HLCL-61 is a potent and selective PRMT5 inhibitor for treatment of acute myeloid leukemia. HLCL-61 resulted in significantly increased expression of miR-29b and consequent suppression of Sp1 and FLT3 in AML (acute myeloid leukemia) cells. As a result, significant antileukemic activity was achieved. The increased PRMT5 activity enhanced AML growth in vitro and in vivo while PRMT5 downregulation reduced it. In AML cells, PRMT5 interacted with Sp1 in a transcription repressor complex and silenced miR-29b preferentially via dimethylation of histone 4 arginine residue H4R3.
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化学信息
名称 | HLCL-61 |
Iupac 化学名称 | 1-(9-ethyl-9H-carbazol-3-yl)-N-(2-methoxybenzyl)methanamine hydrochloride |
同义词 | HLCL 61; HLCL-61. |
英文同义词 | HLCL 61; HLCL-61. |
分子式 | C23H25ClN2O |
分子量 | 380.916 |
Smile | Cl.C(C)N1C2=CC=CC=C2C=2C=C(C=CC12)CNCC1=C(C=CC=C1)OC |
InChiKey | XYAVCNMZZKTEGR-UHFFFAOYSA-N |
InChi | InChI=1S/C23H24N2O.ClH/c1-3-25-21-10-6-5-9-19(21)20-14-17(12-13-22(20)25)15-24-16-18-8-4-7-11-23(18)26-2;/h4-14,24H,3,15-16H2,1-2H3;1H |
Cas号 | 586395-74-6 |
相关CAS号 | |
外观性状 | Solid powder |
纯度 | 98% by HPLC |
存储 | -20 ºC for 3 years |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |