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3,6-DMAD hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
3,6-DMAD hydrochloride图片
包装:5mg
规格:98%
市场价:3148元
分子量:365.52

产品介绍
3,6-DMADhydrochloride是未折叠蛋白质应答(IRE1α-XBP1)通路的抑制剂。
货号:ajcx13476
CAS:N/A
分子式:C22H31N5 xHCl
分子量:365.52
溶解度:DMSO : 25 mg/mL (68.40 mM)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

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.

Protocol:

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].

参考文献:

[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.