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

YM-254890 

Cat. No.: HY-111557 Purity: >95.0%
Handling Instructions

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.

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YM-254890 Chemical Structure

YM-254890 Chemical Structure

CAS No. : 568580-02-9

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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

Gαq/11 protein[1][2]

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].

Molecular Weight

960.08

Formula

C₄₆H₆₉N₇O₁₅

CAS No.

568580-02-9

SMILES

CN([[email protected]@H](C)C(N[[email protected]@H]([[email protected]](OC([[email protected]@H](NC(C)=O)[[email protected]@H](C(C)C)O)=O)C(C)C)C(N(C)[[email protected]@H]([[email protected]](OC)C)C(O[[email protected]@H]1C)=O)=O)=O)C([[email protected]](C)NC(C(N(C([[email protected]@H](CC2=CC=CC=C2)OC([[email protected]]1NC(C)=O)=O)=O)C)=C)=O)=O

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Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >95.0%

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Keywords:

YM-254890YM254890YM 254890P2Y ReceptorGq-proteinG11-proteinP2Y1ChromobacteriumplateletaggregationADPcalciummobilizationpulmonaryhypertensionInhibitorinhibitorinhibit

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