YM-254890

(HB6283)

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Product overview

Name YM-254890
Purity >98%
Description

Potent Gq/11 signaling inhibitor. Reported as Gq- G-protein inhibitor and broad-spectrum inhibitor for Gq- and Gs-proteins.

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Biological Data

Biological description

Gq- G-protein inhibitor which potently inhibits Gq/11 heterotrimeric G protein signaling by blocking GDP exchange of GTP on the α- subunit of the Gq complex. Recently reported to act as a broad-spectrum inhibitor for Gq- and Gs-proteins and exhibits a biased inhibition on Gi/o signaling, without affecting non-GPCR-mediated cellular signaling (Peng et al 2021). Shown to attenuate ADP-, collagen-, TRAP-, arachidonic acid- and U46619-induced platelet aggregation to show antithrombotic effects.

Solubility & Handling

Solubility overview

Soluble in DMSO (10mg/ml)

Storage instructions

-20°C

Storage of solutions Prepare and use solutions on the same day if possible. Store solutions at -20°C for up to one month if storage is required. Equilibrate to RT and ensure the solution is precipitate free before use.
Shipping Conditions Stable for ambient temperature shipping. Follow storage instructions on receipt.
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use

Calculators

Molarity

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Dilution

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Chemical Data

Purity >98%
Chemical name

[(1R)-1-[(3S,6S,9S,12S,18R,21S,22R)-21-acetamido-18-benzyl-3-[(1R)-1-methoxyethyl]-4,9,10,12,16,22-hexamethyl-15-methylidene-2,5,8,11,14,17,20-heptaoxo-1,19-dioxa-4,7,10,13,16-pentazacyclodocos-6-yl]-2-methylpropyl] (2S,3R)-2-acetamido-3-hydroxy-4-methylpentanoate

Molecular Weight 960.1
Molecular Formula C46H69N7O15
CAS Number 568580-02-9
PubChem identifier 9919454
SMILES C[C@@H]1[C@@H](C(=O)O[C@@H](C(=O)N(C(=C)C(=O)N[C@H](C(=O)N([C@H](C(=O)N[C@H](C(=O)N([C@H](C(=O)O1)[C@@H](C)OC)C)[C@@H](C(C)C)OC(=O)[C@H]([C@@H](C(C)C)O)NC(=O)C)C)C)C)C)CC2=CC=CC=C2)NC(=O)C
Source Chromobacterium sp.
InChi InChI=1S/C46H69N7O15/c1-22(2)37(56)34(49-30(11)55)45(63)68-38(23(3)4)35-43(61)53(14)36(28(9)65-15)46(64)66-27(8)33(48-29(10)54)44(62)67-32(21-31-19-17-16-18-20-31)42(60)52(13)25(6)39(57)47-24(5)41(59)51(12)26(7)40(58)50-35/h16-20,22-24,26-28,32-38,56H,6,2
InChiKey QVYLWCAYZGFGNF-WBWCVGBTSA-N

References for YM-254890

References are publications that support the biological activity of the product
  • Functional evidence for biased inhibition of G protein signaling by YM-254890 in human coronary artery endothelial cells

    Peng et al (2021) Eur J Pharmacol. 173706 : 891
  • Structural and Dynamical Basis of G Protein Inhibition by YM-254890 and FR900359: An Inhibitor in Action

    Tietze et al (2019) J Chem Inf Model. 59(10) : 4361-4373
  • Effect of YM-254890, a specific Galphaq/11 inhibitor, on experimental peripheral arterial disease in rats

    Uemura et al (2006) Eur J Pharmacol. 536(1-2) : 154-61
  • Biological properties of a specific Galpha q/11 inhibitor, YM-254890, on platelet functions and thrombus formation under high-shear stress

    Uemura et al (2006) Br J Pharmacol. 148(1) : 61-9
  • Pharmacological properties of YM-254890, a specific G(alpha)q/11 inhibitor, on thrombosis and neointima formation in mice

    Kawasaki et al (2005) Thromb Haemost. 94(1) : 184-92.

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