- Cat. No.
- A12851
OTSSP167
OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.
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MELK inhibitors block maternal embryonic leucine zipper kinase, a kinase studied in cell division. Maternal embryonic leucine zipper kinase (MELK) was described in 1997 as a new member of the adenosine monophosphate-activated protein kinase (AMPK) family. It was first found in mouse eggs and preimplantation embryos. OTSSP167 was reported in 2012 as an orally available MELK inhibitor that suppressed the growth of several human cancer cell types. A 2017 gene-editing study found that cancer cell lines lacking MELK grew normally, which questioned the kinase as a cancer dependency. OTSSP167 also inhibits other kinases, so compounds such as MELK-8a and HTH-01-091 help to separate MELK-specific effects. JNJ-47117096 and MELK-IN-1 are further MELK inhibitors listed in this category.
OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM.
MELK-IN-1 is a potent inhibitor of maternal embryonic leucine zipper kinase (MELK) with an IC50 and a Ki of 3 nM and 0.39 nM, respectively.
Synonyms: MELK-T1 hydrochloride; JNJ47117096
JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.
MELK-8a hydrochloride is a novel maternal embryonic leucine zipper kinase (MELK) inhibitor with an IC50 of 2 nM.
OTSSP167 (hydrochloride) is a highly potent MELK inhibitor with IC50 value of 0.41 nM.
HTH-01-091 is a selective inhibitor of maternal embryonic leucine zipper kinase (MELK), exhibiting an IC50 of 10.5 nM. In addition to its primary target, HTH-01-091 also demonstrates inhibitory activity against PIM1/2/3, RIPK2, DYRK3, smMLCK, and CLK2. This compound is valuable for research applications focused on breast cancer and elucidating the role of MELK in tumorigenesis.
JNJ-47117096 is a selective inhibitor of the maternal embryonic leucine zipper kinase (MELK), exhibiting an IC50 of 23 nM. Additionally, it demonstrates significant inhibition of Flt3, with an IC50 of 18 nM. This compound is valuable for research applications focused on cancer biology, particularly in studies investigating cell proliferation and survival pathways associated with MELK and Flt3.
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Synonyms: NVS-MELK8a
MELK-8a is a highly potent and selective inhibitor of maternal embryonic leucine zipper kinase (MELK), demonstrating an IC50 of 2 nM. This compound also inhibits Flt3 (ITD), Haspin, and PDGFRα with IC50 values of 0.18, 0.19, and 0.42 μM, respectively. MELK-8a's primary application lies in cancer research, where MELK is crucial for regulating cell mitosis in specific cancer cell types. This makes MELK-8a a valuable tool for exploring therapeutic strategies targeting MELK-associated pathways in cancer.