3,6-DMAD dihydrochloride 是一种吖啶衍生物，是一种有效的IRE1α-XBP1s通路抑制剂。 3,6-DMAD dihydrochloride 通过 IRE1α-XBP1s 通路促进 IL-6 分泌。3,6-DMAD dihydrochloride 可抑制 IRE1α 寡聚化和核糖核酸内切酶 (RNase) 活性。3,6-DMAD dihydrochloride 可用于癌症的研究。

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 [1] [2].

3,6-DMAD dihydrochloride (0-6 μM; 24 h; RPMI 8226 and MM1.R human MM cells) has cytotoxicity against MM cell lines [1]. 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 [1]. 3,6-DMAD dihydrochloride (0.1-500 μM; 14 h; HT1080 cells treated with Tg (0.3 μM)) inhibits IRE1α endonuclease activity [1]. 3,6-DMAD dihydrochloride (1-60 μM; 2 h; HEK293 cells) inhibits IRE1α oligomerization and IRE1α-GFP foci formation [1]. Cell Viability Assay [1] 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 [1] 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.

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 [1]. 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 [1]. Animal Model: NOD Scid mice (4-6 weeks) with RPMI 8226 xenograft [1] 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 [1] 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.

2226511-77-7

C22H33Cl2N5

438.44

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years