OTSSP167 | B1065

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.

B1065 | OTSSP167 DataSheet

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