Recettore degli androgeni
Il recettore degli androgeni (AR) è un recettore ormonale nucleare che viene attivato dal legame con gli androgeni, come il testosterone e il diidrotestosterone. Questo recettore svolge un ruolo cruciale nello sviluppo e nel mantenimento delle caratteristiche maschili, nonché nella regolazione di diversi processi fisiologici, tra cui la crescita muscolare, la libido e la densità ossea. Gli inibitori del recettore degli androgeni sono ampiamente studiati nel contesto del cancro alla prostata, dove la segnalazione dell'AR è spesso sovraregolata. Presso CymitQuimica, offriamo una gamma di modulatori del recettore degli androgeni di alta qualità per supportare la tua ricerca in endocrinologia, biologia del cancro e regolazione ormonale.
Trovati 229 prodotti di "Recettore degli androgeni"
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SC428
CAS:SC428 acts as an inhibitor of the androgen receptor (AR), specifically targeting the N-terminal domain of AR. This compound effectively diminishes the transactivation of various AR forms, including AR-V7, ARv567es, full-length AR (AR-FL), and its LBD mutants. Additionally, SC428 significantly inhibits AR-FL nuclear translocation, chromatin binding, and AR-regulated gene transcription under androgen stimulation. In vitro, SC428 suppresses the proliferation of tumor cells. In vivo, it inhibits tumor growth in mice transplanted with 22Rv1 cells by inducing apoptosis.Formula:C15H10F3N3OSColore e forma:SolidPeso molecolare:337.32ERβ agonist-1
CAS:<p>ERβagonist-1 (Compound 8) functions as a dual-active selective ERβ agonist (EC50: 46.8 nM) and an AR antagonist (IC50: 1555 nM). By binding to ERβ, it activates its signaling pathways while simultaneously inhibiting AR activity. Retaining selective ERβ agonist activity in mouse models, ERβagonist-1 is applicable in prostate cancer research.</p>Formula:C25H36O2Colore e forma:SolidPeso molecolare:368.55GLPG0492 (R enantiomer)
CAS:GLPG0492 R enantiomer is the R enantiomer of GLPG-0492, a novel selective androgen receptor modulator.Formula:C19H14F3N3O3Colore e forma:SolidPeso molecolare:389.33JNJ-1250132
CAS:JNJ-1250132 is a steroidal progesterone receptor modulator that inhibits binding of the receptor to DNA in vitro.Formula:C33H41NO4Colore e forma:SolidPeso molecolare:515.68ID11916
CAS:<p>ID11916 is an orally active compound functioning as both an androgen receptor (AR) antagonist and a phosphodiesterase 5 (PDE5) inhibitor. It disrupts androgen binding to AR, impedes nuclear translocation, and blocks androgen-dependent transcriptional activity of AR, while simultaneously elevating intracellular cGMP levels by inhibiting PKG activation. Moreover, ID11916 exhibits potent anticancer effects in prostate cancer cell lines VCaP and 22Rv1, as well as in AR-positive breast cancer cell line SK-BR-3.</p>Formula:C29H27F3N8O3SColore e forma:SolidPeso molecolare:624.637AR antagonist 11
CAS:AR antagonist 11 (Compound c2) is a selective androgen receptor antagonist with an IC50 of 0.019 μM. It is also effective against the ARF877L/T878A mutant (IC50: 1.03 μM). Additionally, AR antagonist 11 inhibits LNCaP cell proliferation and decreases PSA protein expression (IC50: 0.54 μM). This compound is applicable in prostate cancer (PCa) research.Formula:C20H17ClN2OColore e forma:SolidPeso molecolare:336.815AR antagonist 4
AR antagonist 4 (Compound 67-b) is an orally active androgen receptor (AR) antagonist that acts on wild-type AR (IC50: 246.6 nM).Formula:C29H36N4OColore e forma:SolidPeso molecolare:456.62AR/BET protein degrader-1
CAS:AR/BET protein degrader-1 (Compound 149) is a dual-targeting protein degrader of Androgen Receptor and BET (bromodomain and extra-terminal domain), suitable for cancer research.Formula:C43H44N6O5Peso molecolare:724.85Androgen receptor antagonist 13
CAS:Androgen receptor antagonist 13 (compound 8a) is an orally active androgen receptor antagonist with an IC50 of 0.20 μM. It is used in prostate cancer research.Formula:C16H15N3O3SColore e forma:SolidPeso molecolare:329.37VNPP433-3β
