2. Epigenetics
  3. Protein Arginine Deiminase
  4. GSK484 hydrochloride

GSK484 (hydrochloride)  (Synonyms: GSK484 HCl)

製品番号: HY-100514 純度: 99.48%
COA 取扱説明書 Technical Support

GSK484 hydrochloride is a selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor. GSK484 hydrochloride demonstrates high affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed.

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CAS 番号 : 1652591-81-5

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 213 在庫あり
Solution
10 mM * 1 mL in DMSO USD 213 在庫あり
Solid
5 mg $190 在庫あり
10 mg $290 在庫あり
25 mg $550 在庫あり
50 mg $900 在庫あり
100 mg $1300 在庫あり
200 mg $1888 在庫あり
500 mg $3780 在庫あり
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カスタマーレビュー

Based on 49 publication(s) in Google Scholar

Other Forms of GSK484 hydrochloride:

GSK484 (hydrochloride) 関連抗体

Top Publications Citing Use of Products

顧客検証

In Vivo Efficacy Study

    GSK484 hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2025 Jul 30:S1535-6108(25)00320-4.  [Abstract]

    Schema for GSK484 treatment protocol and summary tumor growth curves of MC38 in Dnase1l3fl/fl and Dnase1l3cko mice (n = 7).

    GSK484 hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7.  [Abstract]

    Mice were treated with GSK484 (20 mg/kg, i.p. daily shots for 20 days from day 7, and then maintenance shots every two days) following orthotopic injection of AT3 cells. Shown are BLI quantification of primary tumor growth at day 19.

    GSK484 hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7.  [Abstract]

    Mice were treated with GSK484 (20 mg/kg, i.p. daily shots for 20 days from day 7, and then maintenance shots every two days) following orthotopic injection of AT3 cells. Shown are BLI quantification of lung metastasis at week 5.

    GSK484 hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7.  [Abstract]

    Mice were treated with GSK484 (20 mg/kg, i.p. daily shots for 20 days from day 7, and then maintenance shots every two days) following orthotopic injection of AT3 cells. Shown are pulmonary surface nodules at week 5.

    GSK484 hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Cell. 2021 Mar 8;39(3):423-437.e7.  [Abstract]

    Mice were treated with GSK484 (20 mg/kg, i.p. daily shots for 20 days from day 7, and then maintenance shots every two days) following orthotopic injection of AT3 cells. Shown are NET formation in lung metastases.

    • 生物活性

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    • 参考文献

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    製品説明

    GSK484 hydrochloride is a selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor. GSK484 hydrochloride demonstrates high affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed.

    IC50 & Target

    IC50: 50 nM (PAD4, in the absence of Calcium), 250 nM (PAD4, in the presence of 2 mM Calcium)[1]
    体外実験

    GSK484 demonstrates high affinity binding to the low-calcium form of PAD4 with IC50s of 50 nM and 250 nM in the absence of Calcium (0 mM) and Calcium (2 mM), respectively. GSK484 also inhibits PAD4 citrullination (at 0.2 mM Calcium) of benzoyl-arginine ethyl ester (BAEE) substrate in a concentration-dependent manner, as detected using an NH3 release assay[1].

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

    GSK484 (hydrochloride) 関連抗体
    体内実験

    To address whether PAD4 inhibition can suppress cancer-associated kidney injury, MMTV-PyMT mice are treated with the PAD4 inhibitor GSK484 at 4 mg/kg daily for one week. This dose suppress the elevated number of neutrophils undergoing NETosis in peripheral blood in mice with cancer. In parallel, the total protein level in urine from MMTV-PyMT mice is significantly reduced compared with untreated tumor-bearing mice, further supporting an improved functional status of the kidneys after GSK484 treatment. Administration of GSK484 at a dose of 4 mg/kg daily during one week reverts signs of kidney dysfunction in tumor-bearing mice to the same extent as DNase I treatment, without any detectable signs of toxicity[2].

