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.

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SPHINX31 Chemical Structure

SPHINX31 Chemical Structure

CAS No. : 1818389-84-2

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Based on 4 publication(s) in Google Scholar

SPHINX31 Related Antibodies

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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 : 17.33 mg/mL (34.15 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

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.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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
30 mM 0.0657 mL 0.3284 mL 0.6568 mL 1.6420 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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