| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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NBDHEX is a novel and potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor with anticancer activity by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors.
| ln Vitro |
Lung cancer H69 and H69AR cells respond cytotoxically to NBDHEX (0.05–20 μM; 48 hours) [2]. H69AR cell lines treated with NBDHEX (0-5 μM; 24 hours) show screening questionnaire findings. Phosphorylation of JNK/c-Jun in H69AR cells is increased by NBDHEX (3 μM; 1–12 hours) treatment. Dependence on time [2]. Following NBDHEX therapy, p38MAPK phosphorylation rose noticeably.
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| ln Vivo |
Treatment with NBDHEX (0.8–80 mg/kg/day; baseline disclosure; daily; for 15 days; SCID female mice) produced a statistically significant (70%–80%) reduction in tumors [2].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: H69 and H69AR cells Tested Concentrations: 0.05-20 μM Incubation Duration: 48 hrs (hours) Experimental Results: The dose response curve demonstrated good, and the GSSG content in H69 cells also increased with the addition of Time changes[2]. It has cytotoxic activity in both the sensitive H69 cell line (LC50 is 2.3 μM) and the doxorubicin-resistant cell line H69AR (LC50 is 4.5 μM). Apoptosis analysis [2] Cell Types: H69AR Cell Tested Concentrations: 0 μM, 0.5 μM, 1 μM, 2 μM, 3 μM, 4 μM, 5 μM Incubation Duration: 24 hrs (hours) Experimental Results: Caused dose-dependent apoptosis of H69AR cells Wire. Western Blot Analysis [2] Cell Types: H69AR cells Tested Concentrations: 3 μM Incubation Duration: 1 hour, 3 hrs (hours), 6 hrs (hours), 12 hrs (hours) Experimental Results: The phosphorylation of JNK/c-Jun in H69AR cells increased in a time-dependent manner. |
| Animal Protocol |
Animal/Disease Models: SCID female mice (4-5 weeks) are injected with Me501 cells [3]
Doses: 0.8 mg/kg/day, 8.0 mg/kg/day or 80 mg/kg/day Route of Administration: po (po (oral gavage)) daily; Results lasting 15 days: Statistically significant tumor inhibition (approximately 70%) was observed. |
| References |
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| Molecular Formula |
C12H15N3O4S
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|---|---|
| Molecular Weight |
297.33
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| Exact Mass |
297.078
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| CAS # |
787634-60-0
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| PubChem CID |
9817686
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.31 g/cm3
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| LogP |
2.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
20
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| Complexity |
316
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RGXYYAZGELLKDA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H15N3O4S/c16-7-3-1-2-4-8-20-10-6-5-9(15(17)18)11-12(10)14-19-13-11/h5-6,16H,1-4,7-8H2
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| Chemical Name |
6-[(7-nitro-2,1,3-benzoxadiazol-4-yl)sulfanyl]hexan-1-ol
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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 : ~125 mg/mL (~420.41 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3633 mL | 16.8163 mL | 33.6327 mL | |
| 5 mM | 0.6727 mL | 3.3633 mL | 6.7265 mL | |
| 10 mM | 0.3363 mL | 1.6816 mL | 3.3633 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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