SPHINX31 是一种有效的、丝氨酸/富含精氨酸的蛋白激酶1(SRPK1)的选择性抑制剂，其IC50值为 5.9 nM。SPHINX31 能够抑制富丝氨酸/精氨酸剪接因子 1 (SRSF1) 的磷酸化。SPHINX31 还能降低促血管生成基因VEGF-A165a 亚型的 mRNA 表达。SPHINX31 可用于研究新生血管性眼病。
| 生物活性 | SPHINX31 is a potent and selectiveSRPK1inhibitor, with anIC50of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenicVEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease[1][2][3]. |
| IC50& Target | IC50: 5.9 nM (SRPK1)[1]
VEGF-A165a[2] |
体外研究
(In Vitro) | SPHINX31 (0.3-10 μM; 24 h) significantly down-regulates the expression of VEGF-A165a mRNA[2].
SPHINX31 (0.3 μM; 24 h) suppresses SRSF1 phosphorylation and nuclear localization[2].
SPHINX31 (0.3-10 μM; 24 h) decreases pre-tube formation and the rate of migration for human umbilical vein endothelial cells (HUVECs)[2].
RT-PCR[2] | 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[2] | 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[2] | 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.
Decreased the rate of migration for HUVECs. |
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体内研究
(In Vivo) | SPHINX31 (200 μg/mL; twice daily topical eye drops) protects the retinal endothelial permeability barrier from diabetes-associated loss of integrity[3].
| Animal Model: | Norway Brown rats (intraperitoneally injected with 50 mg/kgStreptozotocin(HY-10219) to induce type I diabetes)[3] | | Dosage: | 200 μg/mL | | Administration: | Twice daily topical eye drops | | Result: | Reduced retinal permeability in the diabetics (7.92 ± 1.65 × 10-4cms-1) less than before induction of diabetes (8.15 ± 2.33 × 10-4cms-1), and less than the control group (8.85 ± 1.29 × 10-4cms-1), while the diabetes group was 12.67 ± 1.09 × 10-4cms-1. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 17.33 mg/mL(34.15 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9704 mL | 9.8520 mL | 19.7040 mL | | 5 mM | 0.3941 mL | 1.9704 mL | 3.9408 mL | | 10 mM | 0.1970 mL | 0.9852 mL | 1.9704 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
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此方案可获得 ≥ 2 mg/mL (3.94 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2 mg/mL (3.94 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (3.94 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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