产品说明书
SPHINX31
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同义名 : | - |
| CAS号 : | 1818389-84-2 | |
| 货号 : | A981488 | |
| 分子式 : | C27H24F3N5O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 507.507 | |
| MDL号 : | MFCD31810499 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 16 mg/mL(31.53 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | SRPK1 (serine/arginine-protein kinase 1) regulates splicing of pro-angiogenic VEGFA165a through phosphorylation of SRSF1, enabling SRSF1 nuclear translocation and binding to the proximal splice site in VEGF-A pre-mRNA. SPHINX31 is a highly selective SRPK1 inhibitor with IC50 value of 6nM. Treatment with SPHINX31 dose-dependently inhibited TNFα-induced phosphorylation of SRSF1 (serine/arginine splicing factor 1) mediated by SRPK1 with EC50 value of about 360nM in PC3 prostate cancer cells and switched splicing from VEGF-A165a to VEGF-A165b in RPE cells. SPHINX31 exhibited ocular penetrance and showed anti-angiogenic efficacy as it potently inhibited blood vessel growth in models of wet age-related macular degeneration in vivo when used as eye drops (20 μg/ml) post 14 days. Inhibition of SRPK1 by SPHINX31 halted AML expansion in vitro and in vivo, leading to cell cycle arrest, leukemic cell differentiation, and prolonged survival of immunocompromised mice transplanted with MLL-rearranged AML cells, and affected BRD4 recruitment to chromatin. | ||
| 作用机制 | SPHINX31 occupies a binding pocket created by the unique helical insert of SRPK1 and triggers a backbone flip in the hinge region, resulting potent and selective inhibition of SRPK1 kinase activity.[1] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.97mL 0.39mL 0.20mL |
9.85mL 1.97mL 0.99mL |
19.70mL 3.94mL 1.97mL |
| 参考文献 |
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