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HTH-01-091 TFA
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
HTH-01-091 TFA图片
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
HTH-01-091 TFA 是一种强效且选择性的maternal embryonic leucine zipper kinase (MELK)抑制剂，其IC50为 10.5 nM。HTH-01-091 TFA 还能抑制PIM1/2/3、RIPK2、DYRK3、smMLCK和CLK2。HTH-01-091 TFA 可用于乳腺癌研究。
生物活性

HTH-01-091 TFA is a potent and selectivematernal embryonic leucine zipper kinase (MELK)inhibitor, with anIC50of 10.5 nM. HTH-01-091 TFA also inhibitsPIM1/2/3,RIPK2,DYRK3,smMLCKandCLK2. HTH-01-091 TFA can be uesd for breastcancerresearch[1].

IC50& Target

IC50: 10.5 nM (MELK), 41.8 nM (DYRK3), 42.5 nM (RIPK2), 60.6 nM (PIM1), 108.6 nM (smMLCK), 632 nM (mTOR), 962 nM (PIK3CA), 1230 nM (CDK7), 1740 nM (GSK3A)[1]

体外研究
(In Vitro)

HTH-01-091 (1 μM) TFA 选择性抑制 4% 的激酶超过 90%[1]。
HTH-01-091 (0-10 μM, 1 h) TFA 具有细胞渗透性并导致 MELK 降解[1]。
HTH-01-091（0-10 μM，3 天）TFA 在乳腺癌细胞中表现出轻微的抗增殖作用[1]。

Cell Proliferation Assay[1]

Cell Line:MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells
Concentration:0, 0.001, 0.01, 0.1, 1.0, and 10 μM
Incubation Time:3 day
Result:Showed antiproliferative activities in a panel of breast cancer cell lines, including MDA-MB-468, BT-549, HCC70, ZR-75-1, MCF7, and T-47D cells, with IC50values of 4.00 μM, 6.16 μM, 8.80 μM, >10 μM, 8.75 μM, and 3.87 μM, respectively.

Western Blot Analysis[1]

Cell Line:MDA-MB-468 cells
Concentration:0, 0.1, 1.0, and 10 μM
Incubation Time:1 h
Result:Reduced MELK protein levels in MDA-MB-468 cells; Dose-dependently decreased MELK pull-down by streptavidin beads, demonstrating that the compound is cell permeable and binds to MELK in an ATP-competitive fashion. Had no effect on ERK1/2 pull-down, showing no binding affinity of HTH-01-091 to ERK1/2.
分子量

613.46

性状

Solid

Formula

C28H29Cl2F3N4O4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month