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.
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.
Alternate Name/Synonyms: 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
Formulation: N/A
CAS Number: 1431697-89-0
Structure Available?: Yes
Peptide sequence: N/A
Salt Form: No
Molecular Formula: C₂₅H₂₈Cl₂N₄O₂
Molecular Weight: 487.42
Cell-Permeable?: Yes
Purity: ≥98% by HPLC
Solubilities: DMSO (>20 mg/ml)
Handling: Protect from air and light
Country of Origin: USA
Tag Line: A maternal embryonic leucine zipper kinase (MELK) inhibitor
MDL Number: N/A
PubChem CID: 71543332
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
Additional Information
Storage Condition: |
-20°C |
Shipping Condition: |
Gel Pack |
Shelf Life: |
36 months |