Thiamet G | O-GlcNAcase Inhibitor

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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

GHS Pictogram:
Signal Word:	Warning
Hazard Statements:	H317
Precautionary Statements:	P261-P280

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

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

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CAS No.: 1009816-48-1

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CAS No.: 1009816-48-1

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Preparing Stock Solutions		1mg	5mg	10mg
Preparing Stock Solutions	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	Animal experiment 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. Protocol 1 Protocol 2 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. Protocol 1

Precautionary Statements-General
Code	Phrase
P101	If medical advice is needed,have product container or label at hand.
P102	Keep out of reach of children.
P103	Read label before use
Prevention
Code	Phrase
P201	Obtain special instructions before use.
P202	Do not handle until all safety precautions have been read and understood.
P210	Keep away from heat/sparks/open flames/hot surfaces. - No smoking.
P211	Do not spray on an open flame or other ignition source.
P220	Keep/Store away from clothing/combustible materials.
P221	Take any precaution to avoid mixing with combustibles
P222	Do not allow contact with air.
P223	Keep away from any possible contact with water, because of violent reaction and possible flash fire.
P230	Keep wetted
P231	Handle under inert gas.
P232	Protect from moisture.
P233	Keep container tightly closed.
P234	Keep only in original container.
P235	Keep cool
P240	Ground/bond container and receiving equipment.
P241	Use explosion-proof electrical/ventilating/lighting/equipment.
P242	Use only non-sparking tools.
P243	Take precautionary measures against static discharge.
P244	Keep reduction valves free from grease and oil.
P250	Do not subject to grinding/shock/friction.
P251	Pressurized container: Do not pierce or burn, even after use.
P260	Do not breathe dust/fume/gas/mist/vapours/spray.
P261	Avoid breathing dust/fume/gas/mist/vapours/spray.
P262	Do not get in eyes, on skin, or on clothing.
P263	Avoid contact during pregnancy/while nursing.
P264	Wash hands thoroughly after handling.
P265	Wash skin thouroughly after handling.
P270	Do not eat, drink or smoke when using this product.
P271	Use only outdoors or in a well-ventilated area.
P272	Contaminated work clothing should not be allowed out of the workplace.
P273	Avoid release to the environment.
P280	Wear protective gloves/protective clothing/eye protection/face protection.
P281	Use personal protective equipment as required.
P282	Wear cold insulating gloves/face shield/eye protection.
P283	Wear fire/flame resistant/retardant clothing.
P284	Wear respiratory protection.
P285	In case of inadequate ventilation wear respiratory protection.
P231 + P232	Handle under inert gas. Protect from moisture.
P235 + P410	Keep cool. Protect from sunlight.
Response
Code	Phrase
P301	IF SWALLOWED:
P304	IF INHALED:
P305	IF IN EYES:
P306	IF ON CLOTHING:
P307	IF exposed:
P308	IF exposed or concerned:
P309	IF exposed or if you feel unwell:
P310	Immediately call a POISON CENTER or doctor/physician.
P311	Call a POISON CENTER or doctor/physician.
P312	Call a POISON CENTER or doctor/physician if you feel unwell.
P313	Get medical advice/attention.
P314	Get medical advice/attention if you feel unwell.
P315	Get immediate medical advice/attention.
P320
P302 + P352	IF ON SKIN: wash with plenty of soap and water.
P321
P322
P330	Rinse mouth.
P331	Do NOT induce vomiting.
P332	IF SKIN irritation occurs:
P333	If skin irritation or rash occurs:
P334	Immerse in cool water/wrap n wet bandages.
P335	Brush off loose particles from skin.
P336	Thaw frosted parts with lukewarm water. Do not rub affected area.
P337	If eye irritation persists:
P338	Remove contact lenses, if present and easy to do. Continue rinsing.
P340	Remove victim to fresh air and keep at rest in a position comfortable for breathing.
P341	If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P342	If experiencing respiratory symptoms:
P350	Gently wash with plenty of soap and water.
P351	Rinse cautiously with water for several minutes.
P352	Wash with plenty of soap and water.
P353	Rinse skin with water/shower.
P360	Rinse immediately contaminated clothing and skin with plenty of water before removing clothes.
P361	Remove/Take off immediately all contaminated clothing.
P362	Take off contaminated clothing and wash before reuse.
P363	Wash contaminated clothing before reuse.
P370	In case of fire:
P371	In case of major fire and large quantities:
P372	Explosion risk in case of fire.
P373	DO NOT fight fire when fire reaches explosives.
P374	Fight fire with normal precautions from a reasonable distance.
P376	Stop leak if safe to do so. Oxidising gases (section 2.4) 1
P377	Leaking gas fire: Do not extinguish, unless leak can be stopped safely.
P378
P380	Evacuate area.
P381	Eliminate all ignition sources if safe to do so.
P390	Absorb spillage to prevent material damage.
P391	Collect spillage. Hazardous to the aquatic environment
P301 + P310	IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.
P301 + P312	IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.
P301 + P330 + P331	IF SWALLOWED: Rinse mouth. Do NOT induce vomiting.
P302 + P334	IF ON SKIN: Immerse in cool water/wrap in wet bandages.
P302 + P350	IF ON SKIN: Gently wash with plenty of soap and water.
P303 + P361 + P353	IF ON SKIN (or hair): Remove/Take off Immediately all contaminated clothing. Rinse SKIN with water/shower.
P304 + P312	IF INHALED: Call a POISON CENTER or doctor/physician if you feel unwell.
P304 + P340	IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P304 + P341	IF INHALED: If breathing is difficult, remove victim to fresh air and keep at rest in a position comfortable for breathing.
P305 + P351 + P338	IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing.
P306 + P360	IF ON CLOTHING: Rinse Immediately contaminated CLOTHING and SKIN with plenty of water before removing clothes.
P307 + P311	IF exposed: call a POISON CENTER or doctor/physician.
P308 + P313	IF exposed or concerned: Get medical advice/attention.
P309 + P311	IF exposed or if you feel unwell: call a POISON CENTER or doctor/physician.
P332 + P313	IF SKIN irritation occurs: Get medical advice/attention.
P333 + P313	IF SKIN irritation or rash occurs: Get medical advice/attention.
P335 + P334	Brush off loose particles from skin. Immerse in cool water/wrap in wet bandages.
P337 + P313	IF eye irritation persists: Get medical advice/attention.
P342 + P311	IF experiencing respiratory symptoms: call a POISON CENTER or doctor/physician.
P370 + P376	In case of fire: Stop leak if safe to Do so.
P370 + P378	In case of fire:
P370 + P380	In case of fire: Evacuate area.
P370 + P380 + P375	In case of fire: Evacuate area. Fight fire remotely due to the risk of explosion.
P371 + P380 + P375	In case of major fire and large quantities: Evacuate area. Fight fire remotely due to the risk of explosion.
Storage
Code	Phrase
P401
P402	Store in a dry place.
P403	Store in a well-ventilated place.
P404	Store in a closed container.
P405	Store locked up.
P406	Store in corrosive resistant/ container with a resistant inner liner.
P407	Maintain air gap between stacks/pallets.
P410	Protect from sunlight.
P411
P412	Do not expose to temperatures exceeding 50 oC/ 122 oF.
P413
P420	Store away from other materials.
P422
P402 + P404	Store in a dry place. Store in a closed container.
P403 + P233	Store in a well-ventilated place. Keep container tightly closed.
P403 + P235	Store in a well-ventilated place. Keep cool.
P410 + P403	Protect from sunlight. Store in a well-ventilated place.
P410 + P412	Protect from sunlight. Do not expose to temperatures exceeding 50 oC/122oF.
P411 + P235	Keep cool.
Disposal
Code	Phrase
P501	Dispose of contents/container to ...
P502	Refer to manufacturer/supplier for information on recovery/recycling

