SGC8158
Based on 1 Customer Validation
SGC8158 is a selective PRMT7 inhibitor. SGC8158 occupies the adenosine/hydrophobic pocket, blocks PRMT7 methylation, and is noncompetitive with peptide. SGC8158 has an IC50 of <2.5 nM and a Kd of 6.4 nM against PRMT7. SGC8158 is not cell membrane permeable and requires the prodrug SGC3027 (HY-112445) to exert cellular activity, being released by reductases to reduce Socs3 transcription, STAT3 occupancy, HSP70, survival/proliferation, and increase ER stress, DNA damage, endothelial death, and impair angiogenesis. SGC8158 can be used for research on SARS-CoV-2 infection and C. difficile infection.
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- Pureza : 97.6%
- No. CAS: 3062376-84-2
- Fòrmula: C27H31ClN6O3S
- Peso molecular:555.09
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Almacenamiento:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Actividad biológica
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Chemical Information
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- Pureza y Documentación
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Ver todos los productos específicos de isoformas Histone Methyltransferase
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Actividad biológica
Descripciòn
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PRMT7 <2.5 nM (IC50) |
PRMT7 6.4 nM (Kd) |
PRMT4 140 nM (IC50) |
PRMT5 150 nM (IC50) |
In Vitro
SGC8158 (varying concentrations; 2.5 min) inhibits CamA DNA adenine methyltransferase activity in vitro with an IC50 of 7.1 µM[8].
SGC8158 (30 µM) binds CamA in a cell-free ITC assay with KD 6 µM[8].
SGC8158 (1 μM; 24 h) reduces Socs3 transcription in H9c2 cardiomyocytes under JAK/STAT3-activating conditions[3].
SGC8158 (1 μM; 24 h) inhibition of Prmt7 in H9c2 cells reduces STAT3 recruitment to the Socs3 promoter and alters histone modifications consistent with restricted chromatin accessibility[3].
SGC8158 (1 µM; 24 h) impairs proliferation, migration, tube formation, and survival while exacerbating ER stress and DNA damage in stressed C166 endothelial cells[4].
SGC8158 (500 μM) binds the SARS-CoV-2 nsp14/nsp10 complex with a Kd of ~6 μM by ITC[5].
SGC8158 (<2.5 nM-10 µM; 60 min at 23 °C) potently inhibits PRMT7 methyltransferase activity in vitro with IC50 <2.5 nM for H2B peptide and 294 nM for full-length HSPA8, and PRMT7-dependent HSPA8 methylation shows apparent Km values of 1.6 µM for SAM and 10.6 µM for HSPA8[1].
SGC8158 (1.85-150 nM; 60 s contact) binds PRMT7 with a KD of 6.4 nM in SPR[1].
SGC8158 selectively inhibits PRMT7 with an IC50 <2.5 nM and has an IC50 of 140 nM against PRMT4[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H9c2 rat cardiomyoblast cells
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Concentration:1 μM
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Incubation Time:24 h
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Result:Decreased Socs3 expression relative to control.
- Research Protocol for Infectious Diseases
- Human pluripotent stem cell endothelial-cell differentiation
- Vascular/Branching Fractal Analysis
- Endothelial Tube Formation Assay
- Genotoxicity/Mutagenicity Study
- Endothelial Cell Migration/Angiogenic Sprouting Assay
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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No. CAS 3062376-84-2
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Appearance Solid
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Peso molecular 555.09
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Fòrmula C27H31ClN6O3S
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Color White to off-white
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SMILES
O[C@H]1[C@@H](O)[C@H](N2C(N=CN=C3N)=C3N=C2)O[C@@H]1CSCCCCNCC4=CC=CC(C5=CC=C(Cl)C=C5)=C4
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[6]. Kulkarni AS, et al. Tailoring PRMT Inhibition: Shifting PRMT7 Selectivity to PRMT4 through “T-Shape” Strategy and “Linker-Specific” Preferences. Journal of Medicinal Chemistry. 2026 May 1;69(9):9977-90. [Content Brief]
[7]. Talukdar A, et al. Fascinating Transformation of SAM-Competitive Protein Methyltransferase Inhibitors from Nucleoside Analogues to Non-Nucleoside Analogues. Journal of medicinal chemistry. 2022 Feb 10;65(3):1662-1684. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SGC8158 Related Classifications
HY-114211 Related Classifications
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