Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 21 nM, while exhibiting 37, 000-fold selectivity over human lysosomal –hexosaminidase.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
2 mg | In stock | $ 37.00 | |
5 mg | In stock | $ 57.00 | |
10 mg | In stock | $ 94.00 | |
25 mg | In stock | $ 198.00 | |
50 mg | In stock | $ 361.00 | |
100 mg | In stock | $ 537.00 | |
500 mg | In stock | $ 1,190.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 57.00 |
Description | Thiamet G is a potent, selective O-GlcNAcase inhibitor with Kiof 21 nM, while exhibiting 37, 000-fold selectivity over human lysosomal –hexosaminidase. |
Targets&IC50 | O-GlcNAcase:21 nM(Ki) |
In vitro | In NGF-differentiated PC-12 cells, inhibition of O-GlcNAcase by Thiamet G increases the cellular levels of O-GlcNAc with EC50 of approximately 30 nM. Thiamet G (100 mM) reduces tau phosphorylation by approximately 2.1-fold, 2.7-fold, 1.2-fold and 1.3-fold for Ser396, Thr231, Ser422 and Ser262, respectively. [1] Thiamet G (12.5 nM and 25 nM) significantly enhances p38 phosphorylation by increasing O-GlcNAcylation in mesangial cells. [2] In O-GlcNAc transferase or O-GlcNAcase gain of function cells, thiamet-G restores the assembly of the spindle and partially rescues histone phosphorylation. [3] |
In vivo | In rats, thiamet G (50 mg/kg) administrated by i.v. crosses the blood brain barrier and then results in increase in brain O-GlcNAc levels in a dose- and time-dependent manner, and reduction of tau phosphorylation in rat brain. Thiamet G is also orally bioavailable. [1] O-GlcNAc accumulation induced by thiamet G stimulates chondrogenic differentiation in C57/bl mice by increasing the gene expression of differentiation markers, as well as the activity of MMP-2 and -9. [4] |
Kinase Assay | All enzymatic assays are performed in triplicate at 37°C using 4-methylumbelliferyl N-acetyl-β-d-glucosaminide dehydrate as substrate. 1 nM of purified OGA is incubated with the compounds for 5 min, and then 0.2 mM of the substrate is added. The liberation of 4-methylumbellifery is monitored by kinetic reading at excitation/emission 355/460 nm using a Tecan M200 plate in a mode of 60 s/cycle and 15 cycles in total. |
Cell Research | Jurkat cells are seeded at 6000 cells/well in a 96-well plate, and 12 h later, cells are treated with compounds for the indicated time. Cell viability is determined by XTT assay. |
Synonyms | TMG |
Molecular Weight | 248.3 |
Formula | C9H16N2O4S |
CAS No. | 1009816-48-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12.4 mg/mL (50 mM)
You can also refer to dose conversion for different animals. More
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Thiamet G 1009816-48-1 Autophagy Others Inhibitor TMG inhibit inhibitor