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

GSK3326595  (Synonyms: EPZ015938)

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

Molarity Calculator

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

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 70 In-stock
50 mg USD 250 In-stock
100 mg USD 450 In-stock
200 mg USD 750 In-stock
500 mg   Get quote  
1 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 18 publication(s) in Google Scholar

GSK3326595 Related Antibodies

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.

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

    View All CDK Isoform Specific Products:

    View All Isoforms
    CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

    • 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

     

    Cellular Effect
    Cell Line Type Value Description References
    HCT-116 IC50
    189 nM
    Compound: GSK3326595
    Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
    Antiproliferative activity against MTAP knockout human HCT-116 cells assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
    		[PMID: 35041419]
    HCT-116 IC50
    237 nM
    Compound: GSK3326595
    Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
    Antiproliferative activity against human HCT-116 cells expressing wild type MTAP assessed as reduction in cell viability incubated for 5 days followed by replacement with fresh medium containing compound and measured after 5 days by CTG assay
    		[PMID: 35041419]
    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.

    GSK3326595 Related Antibodies

    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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

    • Protocol 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

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.97%

    SDS (392 KB)

    COA (244 KB) HNMR (279 KB) LCMS (92 KB) Elemental Analysis Report (103 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2097 mL 11.0485 mL 22.0970 mL 55.2425 mL
    5 mM 0.4419 mL 2.2097 mL 4.4194 mL 11.0485 mL
    10 mM 0.2210 mL 1.1049 mL 2.2097 mL 5.5243 mL
    15 mM 0.1473 mL 0.7366 mL 1.4731 mL 3.6828 mL
    20 mM 0.1105 mL 0.5524 mL 1.1049 mL 2.7621 mL
    25 mM 0.0884 mL 0.4419 mL 0.8839 mL 2.2097 mL
    30 mM 0.0737 mL 0.3683 mL 0.7366 mL 1.8414 mL
    40 mM 0.0552 mL 0.2762 mL 0.5524 mL 1.3811 mL
    50 mM 0.0442 mL 0.2210 mL 0.4419 mL 1.1049 mL
    60 mM 0.0368 mL 0.1841 mL 0.3683 mL 0.9207 mL
    80 mM 0.0276 mL 0.1381 mL 0.2762 mL 0.6905 mL
    100 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5524 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    GSK3326595 Related Classifications

    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.

    Keywords:

    GSK33265951616392-22-3EPZ015938GSK 3326595GSK-3326595EPZ 015938EPZ-015938Histone MethyltransferaseSARS-CoVMDM-2/p53CDKApoptosisSARS coronavirusCyclin dependent kinaseHEK-293THK2BEAS-2Bmantle cell lymphoma (MCL)LDL receptor knockout micemyelocytomatosis transgene turned on miceInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email Address *

    Phone Number *

    		 

    Organization Name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    GSK3326595
    Cat. No.:
    HY-101563
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (392 KB) Français - FR (392 KB) Deutsch - DE (392 KB) Norwegian - NO (392 KB) Español - ES (392 KB) Swedish - SV (392 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.