947 ng/mL and an AUC (area under the curve) of 1265 hr*ng/mL[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    546.70

    Appearance

    Solid

    Formula

    C29H44F2N6O2
    CAS No.
    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (91.46 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.92%

    COA (248 KB) LCMS (270 KB)

    Handling Instructions (2659 KB)
    References
    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
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    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.

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    Keywords:

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

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