SRPKIN-1
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.
For research use only. We do not sell to patients.
- Purity : 99.68%
- CAS No.: 2089226-94-6
- Formula: C27H21FN2O3S
- Molecular Weight:472.53
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Storage:
-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 Citing Use of MedChemExpress (MCE) SRPKIN-1
More- Mol Cell. 2023 Aug 17;83(16):3010-3026.e8. [Abstract]
- Leukemia. 2023 Aug;37(8):1649-1659. [Abstract]
- Int J Biol Macromol. 2025 Feb:291:139002. [Abstract]
- PLoS Pathog. 2025 Jun 16;21(6):e1013242. [Abstract]
- Cancers (Basel). 2023 Apr 13;15(8):2271. [Abstract]
- Antiviral Res. 2023 Dec:220:105756. [Abstract]
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IP
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IP
Biological Activity
Description
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. Further protocols information, click here.
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Cell Line:Ba/F3 cells
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Concentration:0-10000 nM
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Incubation Time:72 h
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice[1]
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Dosage:50 nM, 300 nM, 1 μL
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Administration:Intravitreal injection, 5 times
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Result:SRPKIN-1-treated mice is significantly suppressed in a dose-dependent manner based upon measurement of the CNV area[1].
Chemical Information
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CAS No. 2089226-94-6
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Appearance Solid
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Molecular Weight 472.53
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Formula C27H21FN2O3S
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Color White to off-white
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-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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Journal Impact Factor
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Most Recent
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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.
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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
2025 Feb:291:139002. 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
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocols
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Human pluripotent stem cell endothelial-cell differentiation
Human pluripotent stem cell endothelial differentiation is based on stepwise developmental patterning: early activation of WNT/GSK3β inhibition promotes mesodermal or vascular progenitor entry, followed by endothelial specification using VEGF-related signaling, BMP4, FGF2, Notch modulation, or cAMP depending on the published protocol. Endothelial differentiation is read out by acquisition of CD31, CD34, VE-cadherin/CD144, KDR/VEGFR2, vWF, Tie2, NOS3, acetylated LDL uptake, tube/network formation, barrier function, and in vivo vessel-forming capacity where tested.
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Vascular/Branching Fractal Analysis
Vascular/branching fractal analysis quantifies the geometric complexity of vessel trees or vascular networks from segmented 2D images, commonly by converting vessels into binary and/or skeletonized maps and estimating fractal dimension using box-counting or related approaches. Fractal dimension is interpreted as an image-derived readout of vascular branching complexity, space filling, or density, and has been applied to retinal photographs, fluorescein angiography, OCT angiography, capillary perfusion maps, and in vitro Matrigel angiogenesis networks. The assay readout is generated from vessel-positive pixels after image preprocessing, vessel segmentation, binarization, and optional skeletonization; reported outputs include fractal dimension, vessel density, branchpoint density, endpoint density, vessel length density, tortuosity, and generation-based branching metrics when VESGEN-style analysis is used. The biological interpretation is limited to quantitative vascular patterning and s
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Endothelial Tube Formation Assay
Endothelial tube formation assay evaluates the ability of endothelial cells to attach, migrate, align, and organize into capillary-like networks when cultured on gelled basement membrane extract or Matrigel; the readout is the morphology and quantity of tube-like networks, which reflects an in vitro endothelial morphogenesis step related to angiogenesis. Basement membrane extract/Matrigel provides laminin-rich extracellular matrix cues that support endothelial differentiation into capillary-like structures, but it can contain biologically active growth factors, so growth-factor-reduced matrix is preferred when testing defined angiogenic stimulators or inhibitors.
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Endothelial Cell Migration/Angiogenic Sprouting Assay
Endothelial cell migration and angiogenic sprouting assays are in vitro (and partially ex vivo-adapted) functional models that quantify the ability of endothelial cells to undergo coordinated migration, extracellular matrix invasion, and multicellular organization into capillary-like sprouts in response to pro-angiogenic stimuli such as VEGF, bFGF, or conditioned microenvironments. These assays are used to model early angiogenic events including tip-cell formation, directional migration, and lumen-like sprout extension, which collectively reflect angiogenic activation and vascular morphogenesis processes observed in vivo.
Purity & Documentation
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Data Sheet (275 KB)
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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)
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Handling Instructions (2659 KB)
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, 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.
| 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 |