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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-ZLD115
ZLD115

Chemical Structure : ZLD115

CAS No.: 2980653-93-6

ZLD115 (ZLD-115)

货号: PC-23648Not For Human Use, Lab Use Only.

ZLD115 is a potent, selective inhibitor of fat mass and obesity-associated protein (FTO) with IC50 of 2.3 uM in PAGE-based assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ZLD115 is a potent, selective inhibitor of fat mass and obesity-associated protein (FTO) with IC50 of 2.3 uM in PAGE-based assays.
ZLD115 inhibitsFTO demethylase by more than 70% at a concentration of 20 μM, does not inhibit the in vitro demethylation activity of ALKBH3 and ALKBH5 even at a concentration of 200 μM.
ZLD115 exhibits antiproliferative activity in leukemia cell lines MOLM13 and NB4 with IC50 of 1.7 μM and 1.5 μM respectively.
ZLD115 exhibits considerable antiproliferative effects on leukemia cell lines, such as HEL, KG-1, MV-4-11, and THP-1 cell lines, in addition to MOLM13 and NB4 AML cell lines, with IC50 values of 10.3 ± 0.6, 4.1 ± 0.5, 3.4 ± 0.1, and 6.0 ± 1.8 μM, respectively.
ZLD115 (5-10 uM) results in RARA upregulation and MYC downregulation, increases the RARA protein levels in the MOLM13 cells but decreases the abundance of MYC protein.
ZLD115 (40 mg/kg) inhibits leukemia progressionxenograft mouse model by subcutaneously inoculating MV-4-11 cells into female BALB/c nude mice.

物理化学性质&存储条件

分子量 496.00
分子式 C27H30ClN3O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Benzoic acid, 2-[[2-chloro-6-cyclopropyl-4-(3,5-dimethyl-4-isoxazolyl)phenyl]amino]-6-[(tetrahydro-1,4-oxazepin-4(5H)-yl)methyl]-

参考文献

1. Xiao P, et al. J Med Chem. 2023 Jul 27;66(14):9731-9752.

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