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编 号:F749977
分子式:C22H33Cl2N5
分子量:438.44
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3,6-DMAD dihydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD dihydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD dihydrochloride can be used for research of cancer.

体内研究:
3,6-DMAD dihydrochloride (10 mg/kg; i.p.; three times every 12 hours, for 84 hours; NOD Scid mice with RPMI 8226 xenograft) has inhibition of XBP1 splicing in vivo.3,6-DMAD dihydrochloride (10 mg/kg; 24 h; i.p.; every 48 hours, for 12 days; NOD Scid mice with RPMI 8226 xenograft) suppresses multiple myeloma xenograft growth in vivo.Animal Model:NOD Scid mice (4-6 weeks) with RPMI 8226 xenograft
Dosage:10 mg/kg
Administration:Intraperitoneal injection; three times every 12 hours, for 84 hours
Result:Inhibited XBP1-luciferase activity in NOD Scid mice with RPMI 8226 xenograft.
Animal Model:NOD Scid mice (4-6 weeks) with RPMI 8226 xenograft
Dosage:10 mg/kg
Administration:Intraperitoneal injection; every 48 hours, for 12 days
Result:Inhibited tumor growth in NOD Scid mice with RPMI 8226 xenograft.

体外研究:
3,6-DMAD dihydrochloride (0-6 μM; 24 h; RPMI 8226 and MM1.R human MM cells) has cytotoxicity against MM cell lines.3,6-DMAD dihydrochloride (0-30 μM; 14 h; HT1080 cells treated with Tg (0.3 μM)) inhibits XBP1 splicing (XBP1s) in a dose dependent manner.3,6-DMAD dihydrochloride (0.1-500 μM; 14 h; HT1080 cells treated with Tg (0.3 μM)) inhibits IRE1α endonuclease activity.3,6-DMAD dihydrochloride (1-60 μM; 2 h; HEK293 cells) inhibits IRE1α oligomerization and IRE1α-GFP foci formation.
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