[CAS NO. 1009816-48-1] ThiametG
PRODUCTS SPECIFICATIONS [1009816-48-1]
DESCRIPTION [1009816-48-1]
Overview
| MDL | MFCD15144964 |
|---|---|
| Molecular Weight | 248.30 |
| Molecular Formula | C9H16N2O4S |
| SMILES | O[C@H]1[C@H](O)[C@@]2([H])N=C(NCC)S[C@@]2([H])O[C@@H]1CO |
16 Publications Citing Use of MCE
- [1]Nat Chem Biol. 2022 Jul 25.
- [2]Nat Commun. 2021 May 11;12(1):2672.
- [3]Redox Biol. 2021 Jul;43:101994.
- [4]EMBO Mol Med. 2021 Nov 29;e14678.
- [5]Leukemia. 2022 Jan 8.
- [6]Theranostics. 2020 Jun 1;10(16):7178-7192.
- [7]Cell Rep. 2021 Sep 21;36(12):109739.
- [8]Cell Rep. 2019 Aug 27;28(9):2386-2396.e5.
- [9]EMBO Rep. 2021 Apr 15;e51649.
- [10]Neurotherapeutics. 2021 Jan;18(1):340-363.
- [11]J Biomed Sci. 2022 Feb 14;29(1):13.
- [12]J Biol Chem. 2019 Nov 8;294(45):16620-16633.
- [13]Cell Signal. 2021 Apr 3;110002.
- [14]J Cancer Res Clin Oncol. 2022 Nov 18.
- [15]Burns Trauma. 08 October 2021.
- [16]In Vitro Cell Dev Biol Anim. 2022 May 5.
Summary
Thiamet G is a potent and selective inhibitor of O-GlcNAcase (OGA) , which acts to remove O-GlcNAc from modified proteins, with K i of 20 nM for human OGA.
IC50 & Target
Ki: 20 nM (Human OGA) [1]
In Vitro
Thiamet G (1 μM) induces a clear increase in the accumulation of O-GlcNAcylated proteins of ATDC5 cells. O-GlcNAc accumulation induced by Thiamet G also evokes a clear increase in the activity of these MMPs. Thiamet G (1 μM) induces the phosphorylation of JNK, ERK, and p38 but not phosphorylation of Akt [2] . Thiamet G (0.1-10 μM) does not significantly affect the cell viability. Thiamet G decreases phosphorylation of tau and alters the microtubule dynamics [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Thiamet G (500 mg/kg/d) increases global and tau O-GlcNAc and reduces neurodegeneration. Thiamet G-treated group has 1.4-fold more motor neurons and hinders tau-driven neurodegeneration within this transgenic model. Thiamet G treatment therefore has no detectable effect on mice lacking the P301L transgene, indicating that prevention of neurodegeneration and weight loss is mediated by Thiamet G treatment only in the context of the P301L transgene. In Thiamet G-treated mice, the O-GlcNAc increases in the brain and spinal cord tissues [1] . Thiamet G (20 mg/kg, i.p.) increases O-GlcNAc levels in brain, liver, and knee of the C57BL/6 mice in a dose-dependent manner [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
H 2 O : ≥ 50 mg/mL ( 201.37 mM )
DMSO : ≥ 45 mg/mL ( 181.23 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.0274 mL | 20.1369 mL | 40.2739 mL |
| 5 mM | 0.8055 mL | 4.0274 mL | 8.0548 mL |
| 10 mM | 0.4027 mL | 2.0137 mL | 4.0274 mL |
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1.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (201.37 mM); Clear solution; Need ultrasonic
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2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (8.38 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (8.38 mM); Clear solution
References
- [1] Yuzwa SA, et al. Increasing O-GlcNAc slows neurodegeneration and stabilizes tau against aggregation. Nat Chem Biol. 2012 Feb 26;8(4):393-9.
- [2] Andrés-Bergós J, et al. The increase in O-linked N-acetylglucosamine protein modification stimulates chondrogenic differentiation both in vitro and in vivo. J Biol Chem. 2012 Sep 28;287(40):33615-28.
- [3] Ding N, et al. Thiamet-G-mediated inhibition of O-GlcNAcase sensitizes human leukemia cells to microtubule-stabilizing agent NSC 125973. Biochem Biophys Res Commun. 2014 Oct 24;453(3):392-7.