YM-254890
Based on 18 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.18%
- No. CAS: 568580-02-9
- Fòrmula: C46H69N7O15
- Peso molecular:960.08
-
Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) YM-254890
More- Cell. 2026 Jan 22;189(2):640-658.e22. [Abstract]
- Cell. 2023 Nov 22;186(24):5347-5362.e24. [Abstract]
- J Hematol Oncol. 2024 Feb 24;17(1):9. [Abstract]
- Nat Commun. 2025 Dec 8;16(1):10938. [Abstract]
- Cell Rep Med. 2024 Feb 20;5(2):101388. [Abstract]
- Mucosal Immunol. 2020 Nov;13(6):931-945. [Abstract]
- J Autoimmun. 2023 Apr:136:103012. [Abstract]
- J Agric Food Chem. 2026 Apr 22;74(15):12132-12144. [Abstract]
- J Agric Food Chem. 2025 Apr 25. [Abstract]
- JCI Insight. 2024 Feb 15;9(6):e171609. [Abstract]
- Food Funct. 2025 Mar 26. [Abstract]
- Front Pharmacol. 2024 Jul 31:15:1389761. [Abstract]
- Mol Neurobiol. 2025 Feb;62(2):1826-1839. [Abstract]
- FASEB J. 2025 Apr 30;39(8):e70544. [Abstract]
- J Neurochem. 2025 Dec;169(12):e70334. [Abstract]
- Arch Biochem Biophys. 2025 Mar 27:768:110404. [Abstract]
- Curr Eye Res. 2025 Jun 24:1-9. [Abstract]
- University of Michigan. 2023 Sep.
Customer Validation & Images
-
Others
-
Flow Cytometry
-
Cell Proliferation/Viability Assay
-
WB
-
Bio/Physico-chemical Assay
Ver todos los productos específicos de isoformas P2Y Receptor
More
Actividad biológica
|
P2Y1 Receptor |
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.
Chemical Information
-
No. CAS 568580-02-9
-
Appearance Solid
-
Peso molecular 960.08
-
Fòrmula C46H69N7O15
-
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
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (18)
-
Journal Impact Factor
-
Most Recent
-
Cell
2026 Jan 22;189(2):640-658.e22. PMID: 41270732 -
Cell
2023 Nov 22;186(24):5347-5362.e24. PMID: 37963465
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).
-
J Hematol Oncol
2024 Feb 24;17(1):9. PMID: 38402237
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).
-
Nat Commun
Discovery of a β-arrestin-biased CCKBR agonist that blocks CCKBR-dependent long-term potentiation. [Abstract]2025 Dec 8;16(1):10938. PMID: 41360797
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.
-
Cell Rep Med
Cholinergic signaling via muscarinic M1 receptor confers resistance to docetaxel in prostate cancer. [Abstract]2024 Feb 20;5(2):101388. PMID: 38262412
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).
-
Mucosal Immunol
ADP/P2Y1 aggravates inflammatory bowel disease through ERK5-mediated NLRP3 inflammasome activation. [Abstract]2020 Nov;13(6):931-945. PMID: 32518369 -
J Autoimmun
Signal responses to neutral TSH receptor antibody - A cycle of damage in the pathophysiology of Graves' disease. [Abstract]2023 Apr:136:103012. PMID: 36898184 -
J Agric Food Chem
Preventive Effect of Caffeic Acid Phenethyl Ester, an Active Component of Propolis, against TNF-α-Induced Endothelial Dysfunction through the β2-Adrenoceptor-Mediated eNOS/NO Signal Pathway. [Abstract]2026 Apr 22;74(15):12132-12144. PMID: 41957988 -
J Agric Food Chem
Novel Cholecystokinin Secretion-Stimulating Peptides from Oat Protein Hydrolysate: Sequence Identification and Insight into the Mechanism of Action. [Abstract]2025 Apr 25. PMID: 40275796 -
JCI Insight
Molecular mechanism responsible for sex differences in electrical activity of mouse pancreatic β cells. [Abstract]2024 Feb 15;9(6):e171609. PMID: 38358819 -
Food Funct
Bioactive peptides from barley protein hydrolysate stimulate cholecystokinin secretion via calcium-sensing receptor signaling in enteroendocrine cells. [Abstract]2025 Mar 26. PMID: 40134323 -
Front Pharmacol
N-demethylsinomenine metabolite and its prototype sinomenine activate mast cells via MRGPRX2 and aggravate anaphylaxis. [Abstract]2024 Jul 31:15:1389761. PMID: 39144634 -
Mol Neurobiol
Apelin Receptor Homodimerisation Inhibits Hippocampal Neuronal Autophagy via G Protein-Dependent Signalling in Vascular Dementia. [Abstract]2025 Feb;62(2):1826-1839. PMID: 39042220 -
FASEB J
Gαq/11 Signaling Modulates Fibroblast Growth Factor 23 Production and Contributes to Acute Kidney Injury. [Abstract]2025 Apr 30;39(8):e70544. PMID: 40275688 -
J Neurochem
Beta-Arrestin2-Biased Activation by Pilocarpine Suppresses Microglial Inflammatory Response. [Abstract]2025 Dec;169(12):e70334. PMID: 41457680 -
Arch Biochem Biophys
The odorant (R)-(-)-carvone promotes glucose-stimulated insulin secretion via the olfactory receptor Olfr1259 in pancreatic β-TC6 cells. [Abstract]2025 Mar 27:768:110404. PMID: 40157529 -
Curr Eye Res
Kisspeptin Suppresses the Growth of Primary Pterygial Cells via Inhibiting Chemokine (C-X-C Motif) Ligands in Microenvironment. [Abstract]2025 Jun 24:1-9. PMID: 40555256 -
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 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.
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.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
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.
Pureza y Documentación
-
Ficha de datos (282 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Taniguchi M, et al. YM-254890, a novel platelet aggregation inhibitor produced by Chromobacterium sp. QS3666. J Antibiot (Tokyo). 2003 Apr;56(4):358-63. [Content Brief]
[2]. Zhang H, et al. Structure-activity relationship and conformational studies of the natural product cyclic depsipeptides YM-254890 and FR900359. Eur J Med Chem. 2018 Aug 5;156:847-860. [Content Brief]
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 |
YM-254890 Related Classifications
HY-111557 Related Classifications
Powered by Bioz