G-<wbr/>36

G-36

CAT N°: 14397
Price:

From 48.00 40.80

G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens.{23445} It is thought to be involved in estrogen-sensitive cancers.{23445,23446} GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth.{23445} G-36 is a cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17?-estradiol (Item No. 10006315) or the GPER-selective agonist G-1 (Item No. 10008933) (IC50 = 112 and 165 nM, respectively).{23443} It has no detectable binding activity to either ER? or ER?.{23443} G-36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF.{23443} G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ER? and ER? in complex biological systems.{23443,24423}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • (4S)-rel-4-(6-bromo-1,3-benzodioxol-5-yl)-3aR,4,5,9bS-tetrahydro-8-(1-methylethyl)-3H-cyclopenta[c]quinoline
  • Correlated keywords
    • receptors antagonists steroids endocrinology biochemistry cancers diabetes bone-related research bones related G proteins coupled estrogens GPR30 GPR-30 GPRs 30 GPERs cell-permeable cells permeables non-steroidal nonsteroidal non steroidal 17?-estradiol 17beta-estradiol 17.beta.-estradiol 17b-estradiol estradiol G1 G-1 Gs 1 36 G36 ERs Er? ER? ERalpha ERbeta ER.alpha. ER.beta. Era ERb ERKs EGFs
  • Product Overview:
    G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens.{23445} It is thought to be involved in estrogen-sensitive cancers.{23445,23446} GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth.{23445} G-36 is a cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17?-estradiol (Item No. 10006315) or the GPER-selective agonist G-1 (Item No. 10008933) (IC50 = 112 and 165 nM, respectively).{23443} It has no detectable binding activity to either ER? or ER?.{23443} G-36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or G-1 but not by EGF.{23443} G-36 can be used in combination with GPER-selective agonists, like G-1, to distinguish the roles of GPER from those of ER? and ER? in complex biological systems.{23443,24423}

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