Cat. No.: HY-117661

SPHINX31

13 Cited Publications

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Based on 13 publication(s) in Google Scholar

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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Pureté: 99.25%
CAS No.: 1818389-84-2
Formule: C₂₇H₂₄F₃N₅O₂
Masse moléculaire:507.51

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

SPHINX31 Chemical Structure

CAS No.: 1818389-84-2

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

IC₅₀: 5.9 nM (SRPK1)^[1]
VEGF-A₁₆₅a^[2]

Voir tous les produits spécifiques à Isoform VEGFR :

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.

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.

Chemical Information

CAS No. 1818389-84-2
Appearance Solid
Masse moléculaire 507.51
Formule C₂₇H₂₄F₃N₅O₂
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (13)

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Journal Impact Factor

Nat Commun

Hippo signaling pathway regulates Ebola virus transcription and egress. [Abstract]

2024 Aug 13;15(1):6953. PMID: 39138205
Blood Adv

Deep PIM kinase substrate profiling reveals new rational co-therapeutic strategies for acute myeloid leukemia. [Abstract]

2024 Aug 13;8(15):3880-3892. PMID: 38739710

SPHINX31 purchased from MedChemExpress. Usage Cited in: Blood Adv. 2024 Aug 13;8(15):3880-3892. [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.
Sci Signal

Host protein kinases required for SARS-CoV-2 nucleocapsid phosphorylation and viral replication. [Abstract]

2022 Oct 25;15(757):eabm0808. PMID: 36282911

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.
Front Pharmacol

Icariside Ⅱ Attenuates Palmitic Acid-Induced Endothelial Dysfunction Through SRPK1-Akt-eNOS Signaling Pathway. [Abstract]

2022 Jun 30;13:920601. PMID: 35846993

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.
Med Oncol

Effects of PELP1 on proliferation, metastasis and angiogenesis of epithelial ovarian cancer. [Abstract]

2025 Jul 26;42(9):379. PMID: 40715657
BMC Cancer

Inhibition of SRPK1, a key splicing regulator, exhibits antitumor and chemotherapeutic-sensitizing effects on extranodal NK/T-cell lymphoma cells. [Abstract]

2022 Oct 27;22(1):1100. PMID: 36303126
Toxins

Proteome and Phosphoproteome Profiling Reveal the Toxic Mechanism of Clostridium perfringens Epsilon Toxin in MDCK Cells. [Abstract]

2024 Sep 14;16(9):394. PMID: 39330852
Front Oncol

HPV-driven transcriptome and splicing rewiring under SRPK1 inhibition in cervical cancer. [Abstract]

2026 Jan 2:15:1712170. PMID: 41551143
J Food Drug Anal

Xanthohumol as a potential therapeutic strategy for acute myeloid leukemia: Targeting the FLT3/SRPK1 signaling axis. [Abstract]

2025 Mar 31;33(1):31-47. PMID: 40202412
Glycobiology

Compromised CDK12 activity causes dependency on the high activity of O-GlcNAc transferase. [Abstract]

2024 Dec 10;34(12):cwae081. PMID: 39361894
Mol Biol Rep

Targeting SRPK1 to regulate alternative splicing in prostate cancer: the roles of MALAT1 and TUG1. [Abstract]

2025 Nov 6;53(1):55. PMID: 41196435
SSRN

2023 Jun 20.
bioRxiv

The FDA-approved drug Alectinib compromises SARS-CoV-2 nucleocapsid phosphorylation and inhibits viral infection in vitro. [Abstract]

2020 Dec 16:2020.08.14.251207. PMID: 32817937

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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

Stock Solution Working Solution

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.

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.

Working Solution

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

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (283 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Batson J, et al. Development of Potent, Selective SRPK1 Inhibitors as Potential Topical Therapeutics for Neovascular Eye Disease. ACS Chem Biol. 2017 Mar 17;12(3):825-832. [Content Brief]

[2]. Supradit K, et al. Inhibition of serine/arginine-rich protein kinase-1 (SRPK1) prevents cholangiocarcinoma cells induced angiogenesis. Toxicol In Vitro. 2022 Aug;82:105385. [Content Brief]

[3]. C. Allen, et al. The SRPK1 inhibitor SPHINX31 prevents increased retinal permeability in a rodent model of diabetes. Acta Ophthalmologica. Volume 95, Issue S259.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

SPHINX31

13 Cited Publications

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SPHINX31

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Anti-diabetic Compound Library

Anti-Cardiovascular Disease Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SPHINX31

Voir tous les produits spécifiques à Isoform VEGFR

Activité biologique

Chemical Information

Publications (13)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

SPHINX31 Related Classifications

HY-117661 Related Classifications