Physical hazards
Code	Phrase
H200	Unstable explosive
H201	Explosive; mass explosion hazard
H202	Explosive; severe projection hazard
H203	Explosive; fire, blast or projection hazard
H204	Fire or projection hazard
H205	May mass explode in fire
H220	Extremely flammable gas
H221	Flammable gas
H222	Extremely flammable aerosol
H223	Flammable aerosol
H224	Extremely flammable liquid and vapour
H225	Highly flammable liquid and vapour
H226	Flammable liquid and vapour
H227	Combustible liquid
H228	Flammable solid
H229	Pressurized container: may burst if heated
H230	May react explosively even in the absence of air
H231	May react explosively even in the absence of air at elevated pressure and/or temperature
H240	Heating may cause an explosion
H241	Heating may cause a fire or explosion
H242	Heating may cause a fire
H250	Catches fire spontaneously if exposed to air
H251	Self-heating; may catch fire
H252	Self-heating in large quantities; may catch fire
H260	In contact with water releases flammable gases which may ignite spontaneously
H261	In contact with water releases flammable gas
H270	May cause or intensify fire; oxidizer
H271	May cause fire or explosion; strong oxidizer
H272	May intensify fire; oxidizer
H280	Contains gas under pressure; may explode if heated
H281	Contains refrigerated gas; may cause cryogenic burns or injury
H290	May be corrosive to metals
Health hazards
Code	Phrase
H300	Fatal if swallowed
H301	Toxic if swallowed
H302	Harmful if swallowed
H303	May be harmful if swallowed