| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TMBIM6 (transmembrane BAX inhibitor motif containing 6). TMBIM6 antagonist-1 prevents TMBIM6 binding to mTORC2.
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| ln Vitro |
With IC50 values of 1.7 μM, 2.6 μM, and 2.6 μM, respectively, TMBIM6 antagonist-1 (BIA, 0.5-10 μM, 3 days) substantially and dose-dependently decreases the viability of HT1080, MCF7, MDA-MB-2341, and SKBR3 cells. 2.4 μM[1]. Cell migration of HT1080, MCF7, MDA-MB-231, and SKBR3 was decreased by TMBIM6 antagonist-1 (BIA, 10 μM) treatment, but not of TMBIM6 KO HT1080 cells [1].
TMBIM6 antagonist-1 prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and regulates TMBIM6-leaky Ca2+. By inhibiting the interaction between TMBIM6 and mTORC2, the compound modulates mTOR signaling and calcium homeostasis. TMBIM6 antagonist-1 has been shown to dramatically reduce the growth of tumors driven by cells. |
| ln Vivo |
The TMBIM6 antagonist-1 (1 mg/kg, IP, 5 days a week for 25 days) dramatically reduces the growth of tumors driven by cells[1].
In vivo, TMBIM6 antagonist-1 (1 mg/kg, IP, 5 days a week for 25 days) dramatically reduces the growth of tumors driven by cells. As a TMBIM6 antagonist, it disrupts the interaction between TMBIM6 and mTORC2, leading to decreased mTORC2 activity and reduced tumor growth. |
| Enzyme Assay |
In vitro receptor binding assays for TMBIM6 antagonist-1 are performed to evaluate its binding to TMBIM6. The compound's ability to disrupt the interaction between TMBIM6 and mTORC2 is assessed using co-immunoprecipitation or protein-protein interaction assays.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HT1080, MCF7, MDA-MB-2341 and SKBR3 cells. Tested Concentrations: 0.5-10 μM. Incubation Duration: 3 days. Experimental Results: Inhibited cell viability. Western Blot Analysis[1] Cell Types: WT and TMBIM6 KO HT1080 cells. Tested Concentrations: 0, 2, 5 μM. Incubation Duration: Experimental Results: Downregulated the protein levels of AKT-pS473. In vitro cell-based assays are conducted to evaluate the effects of TMBIM6 antagonist-1 on mTOR signaling, calcium homeostasis, and cell viability. Cells are treated with the compound, and mTORC2 activity is measured by assessing AKT phosphorylation at Ser473. Intracellular calcium levels are measured using fluorescent calcium indicators. Cell viability and proliferation are assessed using standard assays such as MTT or CCK-8. |
| Animal Protocol |
Animal/Disease Models: Six- to eight-week BklNbt: BALB/c/nu/nu old mice (HT1080 and MDA-MB-231 cells)[1].
Doses: 1 mg/kg. Route of Administration: IP 5 days per week during 25 days. Experimental Results: Impaired cell-driven tumor growth. In vivo animal studies with TMBIM6 antagonist-1 are conducted in tumor xenograft models. The compound is administered intraperitoneally at a dose of 1 mg/kg, 5 days a week for 25 days. Its effects on tumor growth, survival, and biomarkers of mTOR signaling and calcium homeostasis are assessed. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for TMBIM6 antagonist-1. As a small molecule inhibitor, its ADME properties would be characterized in standard preclinical studies.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for TMBIM6 antagonist-1. As a TMBIM6 antagonist, its toxicity profile would be expected to be related to its mechanism of action. Standard safety assessments would be required for any therapeutic development.
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| References | |
| Additional Infomation |
TMBIM6 antagonist-1 (BAX-inhibitor-1) is a potential TMBIM6 antagonist that prevents TMBIM6 binding to mTORC2, decreases mTORC2 activity, and regulates TMBIM6-leaky Ca2+. It has been shown to dramatically reduce tumor growth in vivo. The compound is a valuable research tool for studying the role of TMBIM6 in cancer, apoptosis, and calcium signaling. It is not approved for human therapeutic use and is strictly for research purposes.
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| Molecular Formula |
C15H12N2O3
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|---|---|
| Molecular Weight |
268.267
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| Exact Mass |
268.084
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| CAS # |
123134-61-2
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| PubChem CID |
11425639
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
20
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| Complexity |
389
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| Defined Atom Stereocenter Count |
0
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| SMILES |
NC1=CC=CC=C1C(=O)/C=C/C1=CC=CC([N+]([O-])=O)=C1
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| InChi Key |
LRMPAVQDWGDIBD-CMDGGOBGSA-N
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| InChi Code |
InChI=1S/C15H12N2O3/c16-14-7-2-1-6-13(14)15(18)9-8-11-4-3-5-12(10-11)17(19)20/h1-10H,16H2/b9-8+
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| Chemical Name |
(E)-1-(2-aminophenyl)-3-(3-nitrophenyl)prop-2-en-1-one
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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 |
| 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) |
DMSO: 50 mg/mL (186.38 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 | 3.7276 mL | 18.6379 mL | 37.2759 mL | |
| 5 mM | 0.7455 mL | 3.7276 mL | 7.4552 mL | |
| 10 mM | 0.3728 mL | 1.8638 mL | 3.7276 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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