3,6-DMAD hydrochloride |
| Catalog No.GC34384 |
El clorhidrato de 3,6-DMAD, un derivado de la acridina, es un potente inhibidor de la vÍa IRE1α-XBP1s. El clorhidrato de 3,6-DMAD promueve la secreciÓn de IL-6 a través de la vÍa IRE1α-XBP1s. El clorhidrato de 3,6-DMAD inhibe la oligomerizaciÓn de IRE1α y la actividad de la endorribonucleasa (RNasa). El clorhidrato de 3,6-DMAD se puede utilizar para la investigaciÓn del cÁncer.
Products are for research use only. Not for human use. We do not sell to patients.
Sample solution is provided at 25 µL, 10mM.
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3,6-DMAD hydrochloride is a inhibitor of the IRE1α-XBP1 pathway of the unfolded protein response.
3,6-DMAD inhibits both IRE1α oligomerization and in vitro endoribonuclease (RNase) activity[1].
Following three intraperitoneal administrations of 3,6-DMAD at a dose of 10 mg/kg every 12 hours, 3,6-DMAD significantly inhibits in vivo XBP1-luciferase activity assessed 3.5 days after the initial treatment. 3,6-DMAD-treatment significantly inhibits tumor xenograft growth[1].
[1]. Jiang D, et al. Acridine Derivatives as Inhibitors of the IRE1α-XBP1 Pathway Are Cytotoxic to Human Multiple Myeloma. Mol Cancer Ther. 2016 Sep;15(9):2055-65.
Kinase experiment: | IRE1α oligomerization assay is set up using the nuclease reaction buffer, 2 μM recombinant hIRE1α, 2 mM ADP, and 60 μM of 3,6-DMAD. All reactions are performed in 20 μL with 10% DMSO to account for vehicle and incubated for 15 min at 30 °C to allow for oligomerization. The optical density of the sample is measured at 500 nm using a NanoDrop 2000[1]. |
Cell experiment: | 2×104 cells per well are plated into 96-well plates and treatment started 0-12 hours after plating. RPMI 8226 and MM1.R human MM cells are treated with 0-6 μM 3,6-DMAD. After 24 hours of treatment, XTT reagent (ATCC) is added to the wells then cells are incubated for 2 hours and absorbance measured at both 475 nM and 660 nM using a BioTek Synergy H1 plate reader.[1]. |
Animal experiment: | Rats[1]5×106RPMI 8226 cells are implanted subcutaneously into the flanks of 4-6 weeks’ old NOD Scid mice. Drug treatment started when the sizes of the tumors reach 150 mm3. Four tumor-bearing mice per group are treated with 10 mg/kg 3,6-DMAD or vehicle (saline) intraperitoneally once every 2 days. Tumor volume is measured[1]. |
References: [1]. Jiang D, et al. Acridine Derivatives as Inhibitors of the IRE1α-XBP1 Pathway Are Cytotoxic to Human Multiple Myeloma. Mol Cancer Ther. 2016 Sep;15(9):2055-65. | |
| Cas No. | SDF | ||
| Canonical SMILES | CN(C1=CC=C2C(N=C3C=C(C=CC3=C2NCCCN(C)C)N(C)C)=C1)C.[x HCl] | ||
| Formula | C22H31N5 xHCl | M.Wt | 365.52 |
| Solubility | DMSO : 25 mg/mL (68.40 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.7358 mL | 13.6791 mL | 27.3583 mL |
| 5 mM | 0.5472 mL | 2.7358 mL | 5.4717 mL |
| 10 mM | 0.2736 mL | 1.3679 mL | 2.7358 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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