SGC3027 |
Catalog No.GC19849
One-Click Copy Product Info
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SGC3027 is a cell-permeable prodrug that is converted by cellular reductases into the active compound SGC8158.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2624313-13-7
Sample solution is provided at 25 µL, 10mM.
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SGC3027 is a cell-permeable prodrug that is converted by cellular reductases into the active compound SGC8158. SGC8158 (low cell permeability) is a potent, selective, and S-adenosyl methionine (SAM)-competitive inhibitor of Protein Arginine Methyltransferase 7 (PRMT7), which suppresses the symmetric dimethylation of histone H4 at arginine 3 (H4R3me2s). Inhibition of PRMT7 leads to a significant reduction in the levels of arginine monomethylated HSP70 family stress-related proteins, thereby affecting protein homeostasis[1][2].
In vitro, SGC3027 (0.3-10µM; 48h) inhibited Hsp70 methylation with IC50 of 2.4±0.1μM in C2C12 cells[2]. SGC3027 (3µM; 48h) pretreatment decreased cell survival and increased apoptosis levels after heat shock (44℃; 20min) in WT MEF cells[2]. SGC3027 (4µM; 48h) pretreatment decreased cell survival after bortezomib (30nM; 20h) treatment in WT MEF[2]. SGC3027 (10μM; 48h) upregulated the expression of interferon pathway-, antigen presentation-, and chemokine-related genes in B16.F10 cells[3].
In vivo, SGC3027 (10μM; intratumorally injected; 4d) significantly decreased tumor growth and increased survival in mice bearing B16.F10 melanoma cells[3]. SGC3027 (50mg/kg; i.p.; administered 1 day before infection and for 2 days after infection) showed improved survival rates following VSV infection (2×108 PFU; i.p.; 24h), and reduced immune cell infiltration and lung injury in WT mice[4].
References:
[1] Cermakova, Katerina, and H Courtney Hodges. “Next-Generation Drugs and Probes for Chromatin Biology: From Targeted Protein Degradation to Phase Separation.” Molecules (Basel, Switzerland) vol. 23,8 E1958. 6 Aug. 2018.
[2] Szewczyk, Magdalena M et al. “Pharmacological inhibition of PRMT7 links arginine monomethylation to the cellular stress response.” Nature communications vol. 11,1 2396. 14 May. 2020.
[3] Srour N, Villarreal OD, Hardikar S, et al. PRMT7 ablation stimulates anti-tumor immunity and sensitizes melanoma to immune checkpoint blockade. Cell Rep. 2022;38(13):110582.
[4] Zhu, Junji et al. “Arginine monomethylation by PRMT7 controls MAVS-mediated antiviral innate immunity.” Molecular cell vol. 81,15 (2021): 3171-3186.e8.
| Cell experiment [1]: | |
Cell lines | C2C12 |
Preparation Method | Cells were treated with SGC3027 for 2 days. After 48h, cells were lysed in lysis buffer. Cell lysates were analyzed in western blot for unmethylated and monomethylated Hsp70 levels. The IC50 value was determined using GraphPad Prism 7 software. |
Reaction Conditions | 0.3-10µM; 48h |
Applications | SGC3027 inhibited Hsp70 methylation with IC50 of 2.4±0.1μM in C2C12 cells. |
| Animal experiment [2]: | |
Animal models | Female Tcra−/− mice |
Preparation Method | 7 to 12 weeks old mice were subcutaneously injected with 1×106 cells/100μL B16.F10 melanoma cells into the right flank on day 0 and then intratumorally injected with 10μM of DMSO or SGC3027 on day 7, 8, 9 and 10 with or without intraperitoneal injection with anti-PD-1 and anti-CTLA-4 on day 3, 6, 9 and 12. Tumor size and overall survival were measured and calculated. |
Dosage form | 10μM; intratumorally injected; 4d |
Applications | SGC3027-treated mice significantly decreased tumor growth and survival, compared with mice injected with either DMSO or combination CTLA-4 and PD-1 blockade. |
References: | |
| Cas No. | 2624313-13-7 | SDF | |
| Formula | C41H47ClN6O6S | M.Wt | 787.37 |
| Solubility | DMSO : 250 mg/mL | Storage | Store at -20°C |
| 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 | 1.2701 mL | 6.3503 mL | 12.7005 mL |
| 5 mM | 254 μL | 1.2701 mL | 2.5401 mL |
| 10 mM | 127 μL | 635 μL | 1.2701 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: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)