miR544-IN-1

Research use only, not for human use.

miR544-IN-1 (SID 3712249) is a selective small molecule inhibitor of miR-544 biogenesis.

miR544-IN-1 (SID 3712249) is a selective small molecule inhibitor of miR-544 biogenesis; selectively inhibits production of the mature microRNA, sensitizes cells to 5-fluorouracil, and derepresses mRNAs affected by miR-544 in cellulo and in vivo, including boosting mTOR expression; reverses a tumor cell's physiological response to hypoxia.

SID 3712249 (compound 1, 20 nM, 48 h) disrupts miR-544-mediated inhibition of BMI1 based on significant increases in the RFP/BFP ratio.SID 3712249 (20 nM, 48 h) inhibits precursor but not mature miR-544 binding to BMI1 or mTOR3’-UTR.SID 3712249 (20 nM, 48 h) results in accumulation of pre-miR-544 and a decrease in miR-544 levels in MCF10A cells.SID 3712249 (20 nM, 5 days) induces apoptosis in MDA-MB-231 and MCF- 7 cells and has no effect on cell survival in normoxic conditions.Apoptosis Analysis Cell Line:MDA-MB-231, MCF-7 cells Concentration:20 nM Incubation Time:5 days Result:Induced apoptosis and has no effect on cell survival in normoxic conditions (flow cytometric analysis of Annexin V and PI stainning).

SID 3712249 (compound 1, 100 μL of 40 μM, intraperitoneal injection) inhibited tumor growth in MDA-MB-231-GFP-luc tumor model.SID 3712249 (20 nM, pre-treated GFP-labeled MDA-MB-231 cells, intraperitoneal injection) inhibited tumor growth in MDA-MB-231-GFP-luc tumor model. Animal Model:MDA-MB-231-GFP-luc tumor model Dosage:100 μL of 40 μM Administration:Intraperitoneal injection Result:Inhibited tumor growth (evidenced by live animal bioluminescent imaging) with no overt side effects.Decreased levels of miR-544, ATM, and HIF-1α and increased levels of mTOR (resected tumor samples).

SID 3712249

Chromatin/Epigenetic

MicroRNA

MicroRNA

Cancer

——

522606-67-3

323.404

C17H21N7

>98% (HPLC)

DMSO : ≥ 30 mg/mL 92.76 mM

N#CC1=C(N2CCCC2)N=C(N)C3=C1C=C(N4CCCC4)N=C3N

1,8-diamino-3,6-di(pyrrolidin-1-yl)-2,7-naphthyridine-4-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years