Cat.NO.:A333018 Purity:98%
Product Details of Thiamet G
| CAS No. : | 1009816-48-1 |
| Formula : |
C9H16N2O4S |
| M.W : |
248.30
|
| SMILES Code : | O[C@H]1[C@H](O)[C@@]2([H])N=C(NCC)S[C@@]2([H])O[C@@H]1CO |
| MDL No. : | MFCD15144964 |
Safety of Thiamet G
| GHS Pictogram: |  |
| Signal Word: | Warning |
| Hazard Statements: | H317 |
| Precautionary Statements: | P261-P280 |
Isoform Comparison
Biological Activity
In Vitro:
| Concentration | Treated Time | Description | References |
| HCT116 cells | 1 μM | 6 hours | To study the response of OGT intron retention to O-GlcNAc levels | PMC5588854 |
| 293A-TOA cells | 1 μM | 6 hours | To study the response of OGT intron retention to O-GlcNAc levels | PMC5588854 |
| Neuroblastoma N2a cells | 5 μM | 12 hours | Thiamet-G (TG), an OGA inhibitor, increased O-GlcNAcylation of N2a cells in a dose-dependent manner without affecting cell viability. TG treatment also inhibited H2O2-induced apoptosis in N2a cells. | PMC10943090 |
| BV2 cells | 200 ng/mL | 12 hours | To evaluate the effect of TMG on M1 polarization of BV2 cells. Results showed that TMG treatment inhibited LPS-induced M1 polarization and reduced mRNA expression of pro-inflammatory cytokines (TNF-α, iNOS, IL-1β, IL-6, and MCP-1). | PMC5536801 |
| RT4 cells | 10 μM | 16 hours | To evaluate the effect of O-GlcNAcylation on autophagy in bladder cancer cells. Results showed that TG treatment increased O-GlcNAcylation and p62 levels and decreased LC3 II expression, indicating inhibition of autophagy. | PMC7063793 |
| 5637 cells | 10 μM | 16 hours | To evaluate the effect of O-GlcNAcylation on autophagy in bladder cancer cells. Results showed that TG treatment increased O-GlcNAcylation and p62 levels and decreased LC3 II expression, indicating inhibition of autophagy. | PMC7063793 |
| Cartilage endplate stem cells (CESCs) | 1 μM | 21 days | Thiamet-G promoted osteogenic differentiation and inhibited chondrogenic differentiation of CESCs | PMC6883626 |
| Human rheumatoid arthritis synovial fibroblasts (RASFs) | 1-5 µM | 24 hours | To evaluate the inhibitory effect of Thiamet G on IL-1β-induced IL-6 and IL-8 production, results showed that Thiamet G dose-dependently inhibited IL-1β-induced IL-6 and IL-8 production and increased the expression of O-GlcNAc-modified proteins. | PMC9400595 |
| BeWo human trophoblast cells | 5 μM | 24 hours | TMG upregulated the expression of syncytiotrophoblast-associated transcription factors OVOL1 and GCM1 and the cell fusion gene ERVFRD1 | PMC7599815 |
| Mouse blastocysts | 5 μM | 24 hours | TMG increased O-GlcNAcylation levels, altered OGT and OGA localization, and promoted mouse blastocyst invasion of endometrial epithelium | PMC7599815 |
| Human umbilical vein endothelial cells (HUVECs) | 1 μM | 24 hours | TMG pretreatment reduced GSDMD-N protein levels, indicating that TMG may function by inhibiting GSDMD cleavage | PMC10776498 |
| Primary mouse vascular smooth muscle cells (VSMC) | 10 μM | 6 hours | Increased O-GlcNAcylation and promoted VSMC calcification | PMC4030422 |
| HEK293 cells | 32 nM (EC50) | 6 hours | To evaluate the effect of Thiamet G on O-GlcNAcylated protein levels, showing a dose-dependent increase in O-protein levels. | PMC5437664 |
In Vivo:
| Administration | Dosage | Frequency | Description | References |
| Mice | DSS-induced colitis model | Oral gavage | 0.2 g/kg | Once daily for 2 weeks | Augmented intestinal epithelial O-GlcNAc signaling, alleviated chemical-induced colitis | PMC6079539 |
| Mouse | R6/2 mouse model | In vitro treatment | 0.5uM | 4 hours | Thiamet-G significantly reduced cell death in primary cortical neurons transfected with HTT 82Q and rescued nucleocytoplasmic trafficking defects with the nuclear restoration of both endogenous Ran and exogenous NLS-tdTomato-NES. | PMC5595097 |
