K145 hydrochloride

SKU: orb1940042

Description

K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 μM and Ki of 6.4 μM. K145 hydrochloride can induce apoptosis and has strong antitumor activity.(In Vitro):K145 hydrochloride inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30 μM. The Lineweaver-Burk analysis revealed a Ki of 6.4±0.7 μM for SphK2 and indicated that K145 hydrochloride is a substrate competitive inhibitor (with sphingosine). K145 hydrochloride accumulates in U937 cells, suppresses the S1P level, and inhibits SphK2. K145 hydrochloride also exhibited inhibitory effects on the growth of U937 cells as well as apoptotic effects in U937 cells, and that these effects may be through the inhibition of downstream ERK and Akt signaling pathways.(In Vivo):In BALB/c-nu mice injected with U937 cells, K145 hydrochloride (50 mg/kg; oral gavage; for 15 days) treatment significantly inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.

Key Properties

• CAS Number: 1449240-68-9
• MW: 384.92
• Purity: >98% (HPLC)
• Formula: C₁₈H₂₅ClN₂O₃S
• SMILES: Cl.CCCCOc1ccc(CC\C=C2/SC(=O)N(CCN)C2=O)cc1
• Target: Apoptosis
• Solubility: In Vitro: H2O : 126.7 mg/mL (329.16 mM)

Bioactivity

• In Vivo:
  K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice. Animal model: BALB/c-nu mice injected with U937 cells. Dosage: 50 mg/kg. Administration: Oral gavage; daily; for 15 days. Result: Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
• In Vitro:
  K145 (0-10 μM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner. K145 (10 μM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells. K145 (4-8 μM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt. Treatment with K145 (10 μM) causes a decrease of total cellular S1P without significant effects on ceramide levels. Cell Viability Assay Cell line: U937 cells. Concentration: 0 μM, 4 μM, 6 μM, 8 μM, 10 μM. Incubation time: 24 hours, 48 hours, 72 hours. Result: Significantly inhibited the growth of U937 cells in a concentration-dependent manner. Apoptosis Analysis Cell line: U937 cells. Concentration: 10 μM. Incubation time: 24 hours. Result: Significantly induced apoptosis in U937 cells. Western blot analysis. Cell line: U937 cells. Concentration: 4 μM, 8 μM. Incubation time: 3 hours. Result: Phosphorylated ERK and Akt were decreased.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

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Gene Symbol

Apoptosis