3,6-DMAD hydrochloride 是一种吖啶衍生物，是一种有效的IRE1α-XBP1s通路抑制剂。 3,6-DMAD hydrochloride 通过 IRE1α-XBP1s 通路促进 IL-6 分泌。3,6-DMAD hydrochloride 可抑制 IRE1α 寡聚化和核糖核酸内切酶 (RNase) 活性。3,6-DMAD hydrochloride 可用于癌症的研究。
| 生物活性 | 3,6-DMAD hydrochloride, an acridine derivative, is a potentIRE1α-XBP1spathway inhibitor. 3,6-DMAD hydrochloride promotesIL-6secretion via the IRE1α-XBP1s pathway. 3,6-DMAD hydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD hydrochloride can be used for research ofcancer[1][2]. |
体外研究
(In Vitro) | 3,6-DMAD hydrochloride (0-6 μM; 24 h; RPMI 8226 and MM1.R human MM cells) has cytotoxicity against MM cell lines[1].
3,6-DMAD hydrochloride (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 hydrochloride (0.1-500 μM; 14 h; HT1080 cells treated with Tg (0.3 μM)) inhibits IRE1α endonuclease activity[1].
3,6-DMAD hydrochloride (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. |
Western Blot Analysis[1] | Cell Line: | HT1080 cells treated with Tg (0.3 μM) | | Concentration: | 0, 5, 10 and 30 μM | | Incubation Time: | 14 hours | | Result: | Showed XBP1s inhibition at as low as 0.5 μM. |
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体内研究
(In Vivo) | 3,6-DMAD hydrochloride (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 hydrochloride (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. |
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| 性状 | |
| Formula | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(Need ultrasonic) |