| Mice | C57BL/6J mice | Intracranial injection | 1 mM | Single injection | Injection of Thiamet G in the VTA and NAc facilitated neuronal O-GlcNAcylation and decreased the operant response to sucrose as well as the latency to fall in rotarod test. | PMC8975958 |
| Rhesus monkeys | Rhesus monkeys and OgaΔBr mice | Intravenous injection | 10 mg/kg | Single dose, PET scan performed 45 minutes after administration | To evaluate the inhibitory effect of Thiamet-G on OGA, results showed that Thiamet-G significantly reduced brain uptake of the radioligand, indicating high efficacy in inhibiting OGA. | PMC6354227 |
| NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice | Xenograft tumor model | Intraperitoneal injection | 20 mg/kg | Once daily for 24 days | To study the effect of ISS deletion on tumor growth | PMC5588854 |
| Mice | Low-dose streptozotocin (STZ)-induced diabetic mouse model | Intravenous injection | 20 mg/kg | Weekly for 2 months | Increased vascular O-GlcNAcylation, accelerated vascular calcification and worsened aortic compliance | PMC4030422 |
| Mouse | REM sleep deprivation (REMSD) model | Intraperitoneal injection | 20 mg/kg | Daily for 72 hours | Thiamet G restored REMSD-induced learning and memory impairment and dendritic spine density | PMC8804064 |
| C57BL/6 mice | Middle cerebral artery occlusion (MCAO) model | Intraperitoneal injection | 20 mg/kg | Preventive group: once daily for 3 days before surgery; Therapeutic group: starting at 0.5 h after surgery, once daily for 3 days | To evaluate the neuroprotective effect of TMG in MCAO mice. Results showed that TMG significantly reduced infarct volume, improved neurological deficit scores, and modulated the expression of pro-inflammatory and anti-inflammatory cytokines. Additionally, TMG reduced the number of Iba1+ cells, decreased expression of M1 markers, and increased expression of M2 markers. | PMC5536801 |
| Mice | Transient or permanent middle cerebral artery occlusion model | Intraperitoneal or intravenous injection | 30 mg/kg | 18 hours before or 30 minutes after stroke induction | Increased O-GlcNAcylation levels, improved stroke outcome in both young and aged mice | PMC5493893 |
| Mice | Young mice (2-month-old) | Intraperitoneal injection | 30 mg/kg/day | Once daily for 35 days | To mimic age-related elevation of O-GlcNAc and study its effect on spermatogenesis. Results showed that high O-GlcNAcylation led to decreased sperm concentration, reduced testis weight and organ index, and impaired spermatogenesis. | PMC10185674 |
| RTg4510 mice | Tauopathy model | Oral | 500 mg/kg/day | Daily administration for 8 weeks | To evaluate the effect of Thiamet G on tau pathology, showing that chronic Thiamet G treatment significantly reduced insoluble tau aggregates and phosphorylated tau species in the brain and decreased total tau levels in cerebrospinal fluid. | PMC5437664 |
| C57BL/6J mice | LPS-induced sepsis model | Intravenous injection | 600 μg/kg | Single dose, lasting 12 hours | TMG treatment increased blood perfusion in the liver, mesentery, and lower limbs of mice and reduced vascular endothelial injury | PMC10776498 |
Protocol
| Bio Calculators | ||||
| Preparing Stock Solutions |  |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
4.03mL 0.81mL 0.40mL |
20.14mL 4.03mL 2.01mL |
40.27mL 8.05mL 4.03mL |
|
| Dissolving Methods |
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:
in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day; The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
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