1. Cell Cycle/DNA Damage
  2. IRE1
  3. 3,6-DMAD hydrochloride

3,6-DMAD hydrochloride 

Cat. No.: HY-U00460 Purity: ≥98.0%
Handling Instructions

3,6-DMAD hydrochloride is a inhibitor of the IRE1α-XBP1 pathway of the unfolded protein response.

For research use only. We do not sell to patients.

3,6-DMAD hydrochloride Chemical Structure

3,6-DMAD hydrochloride Chemical Structure

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Description

3,6-DMAD hydrochloride is a inhibitor of the IRE1α-XBP1 pathway of the unfolded protein response.

IC50 & Target

IRE1α[1]

In Vitro

3,6-DMAD inhibits both IRE1α oligomerization and in vitro endoribonuclease (RNase) activity[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Formula

C₂₂H₃₁N₅.XHCl

SMILES

CN(C1=CC=C2C(N=C3C=C(C=CC3=C2NCCCN(C)C)N(C)C)=C1)C.[x HCl]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (Need ultrasonic)

References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: ≥98.0%

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Keywords:

3,6-DMADIRE1Inositol requiring enzyme 1Inhibitorinhibitorinhibit

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3,6-DMAD hydrochloride
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