Art. -Nr.: HY-116856

SRPKIN-1

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC₅₀s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect.

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Reinheit: 99.68%
CAS. Nr.: 2089226-94-6
Formel: C₂₇H₂₁FN₂O₃S
Molecular Weight:472.53

Speicherung:

-20°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

SRPKIN-1 Chemical Structure

CAS. Nr.: 2089226-94-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SRPKIN-1 is a covalent and irreversible SRPK1/2 inhibitor with IC₅₀s of 35.6 and 98 nM, respectively. Anti-angiogenesis effect^[1].

IC₅₀ & Target

IC50: 35.6 nM (SRPK1), 98 nM (SRPK2)^[1]

In Vitro

SRPKIN-1 treatment at 200 nM (10, 50, 100, 200 nM, 16 hours) significantly reduces SR protein phosphorylation at the steady state with or without washout^[1]. ?

SRPK-IN-1 potently converts VEGF from pro-angiogenic to anti-angiogenic isoform^[1].

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

Cell Viability Assay^[1]

Cell Line:

Ba/F3 cells
Concentration:

0-10000 nM
Incubation Time:

72 h
Result:

Potently decreased the level of SR phosphorylation in a dose-dependent manner, leading to increased VEGF-A165b RNA as well as protein even at a dose of 200 nM^[1].

In Vivo

SRPKIN-1 (50 nM, 300 nM,1 μL, 5 times) blocks angiogenesis in a CNV mouse model through VEGF alternative splicing^[1].

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

Animal Model:

Mice^[1]
Dosage:

50 nM, 300 nM, 1 μL
Administration:

Intravitreal injection, 5 times
Result:

SRPKIN-1-treated mice is significantly suppressed in a dose-dependent manner based upon measurement of the CNV area^[1].

Chemical Information

CAS. Nr. 2089226-94-6
Appearance Solid
Molecular Weight 472.53
Formel C₂₇H₂₁FN₂O₃S
Color White to off-white
SMILES

O=S(C1=CC=CC(C2=C(CC)C=C3C(C(C)(C)C(NC4=C5C=CC(C#N)=C4)=C5C3=O)=C2)=C1)(F)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

Publications (6)

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Mol Cell

FAM120A couples SREBP-dependent transcription and splicing of lipogenesis enzymes downstream of mTORC1. [Abstract]

2023 Aug 17;83(16):3010-3026.e8. PMID: 37595559

SRPKIN-1 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Aug 17;83(16):3010-3026.e8. [Abstract]

Co-IP analysis of LAM cell serum starved overnight (to induce SREBP cleavage) and treated with SREBP cleavage inhibitor (25-Hydroxycholesterol, 25-HC, 10 µM), or SRPK inhibitor (SRPKIN-1, 5 µM) for 4 h.

SRPKIN-1 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2023 Aug 17;83(16):3010-3026.e8. [Abstract]

Co-IP analysis of LAM cell serum starved overnight (to induce SREBP cleavage) and treated with SREBP cleavage inhibitor (25-Hydroxycholesterol, 25-HC, 10 µM), or SRPK inhibitor (SRPKIN-1, 5 µM) for 4 h.
Leukemia

Posttranslational splicing modifications as a key mechanism in cytarabine resistance in acute myeloid leukemia. [Abstract]

2023 Aug;37(8):1649-1659. PMID: 37422594
Int J Biol Macromol

SRPK1 facilitates IBDV replication by phosphorylating VP1 at S48. [Abstract]

2024 Dec 21:139002. PMID: 39716705
PLoS Pathog

Subversion of phosphorylated SR proteins by enterovirus A71 in IRES-dependent translation revealed by RNA-interactome analysis. [Abstract]

2025 Jun 16;21(6):e1013242. PMID: 40522993
Cancers (Basel)

SRSF5 Regulates the Expression of BQ323636.1 to Modulate Tamoxifen Resistance in ER-Positive Breast Cancer. [Abstract]

2023 Apr 13;15(8):2271. PMID: 37190199
Antiviral Res

SRPKIN-1 as an inhibitor against hepatitis B virus blocking the viral particle formation and the early step of the viral infection. [Abstract]

2023 Dec:220:105756. PMID: 37992764

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (211.63 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

2.1163 mL

10.5813 mL

21.1627 mL

5 mM

0.4233 mL

2.1163 mL

4.2325 mL

10 mM

0.2116 mL

1.0581 mL

2.1163 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, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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: ≥ 2.75 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (5.82 mM); Clear solution

This protocol yields a clear solution of ≥ 2.75 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 (27.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Handling Instructions (2659 KB)

Verweise

[1]. Hatcher JM, et al. SRPKIN-1: A Covalent SRPK1/2 Inhibitor that Potently Converts VEGF from Pro-angiogenic to Anti-angiogenic Isoform. Cell Chem Biol. 2018 Apr 19;25(4):460-470.e6. [Content Brief]

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1163 mL	10.5813 mL	21.1627 mL	52.9067 mL
	5 mM	0.4233 mL	2.1163 mL	4.2325 mL	10.5813 mL
	10 mM	0.2116 mL	1.0581 mL	2.1163 mL	5.2907 mL
	15 mM	0.1411 mL	0.7054 mL	1.4108 mL	3.5271 mL
	20 mM	0.1058 mL	0.5291 mL	1.0581 mL	2.6453 mL
	25 mM	0.0847 mL	0.4233 mL	0.8465 mL	2.1163 mL
	30 mM	0.0705 mL	0.3527 mL	0.7054 mL	1.7636 mL
	40 mM	0.0529 mL	0.2645 mL	0.5291 mL	1.3227 mL
	50 mM	0.0423 mL	0.2116 mL	0.4233 mL	1.0581 mL
	60 mM	0.0353 mL	0.1764 mL	0.3527 mL	0.8818 mL
	80 mM	0.0265 mL	0.1323 mL	0.2645 mL	0.6613 mL
	100 mM	0.0212 mL	0.1058 mL	0.2116 mL	0.5291 mL

Keywords

SRPKIN-1

6 Cited Publications

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SRPKIN-1

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Anti-Cardiovascular Disease Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SRPKIN-1

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SRPKIN-1

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Covalent Screening Library

Anti-Cardiovascular Disease Compound Library

Anti-Obesity Compound Library

Targeted Diversity Library

Serine/Threonine Kinase Inhibitor Library

Bioactive Compound Library Max

Anti-Aging Compound Library Mini

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) SRPKIN-1

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

SRPKIN-1 Related Classifications

HY-116856 Related Classifications