CAS:VNPP433-3β acts as a molecular glue degrader, targeting the androgen receptor (AR) and its splice variants (AR-Vs) as well as MAP kinase-interacting serine/threonine protein kinase Mnk1/2. It effectively inhibits the proliferation of cancer cells LNCaP, C4-2B, and CWR22Rv1, with GI50 values of 0.2, 0.3, and 0.31 μM, respectively. Additionally, VNPP433-3β shows favorable pharmacokinetics in CD-1 mice and suppresses tumor growth in the CWR22Rv1 xenograft mouse model.Formula:C29H34N4Colore e forma:SolidPeso molecolare:438.61EN1441
CAS:EN1441 is a covalent degrader that targets the androgen receptor (AR) with an EC50 value of 4.2 μM, as well as its truncated variant AR-V7. It selectively and effectively degrades AR and AR-V7 in androgen-independent prostate cancer cells. EN1441 holds potential for research into androgen-independent prostate cancer.Formula:C13H13ClN2O2Colore e forma:SolidPeso molecolare:264.708(Rac)-Idroxioleic acid sodium
CAS:(Rac)-Idroxioleic acid (2-Hydroxyoleic acid) sodium is a synthetic derivative of oleic acid (OA) that binds to the plasma membrane, altering lipid composition. This compound exhibits antitumor properties.Formula:C18H33NaO3Colore e forma:SolidPeso molecolare:320.44ZNU-IMB-Z15
CAS:Compound Z15 (ZNU-IMB-Z15) acts as an antagonist and degrader of the androgen receptor (AR). It inhibits the proliferation of castration-resistant prostate cancer (CRPC) cell lines that are AR-positive and induces apoptosis. Compound Z15 exhibits anticancer activity both in vivo and in vitro.Formula:C20H17N3O3S2Colore e forma:SolidPeso molecolare:411.5Androgen receptor degrader-5
CAS:Androgen receptor degrader-5 (compound 14k) demonstrates superior capabilities, specifically in androgen receptor degradation and antiproliferative activity, showcasing its promising properties.Formula:C29H25F4N5O2Colore e forma:SolidPeso molecolare:551.53AR antagonist 10
CAS:AR antagonist 10 (Compound Y5) is a potent, orally active androgen receptor (AR) antagonist with an IC50 value of 0.04 μM. It demonstrates a dual mechanism of action: antagonizing AR by disrupting AR dimerization and inducing AR degradation through the ubiquitin-proteasome pathway. This compound shows excellent activity against various resistant AR mutants and effectively inhibits the growth of LNCaP xenograft tumors. AR antagonist 10 is applicable for research in resistant prostate cancer.Formula:C18H17ClN4O3SColore e forma:SolidPeso molecolare:404.871A4B17
A4B17 is an inhibitor of androgen receptor N-terminal with potential for androgen-responsive prostate cancer treatment.Formula:C14H7F4NSColore e forma:SolidPeso molecolare:297.27Androgen receptor antagonist 12
CAS:Compound EF2 (Androgen receptor antagonist 12) is an orally active antagonist of the androgen receptor (AR) with an IC50 of 0.30 µM. It inhibits the transcriptional activity of mutant AR and the proliferation of AR-positive PCa (prostate cancer) cell lines. Additionally, Compound EF2 blocks the nuclear translocation of AR and suppresses tumor growth in the C4-2B xenograft mouse model. This compound is used for research in prostate cancer.Formula:C12H8F3N3O2Colore e forma:SolidPeso molecolare:283.21SJ1008066
CAS:SJ1008066 is a MAGE-A11 inhibitor with an IC50 of 0.13 μM. It binds to the MAGE homology domain (MHD) and disrupts the MAGE-A11:PCF11 interaction.Formula:C21H22N4Colore e forma:SolidPeso molecolare:330.43Androgen receptor ligand 1
CAS:Androgen receptorligand 1 is a ligand for the androgen receptor (AR). It interacts with the CRBN E3 ligase via a linker to form an AR-PROTAC degrader. This compound is useful in prostate cancer research.Formula:C19H16F4N2OColore e forma:SolidPeso molecolare:364.34(+)-JJ-74-138
CAS:(+)-JJ-74-138 is a novel non-competitive androgen receptor (AR) antagonist capable of inhibiting enzalutamide-resistant castration-resistant prostate cancer (CRPC).Formula:C22H22F8N2OSColore e forma:SolidPeso molecolare:514.48
