2. PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK JAK/STAT Signaling Cell Cycle/DNA Damage Stem Cell/Wnt Apoptosis
  3. MELK DYRK Pim mTOR CDK GSK-3 RIP kinase
  4. HTH-01-091

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。

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HTH-01-091 Chemical Structure

HTH-01-091 Chemical Structure

CAS No. : 2000209-42-5

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HTH-01-091 相关抗体

Top Publications Citing Use of Products

查看 DYRK 亚型特异性产品:

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DYRK1 DYRK2 DYRK4

查看 mTOR 亚型特异性产品:

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mTOR mTORC1 mTORC2

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

查看 GSK-3 亚型特异性产品:

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GSK-3 GSK-3α GSK-3β

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HTH-01-091 is a potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor, with an IC50 of 10.5 nM. HTH-01-091 also inhibits PIM1/2/3, RIPK2, DYRK3, smMLCK and CLK2. HTH-01-091 can be uesd for breast cancer research[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HTH-01-091 相关抗体:

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 IC50 values 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
性状

固体

颜色

White to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
纯度 & 产品资料
参考文献

HTH-01-091 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

HTH-01-0912000209-42-5MELKDYRKPimmTORCDKGSK-3RIP kinaseMaternal embryonic leucine zipper kinaseDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinasePim kinasesMammalian target of RapamycinCyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Receptor-interacting protein kinasesRIPKMDA-MB-468BT-549HCC70ZR-75-1MCF7T-47D cellsbreast cancerGSK3AsmMLCKInhibitorinhibitorinhibit

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目录号：
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