1883545-52-5

1883545-52-5

中文名称1883545-52-5
中文同义词化合物MM-102 TFA;MM-102 TFA,WDR5 / MLL相互作用抑制剂;(S)-N-(双(4-氟苯基)甲基)-1-(2-(2-乙基-2-异丁酰氨基丁酰氨基)-5-胍基戊酰氨基)环戊烷-1-甲酰胺 2,2,2-三氟乙酸盐
英文名称MM-102 (trifluoroacetate)
英文同义词MM-102 (trifluoroacetate);MM-102 (TFA);HMTASE INHIBITOR IX (TFA);1-[[(2S)-5-[(Aminoiminomethyl)amino]-2-[[2-ethyl-2-[(2-methyl-1-oxopropyl)amino]-1-oxobutyl]amino]-1-oxopentyl]amino]-N-[bis(4-fluorophenyl)methyl]-cyclopentanecarboxamide trifluoroacetate;MM102,HMTase Inhibitor IX,MM-102,MM 102 TFA,MM 102,inhibit,MM102 TFA,Histone Methyltransferase,Inhibitor;(S)-N-(Bis(4-fluorophenyl)methyl)-1-(2-(2-ethyl-2-isobutyramidobutanamido)-5-guanidinopentanamido)cyclopentane-1-carboxamide 2,2,2-trifluoroacetate
CAS号1883545-52-5
分子式C37H50F5N7O6
分子量783.84
EINECS号
相关类别
Mol文件1883545-52-5.mol
结构式1883545-52-5 结构式

1883545-52-5 性质

储存条件Store at -20°C
溶解度二甲基亚砜:≥100mg/mL(127.58mM)
形态固体
颜色白色至米白色

1883545-52-5 用途与合成方法

MM-102 TFA (HMTase Inhibitor IX TFA) 是一种有效的 WDR5/MLL 相互作用抑制剂, WDR5 结合检测中, IC50 =2.4 nM, Ki< 1 nM。

IC50: 2.4 nM (MLL).

MM-102 (HMTase Inhibitor IX) inhibits MLL1 methyltransferase activity and MLL-1-induced HoxA9 and Meis-1 gene expression in leukemia cells expressing the MLL1-AF9 fusion gene. Also inhibits cell growth and induces apoptosis in leukemia cells harbouring MLL1 fusion proteins. MM-102 (TFA), with the highest binding affinities to WDR5, also show the most potent inhibitory activity in the HMT assay withIC 50 =0.4-0.9 μM. MM-102 (HMTase Inhibitor IX) dose-dependently inhibits cell growth in the MV4;11 and KOPN8 leukemia cell lines, which carry MLL1-AF4 and MLL1-ENL fusion proteins, respectively. MM-102 (HMTase Inhibitor IX) has IC 50 =25 μM in both cell lines and completely inhibits cell growth in these cell lines at 75 μM. MM-102 (HMTase Inhibitor IX) effectively and selectively inhibits cell growth and induces apoptosis in leukemia cells harboring MLL1 fusion proteins and has minimal effect in leukemia cells with wild-type MLL1 protein.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/11/08HY-12220A1883545-52-5
MM-102 TFA
1883545-52-52mg698元
2024/11/08HY-12220A1883545-52-5
MM-102 TFA
1883545-52-55 mg1463元

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