2. GPCR/G Protein
  3. P2Y Receptor
  4. YM-254890

YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM.

For research use only. We do not sell to patients.

CAS No. : 568580-02-9

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Customer Review

Based on 17 publication(s) in Google Scholar

YM-254890 Related Antibodies

Top Publications Citing Use of Products

    YM-254890 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Dec 8;16(1):10938.  [Abstract]

    Normalized amplitudes of fEPSPs before and after TBS with one-hour preincubation with aCSF (Steel, N = 5 mice, 7 slices), 20 μM YM-254890 (Dark purple, N = 3 mice, 6 slices) in C57 mice with representative trace of single fEPSP before (translucent color) and after (solid color) TBS. The results showed that YM254890 significantly inhibited the formation of LTP by inhibiting Gαq/11.

    YM-254890 purchased from MedChemExpress. Usage Cited in: J Hematol Oncol. 2024 Feb 24;17(1):9.  [Abstract]

    BM-MDSCs were pretreated with DMSO (0.1%), FFAR2 Agonist (10 μM), Gαq inhibitor (YM-254890; 1 μM), Ca2+ inhibitor (2-APB; 100 μM) and PPAR-γ-inhibitor (GW9662; 2 μM) for 2 h before adding GM-CSF and IL-6. All MDSCs were treated for 24 h, and the percentage of Arg1+ cells and representative gating strategy were analyzed by flow cytometry (n = 3, biological replicates).

    YM-254890 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Feb 20;5(2):101388.  [Abstract]

    Cell viability assays of control and CHRM1-OE 22Rv1 cells treated with YM-254890 (100 nM) or ARRB2 siRNA for 24 h followed by DTX at various doses for 48 h (n = 4 biological replicates).

    YM-254890 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Feb 20;5(2):101388.  [Abstract]

    Western blot of p-PKCa and p-PKCd in 22Rv1 and 22Rv1DTXR cells treated with YM-254890 (100 nM, 30 min).

    YM-254890 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2024 Feb 20;5(2):101388.  [Abstract]

    Detection of Ca2+ influx in control and CHRM1-OE 22Rv1 cells treated with YM-254890 (100 nM, 5 min) followed by 10 µM carbachol stimulation within a 30-min monitoring period (n = 3 biological replicates).

    YM-254890 purchased from MedChemExpress. Usage Cited in: Cell. 2023 Nov 22;186(24):5347-5362.e24.  [Abstract]

    Effects of SEP (3 mg/kg) or CHA (30 mg/kg) on OFT in MK-801-induced schizophrenia-like mice model pretreated with or without Gq inhibitor YM-254890 (YM, 0.3 mg/kg) (n values were indicated at the bottom of the bars).

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    Description

    YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM[1][2].

    IC50 & Target

    P2Y1 Receptor

     

    In Vitro

    YM-254890 inhibits platelet aggregation induced by ADP (2, 5 and 20 μM) in human platelet-rich plasma with IC50 values of 0.37, 0.39 and 0.51 μM. ADP mediates platelet aggregation via two G protein-coupled receptors, P2Y1 and P2Y12. The effect of YM-254890 on the P2Y1 and P2Y12 signal transduction pathways using C6-15 cells stably expressing the human P2Y1 or P2Y12 receptors is examined. Stimulation of P2Y1-C6-15 cells by 2MeSADP leads to increases in intracellular calcium mobilization. In this assay, YM-254890 inhibits the increase in [Ca2+]i with an IC50 value of 0.031 μM. In contrast, 2MeSADP-induced inhibition of forskolin-stimulated adenylyl cyclase activity in P2Y12-C6-15 cells is unaffected by YM-254890 at 40 μM[1].

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

    YM-254890 Related Antibodies
    Molecular Weight

    960.08

    Formula

    C46H69N7O15
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    CN([C@@H](C)C(N[C@@H]([C@H](OC([C@@H](NC(C)=O)[C@@H](C(C)C)O)=O)C(C)C)C(N(C)[C@@H]([C@H](OC)C)C(O[C@@H]1C)=O)=O)=O)C([C@H](C)NC(C(N(C([C@@H](CC2=CC=CC=C2)OC([C@H]1NC(C)=O)=O)=O)C)=C)=O)=O
    Structure Classification
    Initial Source

    the culture broth of Chromobacterium sp
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (52.08 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 1.0416 mL 5.2079 mL 10.4158 mL
    5 mM 0.2083 mL 1.0416 mL 2.0832 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. 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)

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 1.25 mg/mL (1.30 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1.25 mg/mL (1.30 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
    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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    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).
    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: 99.18%

    SDS (251 KB)

    COA (262 KB) HNMR (294 KB) RP-HPLC (257 KB) LCMS (97 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. 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 1.0416 mL 5.2079 mL 10.4158 mL 26.0395 mL
    5 mM 0.2083 mL 1.0416 mL 2.0832 mL 5.2079 mL
    10 mM 0.1042 mL 0.5208 mL 1.0416 mL 2.6039 mL
    15 mM 0.0694 mL 0.3472 mL 0.6944 mL 1.7360 mL
    20 mM 0.0521 mL 0.2604 mL 0.5208 mL 1.3020 mL
    25 mM 0.0417 mL 0.2083 mL 0.4166 mL 1.0416 mL
    30 mM 0.0347 mL 0.1736 mL 0.3472 mL 0.8680 mL
    40 mM 0.0260 mL 0.1302 mL 0.2604 mL 0.6510 mL
    50 mM 0.0208 mL 0.1042 mL 0.2083 mL 0.5208 mL
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    YM-254890 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:

    YM-254890568580-02-9YM254890YM 254890P2Y ReceptorGq-proteinG11-proteinP2Y1ChromobacteriumplateletaggregationADPcalciummobilizationpulmonaryhypertensionInhibitorinhibitorinhibit

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