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

    510.03

    分子式

    C27H32ClN5O3
    CAS 番号
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(N1C[C@H](N)[C@H](O)CC1)C2=CC(OC)=C3C(N=C(C(N4CC5CC5)=CC6=C4C=CC=C6)N3C)=C2.[H]Cl
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, stored under nitrogen, away from moisture

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

    H2O : 100 mg/mL (196.07 mM; Need ultrasonic)

    DMSO : 100 mg/mL (196.07 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 1.9607 mL 9.8033 mL 19.6067 mL
    5 mM 0.3921 mL 1.9607 mL 3.9213 mL
    10 mM 0.1961 mL 0.9803 mL 1.9607 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, 1 year; -20°C, 6 months (stored under nitrogen, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体内:

    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: ≥ 2.08 mg/mL (4.08 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (4.08 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    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:  Saline

      Solubility: 100 mg/mL (196.07 mM); Clear solution; Need ultrasonic

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

    Dosage

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    純度とドキュメンテーション

    純度: 99.48%

    COA (250 KB) HNMR (286 KB) RP-HPLC (261 KB) LCMS (96 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [1]

    PAD4 is serially diluted in the presence of 10 nM GSK215 in assay buffer (100 mM HEPES, pH 8, 50 mM NaCl, 5% glycerol, 1 mM CHAPS, 1 mM DTT) at varying concentrations of calcium (0, 0.2, 2 and 10 mM). Following incubation for 50 min, apparent Kds for each calcium concentration are determined using a single site saturation curve. For IC50 determination, test compounds (e.g., GSK484) are serially diluted in DMSO (1% final assay concentration) and tested at the same range of calcium concentrations in the presence of PAD4 (at the calculated Kd for each calcium condition) and 10 nM GSK215 in the same assay buffer and volume. Reactions are incubated for 50 min after which IC50 values are calculated using a four-parameter logistic equation[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [1]

    HEK293 cells stably expressing N-terminal FLAG-tagged PAD1, PAD2, PAD3 or PAD4 are engineered by retroviral transduction. Cells are grown in 15 cm diameter plates to subconfluency in DMEM supplemented with 10% Foetal Bovine Serum, harvested by centrifugation and washed once in PBS/2 mM EGTA. Cells are lysed in 50 mM Tris-Cl, pH 7.4, 1.5 mM MgCl2, 5% glycerol, 150 mM NaCl, 25 mM NaF, 1 mM Na3VO4, 0.4% NP40, 1 mM DTT with protease inhibitors. Lysates are pre-incubated for 20 min at 4°C with DMSO alone (2%), 100 µM of GSK199, GSK484, GSK106 or 200 µM Cl-amidine. Citrullination reactions are performed for 30 min at 37°C in the presence of 2 mM calcium. Extracts are loaded on to gels, proteins separated by SDS-PAGE and transferred to PVDF membranes. Citrullinated proteins are then chemically modified and detected using anti-modified citrulline antibody. FLAG-PAD constructs are detected using anti-FLAG antibody[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [2]

    Mice[2]
    The study includes two transgenic mouse models, the MMTV-PyMT mouse model for mammary carcinoma (FVB/n background) and the RIP1-Tag2 mouse model for pancreatic neuroendocrine carcinoma (C57BL/6 background). Mice are treated daily by intra-peritoneal injections of the PAD4 inhibitor GSK484 (4 mg/kg). GSK484 is dissolved in 99.9% ethanol at a concentration of 25 mg/mL to generate a stock solution and further diluted 1:50 in 0.9% NaCl shortly before injection of 200 μL/mouse[2].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

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

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.9607 mL 9.8033 mL 19.6067 mL 49.0167 mL
    5 mM 0.3921 mL 1.9607 mL 3.9213 mL 9.8033 mL
    10 mM 0.1961 mL 0.9803 mL 1.9607 mL 4.9017 mL
    15 mM 0.1307 mL 0.6536 mL 1.3071 mL 3.2678 mL
    20 mM 0.0980 mL 0.4902 mL 0.9803 mL 2.4508 mL
    25 mM 0.0784 mL 0.3921 mL 0.7843 mL 1.9607 mL
    30 mM 0.0654 mL 0.3268 mL 0.6536 mL 1.6339 mL
    40 mM 0.0490 mL 0.2451 mL 0.4902 mL 1.2254 mL
    50 mM 0.0392 mL 0.1961 mL 0.3921 mL 0.9803 mL
    60 mM 0.0327 mL 0.1634 mL 0.3268 mL 0.8169 mL
    80 mM 0.0245 mL 0.1225 mL 0.2451 mL 0.6127 mL
    100 mM 0.0196 mL 0.0980 mL 0.1961 mL 0.4902 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    GSK484 hydrochloride Related Classifications

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    Keywords:

    GSK4841652591-81-5GSK 484GSK-484Protein Arginine DeiminasePeptidylarginine DeiminaseInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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