OTSSP167 hydrochloride

SKU: orb1306298

Description

OTSSP167 hydrochloride is a potent and selective MELK inhibitor with an IC50 of 0.41 nM. It is a valuable chemical probe for studying MELK's role in cancer cell proliferation and has been utilized in both in vitro and in vivo oncology research models.

Research Area

Signal Transduction

Key Properties

• CAS Number: 1431698-10-0
• MW: 523.88
• Purity: 99.97%
• Formula: C₂₅H₂₉Cl₃N₄O₂
• SMILES: Cl.CN(C)C[C@H]1CC[C@@H](CC1)Nc1c(cnc2ccc(nc12)-c1cc(Cl)c(O)c(Cl)c1)C(C)=O
• Target: MELK
• Solubility: H2O:7.14 mg/mL (13.63 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (4.77 mM);DMSO:33 mg/mL (62.99 mM)

Bioactivity

• Target IC50:
  MELK:0.41 nM (IC50)
• In Vitro:
  OTSSP167 is a highly potent MELK inhibitor with IC of 0.41 nM. OTSSP167 inhibited the phosphorylation of PSMA1 (proteasome subunit alpha type 1) and DBNL (drebrin-like), which we identified as novel MELK substrates and are important for stem-cell characteristics and invasiveness. The compound suppressed mammosphere formation of breast cancer cells and exhibited significant tumor growth suppression in xenograft studies using breast, lung, prostate, and pancreas cancer cell lines in mice by both intravenous and oral administration. This MELK inhibitor should be a promising compound possibly to suppress the growth of tumor-initiating cells and be applied for treatment of a wide range of human cancer.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, MELK, Maternal embryonic leucine zipper kinase, inhibit, OTS167, OTS-167, OTS 167, OTSSP 167, OTSSP 167 Hydrochloride, OTSSP167, OTSSP-167, OTSSP167 Hydrochloride, OTSSP167 hydrochloride, OTSSP-167 Hydrochloride, OTSSP-167 hydrochloride

Compound Identifiers

PubChem CID

135565272