GSK3368715 3HCl

Catalog No.S8858 Batch:S885801

Technical Data

Formula

C₂₀H₄₁Cl₃N₄O₂

Molecular Weight

475.92

CAS No.

2227587-26-8

Solubility (25°C)*

In vitro

DMSO

81 mg/mL (170.19 mM)

Water

81 mg/mL (170.19 mM)

Ethanol

81 mg/mL (170.19 mM)

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.05mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 81 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.675mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 13.5 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

GSK3368715 3HCl is a potent inhibitor of type I protein arginine methyltransferases (PRMT) that inhibits PRMT1, 3, 4, 6 and 8 with Ki^app vaules ranging from 1.5 to 81 nM.

Targets

PRMT1 ^[1]

PRMT3 ^[1]

PRMT4 ^[1]

PRMT6 ^[1]

PRMT8 ^[1]

In vitro

GSK3368715 is a potent, reversible, SAM uncompetitive inhibitor of type I PRMTs that produces a shift in arginine methylation states on hundreds of substrates from ADMA to MMA and SDMA. As a monotherapy, GSK3368715 induces anti-proliferative effects on cell lines from a broad range of hematological and solid tumor types in vitro.^[1]

In vivo

GSK3368715 has potent, anti-proliferative activity across cell lines representing a range of solid and hematological malignancies and can completely inhibit tumor growth or cause regressions of tumor models in vivo.^[1]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines 249 cancer cell lines (Toledo cells, BxPC3 cells, MiaPaca-2 cells, ACHN cells, MDA-MB-468 cells, RKO cells, Panc03.27 cells, etc.) Concentrations 0.75 nM, 2 μM Incubation Time 30 min, 3 h - 168 h Method In Cell Western. RKO cells are seeded in a clear bottom 384 well plates andtreated with a 20-point two-fold dilution series of GSK3368715 (29,325.5 to 0.03 nM) or 0.15% DMSO. Plates are incubated for 3 days at 37℃ in 5% CO₂. Cells are fixed with ice-cold methanol for 30 minutes at room temperature, washed with phosphate buffered saline (PBS), then incubated with Odyssey blocking buffer (Licor) for 1 hour at room temperature.
Animal Study:^{^[1]}	Animal Models Female NMRI nu/nu mice (NMRI-Foxn1nu) implanted with tumor fragment Dosages 75 mg/kg, 150 mg/kg, 300 mg/kg Administration Oral gavage

Cell Assay:^{^[1]}

Cell lines
249 cancer cell lines (Toledo cells, BxPC3 cells, MiaPaca-2 cells, ACHN cells, MDA-MB-468 cells, RKO cells, Panc03.27 cells, etc.)
Concentrations
0.75 nM, 2 μM
Incubation Time
30 min, 3 h - 168 h
Method
In Cell Western. RKO cells are seeded in a clear bottom 384 well plates andtreated with a 20-point two-fold dilution series of GSK3368715 (29,325.5 to 0.03 nM) or 0.15% DMSO. Plates are incubated for 3 days at 37℃ in 5% CO₂. Cells are fixed with ice-cold methanol for 30 minutes at room temperature, washed with phosphate buffered saline (PBS), then incubated with Odyssey blocking buffer (Licor) for 1 hour at room temperature.

Animal Study:^{^[1]}

Animal Models
Female NMRI nu/nu mice (NMRI-Foxn1nu) implanted with tumor fragment
Dosages
75 mg/kg, 150 mg/kg, 300 mg/kg
Administration
Oral gavage

References

[1] Andrew Fedoriw, et al. Cancer Cell. 2019 Jul 8;36(1):100-114.e25.

Selleck's GSK3368715 3HCl has been cited by 5 publications

PRMT1 mediated methylation of cGAS suppresses anti-tumor immunity [ Nat Commun, 2023, 14(1):2806]	PubMed: 37193698
FACS-based genome-wide CRISPR screens define key regulators of DNA damage signaling pathways [ Mol Cell, 2023, 83(15):2810-2828.e6]	PubMed: 37541219
Epigenetic drug screening defines a PRMT5 inhibitor-sensitive pancreatic cancer subtype [ JCI Insight, 2022, 7(10)e151353]	PubMed: 35439169
Modulation of IKs channel-PIP2 interaction by PRMT1 plays a critical role in the control of cardiac repolarization [ J Cell Physiol, 2022, 10.1002/jcp.30775]	PubMed: 35580065
Purification and Identification of Natural Inhibitors of Protein Arginine Methyltransferases from Plants [ Mol Cell Biol, 2022, e0052321]	PubMed: 35311588

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.