HTH-01-091

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HTH-01-091

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CAS NO:

2000209-42-5

HTH-01-091 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 还能抑制PIM1/2/3、RIPK2、DYRK3、smMLCK和CLK2。HTH-01-091 可用于乳腺癌研究。

生物活性

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

IC₅₀& Target

DYRK4

41.8 nM (IC₅₀)

PIM1

60.6 nM (IC₅₀)

mTOR

632 nM (IC₅₀)

CDK7

1230 nM (IC₅₀)

PIM2

PIM3

体外研究
(In Vitro)

HTH-01-091 (1 μM) selectively inhibits 4% of the kinases over 90%^[1].
HTH-01-091 (0-10 μM, 1 h) is cell permeable and causes MELK degradation^[1].
HTH-01-091 (0-10 μM, 3 day) exhibits minor antiproliferative effects in breast cancer cells^[1].

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.

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.

分子量

499.43

Formula

C₂₆H₂₈Cl₂N₄O₂

CAS 号

2000209-42-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.