GSK3368715 dihydrochloride (Synonyms: EPZ019997 dihydrochloride) |
Catalog No.GC36192
One-Click Copy Product Info
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GSK3368715 dihydrochloride is a potent, reversible type I PRMT inhibitor with anti-tumor effects in human cancer models.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1628925-77-8
Sample solution is provided at 25 µL, 10mM.
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GSK3368715 dihydrochloride is a potent, reversible type I PRMT inhibitor with anti-tumor effects in human cancer models[1]. GSK3368715 decrease the PRMT1-specific histone mark H4R3me2a without affecting the methylation of H3R17me2a (by CARM1 and PRMT6) or PABP1 (by CARM1)[3].
In vitro, treatment with 6µM GSK3368715 for 24 hours inhibited cGAS methylation levels in HEK293T cells[1]. Treatment with 6μM GSK3368715 for 48 hours increased the phosphorylation level of IRF3 in HeLa cells expressing wild-type cGAS[1]. The growth half-maximal inhibitory concentration (gIC50) values of GSK3368715 against MM cell lines ranged from 0.021µM to 14.405µM[2]. GSK3368715 at concentrations ranging from 0.12 to 1μM reduced colony growth in a dose-dependent manner when MDA-MB-468 cells were cultured on plastic for 9 days[3].
In vivo, oral administration of GSK3368715 at 80mg/kg once daily for 14 days resulted in elevated mPD-L1 expression across multiple organs and tissues in six-weeks old BALB/c female mice[1]. Treatment with GSK3368715 (80mg/kg; orally; once daily for 5 days) in nude mice bearing MDA-MB-468–derived xenografts led to increased global monomethylation, decreased H4R3me2a levels in tumors, and a significant delay in tumor growth[3].
References:
[1] Liu J, Bu X, Chu C, et al. PRMT1 mediated methylation of cGAS suppresses anti-tumor immunity. Nat Commun. 2023;14(1):2806.
[2] Hussain T, Awasthi S, Shahid F, Yi SS, Sahni N, Aldaz CM. Therapeutic potential of PRMT1 as a critical survival dependency target in multiple myeloma. BMC Cancer. 2025;25(1):1704.
[3] Suresh S, Huard S, Brisson A, et al. PRMT1 Regulates EGFR and Wnt Signaling Pathways and Is a Promising Target for Combinatorial Treatment of Breast Cancer. Cancers (Basel). 2022;14(2):306.
| Cell experiment [1]: | |
Cell lines | HEK293T cells |
Preparation Method | HEK293T cells were treated with MS023 (6µM) or GSK3368715 (6µM) for 24 hours, and the cGAS methylation level was detected. |
Reaction Conditions | 6µM; 24h |
Applications | 6µM GSK3368715 and MS023 blocked cGAS methylation. |
| Animal experiment [1]: | |
Animal models | Six-weeks old BALB/c female mice |
Preparation Method | Six-weeks old BALB/c female mice were treated with GSK3368715 (80mg/kg body weight, by gastric gavage), or respective vehicle, one dose daily for 14 days. GSK3368715 was dissolved in ddH2O. Then, tissues and organs were collected and analyzed the expression of mPD-L1. |
Dosage form | 80mg/kg/d; 14d; p.o. |
Applications | mPD-L1 expression was elevated in multiple mouse organs/tissues in mice treated with GSK3368715, like ovary, spleen, colon… |
References: | |
| Cas No. | 1628925-77-8 | SDF | |
| Synonyms | EPZ019997 dihydrochloride | ||
| Canonical SMILES | CNCCN(CC1=CNN=C1C2CCC(COCC)(COCC)CC2)C.Cl.Cl | ||
| Formula | C20H40Cl2N4O2 | M.Wt | 439.46 |
| Solubility | DMSO: 250 mg/mL (568.88 mM); water：100mg/ml(227.55 mM) | Storage | Store at 4°C, stored under nitrogen |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2755 mL | 11.3776 mL | 22.7552 mL |
| 5 mM | 455.1 μL | 2.2755 mL | 4.551 mL |
| 10 mM | 227.6 μL | 1.1378 mL | 2.2755 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)