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ly303  (MedChemExpress)


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    MedChemExpress ly303
    Effects of LY294 and <t>LY303</t> on Ca 2+ signaling in HEK/5-HT 2C cells. (A) Representative recording of intracellular Ca 2+ in an individual Fura-2-loaded HEK/5-HT 2C cell showing that 3 μM LY294 reversibly inhibited Ca 2+ signals elicited by 4 nM serotonin, while 3 μM LY303 induced agonist-like Ca 2+ transients (N = 215). Here and in the below figures, applications of compounds are indicated by the straight-line segments above the experimental traces. Deviations of cytosolic Ca 2+ in individual cells loaded with Fura-2 are presented as the ratio F 340 / F 380 , where F 340 and F 380 are the instant intensity of cell fluorescence upon excitation at 340 nm and 380 nm, respectively. (B, C) Fractions of HEK/5-HT 2C cells responsive to (B) 4 nM serotonin as a function of LY294 concentration (N = 108–379) and (C) LY303 at varied doses (N = 31–196). The experimental data (filled circles) are presented as a mean ± S.D. The solid curves represent the approximation of the experimental data with the at n = 1.30 and C 0.5 = 1.24 (B) and with at n = 2.20 and C 0.5 = 2.51 (C).
    Ly303, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 93/100, based on 3 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
    https://www.bioz.com/result/ly303/product/MedChemExpress
    Average 93 stars, based on 3 article reviews
    ly303 - by Bioz Stars, 2026-02
    93/100 stars

    Images

    1) Product Images from "Serotonin 5-HT 2C receptor as a cellular target of PI3K inhibitor LY294002 and its analog LY303511"

    Article Title: Serotonin 5-HT 2C receptor as a cellular target of PI3K inhibitor LY294002 and its analog LY303511

    Journal: bioRxiv

    doi: 10.1101/2025.11.06.687025

    Effects of LY294 and LY303 on Ca 2+ signaling in HEK/5-HT 2C cells. (A) Representative recording of intracellular Ca 2+ in an individual Fura-2-loaded HEK/5-HT 2C cell showing that 3 μM LY294 reversibly inhibited Ca 2+ signals elicited by 4 nM serotonin, while 3 μM LY303 induced agonist-like Ca 2+ transients (N = 215). Here and in the below figures, applications of compounds are indicated by the straight-line segments above the experimental traces. Deviations of cytosolic Ca 2+ in individual cells loaded with Fura-2 are presented as the ratio F 340 / F 380 , where F 340 and F 380 are the instant intensity of cell fluorescence upon excitation at 340 nm and 380 nm, respectively. (B, C) Fractions of HEK/5-HT 2C cells responsive to (B) 4 nM serotonin as a function of LY294 concentration (N = 108–379) and (C) LY303 at varied doses (N = 31–196). The experimental data (filled circles) are presented as a mean ± S.D. The solid curves represent the approximation of the experimental data with the at n = 1.30 and C 0.5 = 1.24 (B) and with at n = 2.20 and C 0.5 = 2.51 (C).
    Figure Legend Snippet: Effects of LY294 and LY303 on Ca 2+ signaling in HEK/5-HT 2C cells. (A) Representative recording of intracellular Ca 2+ in an individual Fura-2-loaded HEK/5-HT 2C cell showing that 3 μM LY294 reversibly inhibited Ca 2+ signals elicited by 4 nM serotonin, while 3 μM LY303 induced agonist-like Ca 2+ transients (N = 215). Here and in the below figures, applications of compounds are indicated by the straight-line segments above the experimental traces. Deviations of cytosolic Ca 2+ in individual cells loaded with Fura-2 are presented as the ratio F 340 / F 380 , where F 340 and F 380 are the instant intensity of cell fluorescence upon excitation at 340 nm and 380 nm, respectively. (B, C) Fractions of HEK/5-HT 2C cells responsive to (B) 4 nM serotonin as a function of LY294 concentration (N = 108–379) and (C) LY303 at varied doses (N = 31–196). The experimental data (filled circles) are presented as a mean ± S.D. The solid curves represent the approximation of the experimental data with the at n = 1.30 and C 0.5 = 1.24 (B) and with at n = 2.20 and C 0.5 = 2.51 (C).

