| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| ln Vitro |
Treatment with (-)-DHMEQ (Dehydroxymethylepoxyquinomicin; 2–10 μg/mL; 12-48 hours) dramatically lowers all cell lines' survival in a time- and dose-dependent manner; however, the impact is not statistically significant in the control cell line K562, which lacks constitutive NF-κB activity[2]. In MT-1 and TL-Om1 cell lines, (-)-DHMEQ (10 μg/mL; 0-48 hours; TL-Om1, MT-1, and K562 cells) treatment dramatically increases the Annexin V-positive cells[2]. Under (-)-DHMEQ (10 μg/mL; 4–16 hours; MT-1 cells) treatment, proapoptotic genes such caspase-3, -8, and-9 are up-regulated and Bcl-xL, Bcl-2, c-myc, cyclin D1, Rb, and p53 are down-regulated.Reference [2]. Treatment with (-)-DHMEQ results in a time-dependent increase in cells in the G0 /G1 phase, indicating (-)-DHMEQ's antiproliferative properties[2]. At particular cysteine residues, (-)-DHMEQ binds to p65, cRel, RelB, and p50 but not p52. RelB's DNA binding and interaction with importin are both inhibited by (-)-DHMEQ. RelB becomes unstable as well due to (-)-DHMEQ[1].
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|---|---|
| ln Vivo |
The intraperitoneal injection of (-)-DHMEQ (4 mg/kg or 12 mg/kg) given to SCID mice on day 0 and three times a week for a month significantly increases the mice's survival rate[2].
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: TL-Om1, MT-1, KK-1, ST-1 and K562 cells Tested Concentrations: 2 μg/mL, 5 μg/mL, 10 μg/mL Incubation Duration: 12 hrs (hours), 24 hrs (hours), 48 hrs (hours) Experimental Results: Dramatically decreased the viability of all cell lines in a dose- and time- dependent manner. Apoptosis Analysis[2] Cell Types: TL-Om1, MT-1 and K562 cells Tested Concentrations: 10 μg/mL Incubation Duration: 0 hrs (hours), 24 hrs (hours), 48 hrs (hours) Experimental Results: Annexin V-positive cells were Dramatically increased after 24 to 48 hrs (hours). Western Blot Analysis[2] Cell Types: MT-1 cells Tested Concentrations: 10 μg/mL Incubation Duration: 4 hrs (hours), 8 hrs (hours), 16 hrs (hours) Experimental Results: Annexin V-positive cells were Dramatically increased after 24 to 48 hrs (hours). |
| Animal Protocol |
Animal/Disease Models: Male C.B17-scid/scid (5 weeks old) mice injected with MT-2 cells[2]
Doses: 4 mg/kg or 12 mg/kg Route of Administration: intraperitoneal (ip)injection; on day 0 and 3 times a week ; for one month Experimental Results: demonstrated a significant increase in the survival rate in mice. |
| References |
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| Molecular Formula |
C13H11NO5
|
|---|---|
| Molecular Weight |
261.2301
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| Exact Mass |
261.064
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| CAS # |
287194-40-5
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| Related CAS # |
(+)-DHMEQ; 287194-41-6; DHMEQ racemate; 287194-38-1
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| PubChem CID |
9881652
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| Appearance |
Off-white to gray solid powder
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| LogP |
0.291
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
19
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| Complexity |
446
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| Defined Atom Stereocenter Count |
3
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| SMILES |
C1=CC=C(C(=C1)C(=O)NC2=CC(=O)[C@@H]3[C@H]([C@H]2O)O3)O
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| InChi Key |
IUOMATKBBPCLFR-TUAOUCFPSA-N
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| InChi Code |
InChI=1S/C13H11NO5/c15-8-4-2-1-3-6(8)13(18)14-7-5-9(16)11-12(19-11)10(7)17/h1-5,10-12,15,17H,(H,14,18)/t10-,11+,12-/m0/s1
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| Chemical Name |
2-Hydroxy-N-[(1S,2S,6S)-2-hydroxy-5-oxo-7-oxabicyclo[4.1.0]hept-3-en-3-yl]benzamide
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| Synonyms |
DHMEQ Dehydroxymethylepoxyquinomicin
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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 (e.g. under nitrogen), 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) |
DMSO : ~95 mg/mL (~363.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (19.14 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8280 mL | 19.1402 mL | 38.2804 mL | |
| 5 mM | 0.7656 mL | 3.8280 mL | 7.6561 mL | |
| 10 mM | 0.3828 mL | 1.9140 mL | 3.8280 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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