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OTSSP167

A maternal embryonic leucine zipper kinase (MELK) inhibitor
Catalog #: B1065
SKU-Size Size Price Qty
B1065-5 5 mg
$165.00
B1065-25 25 mg
$625.00
More Sizes Get Quote

Product Details

Alternate 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
Appearance Off-white solid
CAS # 1431697-89-0
Molecular Formula C₂₅H₂₈Cl₂N₄O₂
Molecular Weight 487.42
Purity ≥98% by HPLC
Solubility DMSO (>20 mg/ml)
SMILES CC(=O)C1=CN=C2C=CC(=C3C=C(C(=O)C(=C3)Cl)Cl)NC2=C1NC4CCC(CC4)CN(C)C
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)
InChi Key WZJUACDPTWDYSI-UHFFFAOYSA-N
PubChem CID 71543332
Handling Protect from air and light
Storage Conditions -20°C
Shipping Conditions Gel Pack
USAGE For Research Use Only! Not For Use in Humans.

Details

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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