    Techniques Used: Fluorescence, Concentration Assay

    Activity of LY294 and LY303 against PI3K. (A) Experimental protocol timing. The applications of LY294 or LY303, and insulin are indicated by the line segments above the time axis; the moments of image capturing are indicated by the yellow arrows. (B, C) Representative sequential images of HEK/PH(Akt)-Venus cells obtained at the moments indicated in (A). The left panels , control images of the group of cells obtained right before drug application demonstrate the virtually homogeneous distribution of PH(Akt)-Venus fluorescence over cell bodies. The middle panels , stimulation of cells with 100 nM insulin in the presence of 30 μM LY294 negligibly affected PH(Akt)-Venus distribution compared to control (B), while in the presence of 30 μM LY303 insulin initiated a drop in the fluorescence of the cell cytosol and the appearance of detectable stripe-like fluorescent zones indicated by the white arrows (C), suggesting the insulin-induced accumulation of the PH(Akt)-Venus sensor in the plasmalemma. The right panels, images obtained after LY294 or LY303 washing out and subsequent stimulation with insulin.
    Figure Legend Snippet: Activity of LY294 and LY303 against PI3K. (A) Experimental protocol timing. The applications of LY294 or LY303, and insulin are indicated by the line segments above the time axis; the moments of image capturing are indicated by the yellow arrows. (B, C) Representative sequential images of HEK/PH(Akt)-Venus cells obtained at the moments indicated in (A). The left panels , control images of the group of cells obtained right before drug application demonstrate the virtually homogeneous distribution of PH(Akt)-Venus fluorescence over cell bodies. The middle panels , stimulation of cells with 100 nM insulin in the presence of 30 μM LY294 negligibly affected PH(Akt)-Venus distribution compared to control (B), while in the presence of 30 μM LY303 insulin initiated a drop in the fluorescence of the cell cytosol and the appearance of detectable stripe-like fluorescent zones indicated by the white arrows (C), suggesting the insulin-induced accumulation of the PH(Akt)-Venus sensor in the plasmalemma. The right panels, images obtained after LY294 or LY303 washing out and subsequent stimulation with insulin.

    Techniques Used: Activity Assay, Control, Fluorescence

    The effects of LY303511 on activity of signaling molecules pivotal in serotonin transduction. (A) The effect of LY303511 (LY303) on IP 3 Rs activity. Left panel, representative recording of Ca 2+ transients elicited by IP 3 uncaging in an individual HEK293 cell in control and after pretreatment with 25 μM LY303. Сells were loaded with both caged-Ins(145)P3 for IP 3 uncaging and Fluo-8 for Ca 2+ imaging. IP 3 uncaging was stimulated by 0.8-s UV flashes, which produced optical artifacts that appeared as a marked overshoot in the fluorescence traces. Right panel, averaged fractions of cells responsive to IP 3 uncaging in control and in the presence of 25 μM LY303 (N = 300). Here and in the other right panels, the data are presented as a mean ± S.D. at the indicated numbers of cells. Paired t-test (p values in the graph). (B) The effect of LY303 on PLC activity. Left panel, representative recording of Ca 2+ signals in an individual HEK293 cell induced by 50 μM PLC activator m-3M3FBS in control and after pretreatment with 25 μM LY303 alone or in combination with 3 μM PKA inhibitor H89. Right panel, normalized magnitudes of Ca 2+ signals induced by 50 μM m-3M3FBS under the indicated conditions (N = 65). For each individual cell, its response to 50 μM m-3M3FBS in control was taken as a unit. One-way repeated measures ANOVA with Holm-Sidak post-hoc test (p values in the graph). (C) The effect of LY303 on the phosphoinositide cascade triggered by purinergic GPCR. Left panel, representative recording of Ca 2+ transients induced by 2 μM ATP in an individual HEK293 cell in control and after pretreatment with 25 μM LY303. Right panel, the averaged fractions of ATP-responsive cells (N = 300). Paired t-test (p values in the graph).
    Figure Legend Snippet: The effects of LY303511 on activity of signaling molecules pivotal in serotonin transduction. (A) The effect of LY303511 (LY303) on IP 3 Rs activity. Left panel, representative recording of Ca 2+ transients elicited by IP 3 uncaging in an individual HEK293 cell in control and after pretreatment with 25 μM LY303. Сells were loaded with both caged-Ins(145)P3 for IP 3 uncaging and Fluo-8 for Ca 2+ imaging. IP 3 uncaging was stimulated by 0.8-s UV flashes, which produced optical artifacts that appeared as a marked overshoot in the fluorescence traces. Right panel, averaged fractions of cells responsive to IP 3 uncaging in control and in the presence of 25 μM LY303 (N = 300). Here and in the other right panels, the data are presented as a mean ± S.D. at the indicated numbers of cells. Paired t-test (p values in the graph). (B) The effect of LY303 on PLC activity. Left panel, representative recording of Ca 2+ signals in an individual HEK293 cell induced by 50 μM PLC activator m-3M3FBS in control and after pretreatment with 25 μM LY303 alone or in combination with 3 μM PKA inhibitor H89. Right panel, normalized magnitudes of Ca 2+ signals induced by 50 μM m-3M3FBS under the indicated conditions (N = 65). For each individual cell, its response to 50 μM m-3M3FBS in control was taken as a unit. One-way repeated measures ANOVA with Holm-Sidak post-hoc test (p values in the graph). (C) The effect of LY303 on the phosphoinositide cascade triggered by purinergic GPCR. Left panel, representative recording of Ca 2+ transients induced by 2 μM ATP in an individual HEK293 cell in control and after pretreatment with 25 μM LY303. Right panel, the averaged fractions of ATP-responsive cells (N = 300). Paired t-test (p values in the graph).

