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.
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.
Cell Viability Assay
Cell Line:
RPMI 8226 and MM1.R human MM cells
Concentration:
0, 0.5, 1, 2, 3, 4, 5 and 6 μM
Incubation Time:
24 hours
Result:
Inhibited cell survival rate in a dose dependent manner.
Cell Viability Assay
Cell Line:
0, 5, 10 and 30 μM
Concentration:
0, 0.5, 1, 2, 3, 4, 5 and 6 μM24 hours
Incubation Time:
14 hours
Result:
Showed XBP1s inhibition at as low as 0.5 μM.
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.
分子式
C22H33Cl2N5
分子量
438.44
CAS号
2226511-77-7
运输条件
Room temperature in continental US; may vary elsewhere.