2. Cell Cycle/DNA Damage Protein Tyrosine Kinase/RTK
  3. SRPK VEGFR
  4. SPHINX31

SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease.

For research use only. We do not sell to patients.

CAS No. : 1818389-84-2

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Customer Review

Based on 13 publication(s) in Google Scholar

SPHINX31 Related Antibodies

Top Publications Citing Use of Products

    SPHINX31 purchased from MedChemExpress. Usage Cited in: Blood Adv. 2024 May 13:bloodadvances.2022008144.  [Abstract]

    MLL-rearranged EOL-1 and MV4-11 cells were treated with PIM447 + SPHINX31 (0.25, 0.5, 1.0, 2.0, 4.00 μM for EOL-1 cells; 0.625 1.25 2.5 5.0 10.0 μM for MV4-11 cells; 48 h) or each compound alone. CI values were calculated using CompuSyn. Fa-CI plots were generated based on constant dose ratio drug combination data. CI < 1 indicates synergy; CI > 1 indicates antagonism; CI = 1 indicates additivity. The tan shaded area indicates synergy and strong effect (fraction affected, Fa > 0.75). The results showed that the combination treatment produced a potent synergistic killing effect in EOL-1 and MV4-11 cells.

    SPHINX31 purchased from MedChemExpress. Usage Cited in: Sci Signal. 2022 Oct 25;15(757):eabm0808.  [Abstract]

    Cellular viability (left axis) was measured after ACE2-A549 cells were treated with the indicated concentrations of SPHINX31 (1.5-12 μM; 48 h for viability analysis and 12 h for qRT-PCR analysis). Data are from four independent biological replicates. SARS-CoV-2 viral RNA abundance (right axis) was measured by qRT-PCR analysis 24 hours after infection of cells. Data are from four independent biological replicates.

    SPHINX31 purchased from MedChemExpress. Usage Cited in: Sci Signal. 2022 Oct 25;15(757):eabm0808.  [Abstract]

    Infectious viral titers were measured by plaque assay of the supernatants of cells that were treated with SPHINX31 (12 μM; 12 h) and infected for 48 hours. Data are from four independent biological replicates.

    SPHINX31 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 Jun 30;13:920601.  [Abstract]

    HUVECs were treated with different concentrations of SPHINX31 (1-40 μM; 24-72 h) for the indicated time with cell viability measured via CCK-8. The results showed that SPHINX31 reduced HUVEC cell viability in a dose-dependent manner.

    SPHINX31 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 Jun 30;13:920601.  [Abstract]

    After treatment with different concentrations (2.5 and 5 μM) of SPHINX31 for 24 h, the immunofluorescence staining for Ki-67 (green) and DAPI (blue) was determined.

    SPHINX31 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2022 Jun 30;13:920601.  [Abstract]

    HUVECs were treated with different concentrations of SPHINX31 (1.5-10 μM) for 24 h. The levels of eNOS, phosphor-eNOS (Ser1177), Akt, phosphor-Akt (Ser473), and SRPK1 were determined by western blot. The results showed that SPHINX31 significantly reduced the expression and phosphorylation levels of Akt and eNOS by inhibiting SRPK1, implying that the Akt-eNOS signaling pathway was interdicted by the inhibition of SRPK1.

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    Description

    SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-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]
    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    SPHINX31 Related Antibodies

    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.
    In Vivo

    SPHINX31 (200 μg/mL; twice daily topical eye drops) protects the retinal endothelial permeability barrier from diabetes-associated loss of integrity[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Norway Brown rats (intraperitoneally injected with 50 mg/kg Streptozotocin (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 × 10-4 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.
    Molecular Weight

    507.51

    Formula

    C27H24F3N5O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=C(N2CCN(CC3=CC=CC=N3)CC2)C=CC(C(F)(F)F)=C1)C4=CC=C(O4)C5=CC=NC=C5
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 15 mg/mL (29.56 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9704 mL 9.8520 mL 19.7040 mL
    5 mM 0.3941 mL 1.9704 mL 3.9408 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2 mg/mL (3.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2 mg/mL (3.94 mM); Clear solution

      This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 25 mg/mL (49.26 mM); Suspended solution; Need ultrasonic

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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9704 mL 9.8520 mL 19.7040 mL 49.2601 mL
    5 mM 0.3941 mL 1.9704 mL 3.9408 mL 9.8520 mL
    10 mM 0.1970 mL 0.9852 mL 1.9704 mL 4.9260 mL
    15 mM 0.1314 mL 0.6568 mL 1.3136 mL 3.2840 mL
    20 mM 0.0985 mL 0.4926 mL 0.9852 mL 2.4630 mL
    25 mM 0.0788 mL 0.3941 mL 0.7882 mL 1.9704 mL
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    SPHINX31 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    SPHINX311818389-84-2SPHINX 31SPHINX-31SRPKVEGFRSerine-arginine protein kinasesVascular endothelial growth factor receptorangiogenicneovasculareye diseaseretinal permeabilitydiabeticsHuCCA-1Norway Brown ratsInhibitorinhibitorinhibit

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