SPHINX31

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SPHINX31 是富含丝氨酸/精氨酸的蛋白激酶 1 (SRPK1；IC50: 5.9 nM) 的有效抑制剂。

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

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 hResult:Decreased pre-tube formation of the cells network area to about 50% of the control group.

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.

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Apoptosis

Serine/threonin kinase

SRPK1

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1818389-84-2

507.51

C27H24F3N5O2

>98% (HPLC)

DMSO: 20 mg/mL;Ethanol: 10 mg/mL;Water: Insoluble

FC(F)(F)c1ccc(N2CCN(Cc3ccccn3)CC2)c(NC(=O)c2ccc(o2)-c2ccncc2)c1

5-(4-pyridinyl)-N-[2-[4-(2-pyridinylmethyl)-1-piperazinyl]-5-(trifluoromethyl)phenyl]-2-furancarboxamide

(-20℃)

With Ice Pack

≥ 2 years