| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
CtBP1 and CtBP2 (dehydrogenase activity inhibition) [1]
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| ln Vitro |
Significant derepression of 40% of CtBP target genes (FGF9, CTNNB1, CEBPB, etc.) in MCF-7 (P<0.05) and 46% of CtBP target genes in MBA-MD-231 (P<0.05) was caused by MTOB sodium (10 mM); this increase in anterior epithelial E-cadherin/vimentin ratio was accompanied by a decrease in anterior mesenchymal CD44/CD24 ratio, with the trend being more pronounced in MCF-7 (P<0.05) [2].
Inhibits the dehydrogenase activity of CtBP1 and CtBP2 [1] Attenuates the growth and self-renewal of cancer stem cells in vitro [1] |
| ln Vivo |
Neurological Severity Score (NSS) scores are dramatically lowered and the rise in righting reflex time is effectively inhibited by sodium MTOB (860 mg/kg; IP, 1 hour and 18 hours after the first injury) [1].
In a repeated mild traumatic brain injury (mTBI) mouse model (two 0.5 J impacts spaced 24 h apart), administration of MTOB (860 mg/kg, i.p. at 1 h and 18 h after the first injury) significantly suppressed the increased duration of loss of righting reflex (LRR) following the second injury (p < 0.01) [1] In the same repeated mTBI model, MTOB treatment significantly decreased neurological severity scores (NSS) at 24 h (p < 0.001), 48 h (p < 0.01), and 72 h (p < 0.05) after the first injury [1] MTOB prevented a further increase in mRNA expression levels of CtBP-regulated proinflammatory genes (nine genes including IL1B, IL6, TNFA, S100A8, S100A9, NLRP3, ICAM1, PTGS2, and VCAM1) in brain tissues of mice receiving repeated TBI, with treated mice exhibiting lower or equal expression levels relative to single TBI mice [1] In a mouse model of colon cancer, MTOB decreases tumor burden [1] |
| Cell Assay |
MCF-7 and MDA-MB-231 cells were treated with 10 mM MTOB. After treatment, gene expression was measured by quantitative real-time PCR for CtBP target genes including those involved in genome stability, EMT, and stem cell pathways. Chromatin immunoprecipitation (ChIP) was performed to assess CtBP occupancy at target gene promoters. The E-Cadherin/Vimentin ratio was determined by quantitative methods, and the CD44/CD24 ratio was measured to evaluate stem cell-like properties [2].
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| Animal Protocol |
Animal/Disease Models: C57BL/6 mice (traumatic brain injury) [1]
Doses: 860 mg/kg Route of Administration: intraperitoneal (ip) injection, 1 hour and 18 hrs (hrs (hours)) after the first injury. Experimental Results: Effectively inhibited the increase in the duration of the righting reflex, and Dramatically reduce NSS scores. For the repeated mTBI experiment: MTOB sodium salt was dissolved in water to prepare a stock solution of 425 mg/mL, then diluted in PBS (vehicle) to desired final concentration freshly before use [1] Mice received two successive 0.5 J closed-head impacts spaced 24 h apart. MTOB was delivered via intraperitoneal (i.p.) injection at a dosage of 860 mg/kg at 1 h and 18 h after the first injury [1] |
| References |
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| Additional Infomation |
MTOB is a small-molecule inhibitor of CtBP dehydrogenase activity [1]
It is also known as 4-methylthio-2-oxobutyrate, an intermediate in the methionine salvage pathway [1] MTOB antagonizes the transcriptional regulatory activity of CtBP1 and CtBP2 by eviction from their target promoters [1] It has been shown to attenuate the growth and self-renewal of cancer stem cells in vitro and decrease tumor burden in a mouse model of colon cancer [1] |
| Molecular Formula |
C5H7NAO3S
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|---|---|
| Molecular Weight |
170.16
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| Exact Mass |
170.001
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| CAS # |
51828-97-8
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| PubChem CID |
23696623
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| Appearance |
White to off-white solid powder
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| Melting Point |
>300ºC(lit.)
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
10
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| Complexity |
126
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CSCCC(=O)C(=O)[O-].[Na+]
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| InChi Key |
IFSCKRWNXKWTLR-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C5H8O3S.Na/c1-9-3-2-4(6)5(7)8/h2-3H2,1H3,(H,7,8)/q+1/p-1
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| Chemical Name |
4-Methylsulfanyl-2-oxobutanoic acid sodium salt
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| Synonyms |
MTOB KMBA MTOB salt4-methylthio 2-oxobutyric acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~125 mg/mL (~734.60 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.8768 mL | 29.3841 mL | 58.7682 mL | |
| 5 mM | 1.1754 mL | 5.8768 mL | 11.7536 mL | |
| 10 mM | 0.5877 mL | 2.9384 mL | 5.8768 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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