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1883545-52-5

中文名稱 1883545-52-5
英文名稱 MM-102 (trifluoroacetate)
CAS 1883545-52-5
分子式 C37H50F5N7O6
分子量 783.828
MOL 文件 1883545-52-5.mol
更新日期 2024/11/15 18:20:31
1883545-52-5 結(jié)構(gòu)式 1883545-52-5 結(jié)構(gòu)式

基本信息

中文別名
化合物MM-102 TFA
英文別名
MM-102 (TFA)
MM-102 (trifluoroacetate)
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

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度DMSO: ≥ 100 mg/mL (127.58 mM)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
1883545-52-5價格(試劑級)
報(bào)價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
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
2024/11/08HY-12220A1883545-52-5
MM-102 TFA
1883545-52-510mM * 1mLin DMSO2173元

常見問題列表

生物活性
MM-102 TFA (HMTase Inhibitor IX TFA) 是一種有效的 WDR5/MLL 相互作用抑制劑, WDR5 結(jié)合檢測中, IC50 =2.4 nM, Ki< 1 nM。
靶點(diǎn)

IC50: 2.4 nM (MLL).

體外研究

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.

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