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Alternative_name
4-[7-acetyl-8-[[4-[(dimethylamino)methyl]cyclohexyl]amino]-1H-1,5-naphthyridin-2-ylidene]-2,6-dichlorocyclohexa-2,5-dien-1-one; OTS167
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Description
OTSSP167 is an inhibitor (IC₅₀ = 0.41 nM) of maternal embryonic leucine zipper kinase (MELK) with potential antineoplastic activity. OTSSP167 binds to MELK, which prevents both MELK phosphorylation and activation, thus inhibiting the phosphorylation of downstream MELK substrates. This may lead to an inhibition of both cell proliferation and survival in MELK-expressing tumor cells. MELK, a serine/threonine kinase, is involved in cancer cell survival, invasiveness and cancer-stem cell formation and maintenance; it is highly upregulated in various types of cancer cells and absent in normal, healthy cells.
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CAS Number
1431697-89-0
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Structure Available
Yes
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Salt Form
No
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Molecular Formula
C₂₅H₂₈Cl₂N₄O₂
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Molecular Weight
487.42
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Cell Permeable
Yes
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Purity
≥98% by HPLC
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Solubilities
DMSO (>20 mg/ml)
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Handling
Protect from air and light
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Tag Line
A maternal embryonic leucine zipper kinase (MELK) inhibitor
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Storage Condition
-20°C
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Shipping Condition
gel pack
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Shelf Life
36 months
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PubChem CID
71543332
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SMILES
CC(=O)C1=CN=C2C=CC(=C3C=C(C(=O)C(=C3)Cl)Cl)NC2=C1NC4CCC(CC4)CN(C)C
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InChi
InChI=1S/C25H28Cl2N4O2/c1-14(32)18-12-28-22-9-8-21(16-10-19(26)25(33)20(27)11-16)30-24(22)23(18)29-17-6-4-15(5-7-17)13-31(2)3/h8-12,15,17,30H,4-7,13H2,1-3H3,(H,28,29)
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InChi Key
WZJUACDPTWDYSI-UHFFFAOYSA-N
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MSDS Available
Yes
