SPHINX31

SKU: orb1221159

Description

SPHINX31 is a potent inhibitor of serine/arginine-rich protein kinase 1 (SRPK1; IC50: 5.9 nM).

Key Properties

• CAS Number: 1818389-84-2
• MW: 507.51
• Purity: >98% (HPLC)
• Formula: C₂₇H₂₄F₃N₅O₂
• SMILES: FC(F)(F)c1ccc(N2CCN(Cc3ccccn3)CC2)c(NC(=O)c2ccc(o2)-c2ccncc2)c1
• Target: Serine/threonin kinase
• Solubility: DMSO: 20 mg/mL;Ethanol: 10 mg/mL;Water: Insoluble

Bioactivity

• In Vivo:
  Animal model: Norway Brown rats (intraperitoneally injected with 50 mg/kg Streptozotocin (HY-10219) to induce type I diabetes). Dosage: 200 μg/mL. Administration: Twice daily topical eye drops. Result: Reduced retinal permeability in the diabetics (7.92 ± 1.65 × 10-4 cms-1) less than before induction of diabetes (8.15 ± 2.33 × 10-4 cms-1), and less than the control group (8.85 ± 1.29 × 10-4 cms-1), while the diabetes group was 12.67 ± 1.09 × 10-4 cms-1.
• In Vitro:
  RT-PCR Cell line: HuCCA-1 cells. Concentration: 0.3, 1, 3 and 10 μM Incubation time: 24 h. Result: Significantly down-regulated about 60% of the expression of VEGF-A165a mRNA compared with the control cells. Immunofluorescence Cell line: HuCCA-1 cells. Concentration: 0.3 μM Incubation time: 24 h. Result: Suppressed SRSF1 phosphorylation and nuclear localization, which thereby induced less expression of pro-angiogenic VEGF-A165a in HuCCA-1 cells. Cell Migration Assay Cell line: HuCCA-1 cells. Concentration: 0.3, 1, 3 and 10 μM Incubation time: 24 h. Result: Decreased pre-tube formation of the cells network area to about 50% of the control group.

Storage & Handling

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

Quick Database Links

Gene Symbol

Serine/threonin kinase