    Techniques Used: Activity Assay, Transduction, Control, Imaging, Produced, Fluorescence

    Evidence for LY303 as an agonist of the 5-HT 2C receptor. (A–D) Representative recordings of intracellular Ca 2+ in individual Fura-2-loaded cells. (A) Ca 2+ signals elicited by 2 μM LY303 in HEK/5-HT 2C cells were weakly affected by the reduction of bath Ca 2+ from 2 mM to 260 nM but those were suppressed by 2 μM PLC inhibitor U73122 (N = 64). (B) Parental HEK293 cells were not responsive to serotonin as well as LY303 with Ca 2+ transients, while their functionality was validated by robust responses to 1 μM acetylcholine (ACh) (N = 241). (C) Ca 2+ signals initiated by 2 μM LY303 in HEK/5-HT 2C cells were inhibited in the presence of 300 nM 5-HT 2C receptor antagonist RS102221 (N = 21). (D) Ca 2+ signals initiated by 2 μM LY303 in HEK/5-HT 2C cells were inhibited in the presence of 5 μM LY294 (N = 36).
    Figure Legend Snippet: Evidence for LY303 as an agonist of the 5-HT 2C receptor. (A–D) Representative recordings of intracellular Ca 2+ in individual Fura-2-loaded cells. (A) Ca 2+ signals elicited by 2 μM LY303 in HEK/5-HT 2C cells were weakly affected by the reduction of bath Ca 2+ from 2 mM to 260 nM but those were suppressed by 2 μM PLC inhibitor U73122 (N = 64). (B) Parental HEK293 cells were not responsive to serotonin as well as LY303 with Ca 2+ transients, while their functionality was validated by robust responses to 1 μM acetylcholine (ACh) (N = 241). (C) Ca 2+ signals initiated by 2 μM LY303 in HEK/5-HT 2C cells were inhibited in the presence of 300 nM 5-HT 2C receptor antagonist RS102221 (N = 21). (D) Ca 2+ signals initiated by 2 μM LY303 in HEK/5-HT 2C cells were inhibited in the presence of 5 μM LY294 (N = 36).

    Techniques Used:

    Docking-predicted conformations of the 5-HT 2C receptor in complex with serotonin (A), LY294 (B), and LY303 (C). TM4, TM6, and TM7 are 4th, 6th, and 7th transmembrane helices, respectively. As can be seen, both serotonin and the LY-compounds localize in the transmembrane cavity, although serotonin’s position is closer to the geometric center of the receptor than positions of LY294 and LY303. Binding poses of LY294 and LY303 practically coincide, which perhaps is not unexpected, given how structurally similar they are.
    Figure Legend Snippet: Docking-predicted conformations of the 5-HT 2C receptor in complex with serotonin (A), LY294 (B), and LY303 (C). TM4, TM6, and TM7 are 4th, 6th, and 7th transmembrane helices, respectively. As can be seen, both serotonin and the LY-compounds localize in the transmembrane cavity, although serotonin’s position is closer to the geometric center of the receptor than positions of LY294 and LY303. Binding poses of LY294 and LY303 practically coincide, which perhaps is not unexpected, given how structurally similar they are.

    Techniques Used: Binding Assay

    Molecular dynamics snapshots taken from the trajectories at 25, 50, and 100 ns generated for the 5-HT 2C receptor in complexes with serotonin, LY294, and LY303. Frame labeled as “final” represents the end state of the structures after modeling with accelerated molecular dynamics. In all simulations, docking-predicted conformations were used as the initial structures As can be seen, serotonin and the LY-compounds by and large remained in their initial locations.
    Figure Legend Snippet: Molecular dynamics snapshots taken from the trajectories at 25, 50, and 100 ns generated for the 5-HT 2C receptor in complexes with serotonin, LY294, and LY303. Frame labeled as “final” represents the end state of the structures after modeling with accelerated molecular dynamics. In all simulations, docking-predicted conformations were used as the initial structures As can be seen, serotonin and the LY-compounds by and large remained in their initial locations.

    Techniques Used: Generated, Labeling



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