2. Cell Cycle/DNA Damage
  3. SRPK
  4. SRPKIN-1

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.

CAS No. : 2089226-94-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 6 publication(s) in Google Scholar

SRPKIN-1 Related Antibodies

Top Publications Citing Use of Products

    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.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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.

    SRPKIN-1 Related Antibodies

    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].
    Molecular Weight

    472.53

    Formula

    C27H21FN2O3S
    CAS No.
    Appearance

    Solid

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    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)

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1163 mL 10.5813 mL 21.1627 mL
    5 mM 0.4233 mL 2.1163 mL 4.2325 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, 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.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    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: ≥ 2.75 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.
    • 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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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).

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

    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

    Purity: 99.68%

    SDS (252 KB)

    COA (250 KB) HNMR (466 KB) CNMR (478 KB) RP-HPLC (269 KB) LCMS (98 KB)

    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
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    SRPKIN-1 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:

    SRPKIN-12089226-94-6SRPKIN1SRPKIN 1SRPKSerine-arginine protein kinasesInhibitorinhibitorinhibit

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