1. Epigenetics Anti-infection Apoptosis Cell Cycle/DNA Damage
  2. Histone Methyltransferase SARS-CoV MDM-2/p53 CDK Apoptosis
  3. GSK3326595

GSK3326595  (Synonyms: EPZ015938)

Cat. No.: HY-101563 Purity: 99.97%
COA Handling Instructions

GSK3326595 (EPZ015938) est un inhibiteur de protéine arginine méthyltransférase 5 (PRMT5) qui est puissant, sélectif et réversible avec un IC50 de 6,2 nM.

GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma.

For research use only. We do not sell to patients.

GSK3326595 Chemical Structure

GSK3326595 Chemical Structure

CAS No. : 1616392-22-3

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10 mM * 1 mL in DMSO
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Customer Review

Based on 16 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK3326595 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Jun 8;12(1):3444.  [Abstract]

    Breast cancer cells are treated with DMSO, 0.5 μM GSK3326595 (GSK) for 4 days before examining cell viability.
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GSK3326595 is a protein arginine methyltransferase 5 (PRMT5) inhibitor. GSK3326595 decreases SARS-CoV-2 infection, inhibits cancer cell proliferation and induces pro-inflammatory macrophage polarization and increases hepatic triglyceride levels without affecting atherosclerosis. GSK3326595 can be used for research of relapsed/refractory mantle cell lymphoma[1][2][3][4][5].

    IC50 & Target

    PRMT5

     

    CDK4

     

    CDK6

     

    In Vitro

    GSK3326595 (10-100 nM, 24-72 h) inhibits SARS-CoV-2spike pseudovirus infection HEK-293 cells and A549 cells by attenuating ACE2-RBD interaction[1].
    GSK3326595 (100 nM, 12 h) primes peritoneal macrophages to IFN-gamma-induced M1 polarization[3].
    GSK3326595 (0.15-10 μM, 72 h) induces cell death in MCL cell[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Western Blot Analysis[4]

    Cell Line: HEK-293T cells, A549 cells
    Concentration: 10 nM, 25 nM, 50 nM, 100 nM
    Incubation Time: 48 h
    Result: Strongly inhibited ACE2-RBD interaction at low concentration.
    Inhibited SARS-CoV-2 Omicron and other variants Spike1 binding with ACE2.
    Inhibits SARS-CoV-2 spike pseudovirus infection host cells.

    Cell Cytotoxicity Assay[1]

    Cell Line: MCL cells
    Concentration: 0.15 μM, 0.3 μM, 0.6 μM, 1.25 μM, 2.5 μM, 5 μM, 10 μM
    Incubation Time: 72 h
    Result: Resulted in modest growth inhibition in MCL cells.
    In Vivo

    GSK3326595 (5 mg/kg, Intraperitoneal injection, three times a week for 9 weeks) increased hepatic triglyceride levels without affecting atherosclerosis in LDL receptor knockout mice[3]. GSK3326595 (25-50 mg/kg, Oral, once a day for 2 weeks) enhances the efficacy of anti-programed cell death protein 1 (PD-1) immune checkpoint therapy (ICT) in hepatocellular carcinoma (HCC) in myelocytomatosis transgene turned on (MYC-ON) mice[5].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: LDL receptor knockout mice[3]
    Dosage: 5 mg/kg
    Administration: Intraperitoneal injection (i.p.)
    Result: Did not alter atherosclerosis susceptibility.
    Increased hepatic triglyceride levels without changing the hyperlipidemia extent.
    Activated genes involved in fatty acid acquisition.
    Animal Model: myelocytomatosis transgene turned on mice[5]
    Dosage: 25 mg/kg, 50 mg/kg
    Administration: Oral
    Result: Significantly suppressed tumor growth at 50 mg/kg.
    Showed better therapeutic efficacy at 25 mg/kg.
    Clinical Trial
    Molecular Weight

    452.55

    Formula

    C24H32N6O3

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(C)N1CCC(NC2=NC=NC(C(NC[C@H](O)CN3CCC(C=CC=C4)=C4C3)=O)=C2)CC1

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 62.5 mg/mL (138.11 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2097 mL 11.0485 mL 22.0970 mL
    5 mM 0.4419 mL 2.2097 mL 4.4194 mL
    10 mM 0.2210 mL 1.1049 mL 2.2097 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (5.52 mM); Clear solution

    • 2.

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.52 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.08 mg/mL (4.60 mM); Clear solution; Need ultrasonic

    • 4.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.08 mg/mL (4.60 mM); Suspended solution; Need ultrasonic

    • 5.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (4.60 mM); Clear solution

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

    Purity: 99.97%

    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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    Product Name:
    GSK3326595
    Cat. No.:
    HY-101563
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