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Pathways Recommended: Vitamin D Related/Nuclear Receptor
Results for "

nuclear transcription

" in MedChemExpress (MCE) Product Catalog:

77

Inhibitors & Agonists

3

Screening Libraries

7

Peptides

13

Natural
Products

1

Recombinant Proteins

6

Isotope-Labeled Compounds

31

Antibodies

5

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-120855
    CCG-100602
    2 Publications Verification

    Ras Cardiovascular Disease
    CCG-100602 is a specific inhibitor of myocardin-related transcription factor A/serum response factor (MRTF-A/SRF) signaling. CCG-100602 specifically block MRTF-A nuclear localization and thus inhibit the fibrogenic transcription factor SRF .
    CCG-100602
  • HY-N0866
    20-Deoxyingenol
    4 Publications Verification

    Autophagy Inflammation/Immunology
    20-Deoxyingenol, a diterpene, is isolated from the roots of Euphorbia kansui. 20-Deoxyingenol can promote autophagy and lysosomal biogenesis by promoting the nuclear translocation of transcription factor EB (TFEB) in vitro. 20-Deoxyingenol can be used for the research of osteoarthritis (OA) .
    20-Deoxyingenol
  • HY-44062

    Histone Methyltransferase Inflammation/Immunology Cancer
    G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer .
    G9a-IN-1
  • HY-124500
    AC-4-130
    5 Publications Verification

    STAT Apoptosis Cancer
    AC-4-130 is a potent STAT5 SH2 domain inhibitor. AC-4-130 directly binds to STAT5 and disrupts STAT5 activation, dimerization, nuclear translocation, and STAT5-dependent gene transcription. AC-4-130 induces cell cycle arrest and apoptosis in FLT3-ITD-driven leukemic cells. AC-4-130 has anti-cancer activity and can efficiently block pathological levels of STAT5 activity in acute myeloid leukemia (AML) .
    AC-4-130
  • HY-107494A

    all-trans 4-Keto Retinoic Acid

    Endogenous Metabolite Metabolic Disease
    all-trans-4-Oxoretinoic acid, an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).
    all-trans-4-Oxoretinoic acid
  • HY-136741
    BOT-64
    1 Publications Verification

    IKK Inflammation/Immunology
    BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC50 of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription .
    BOT-64
  • HY-176347S

    Isotope-Labeled Compounds Cancer
    Alpha Feto Protein, Arg- 13C36, 15N4, Lys- 13C6, 15N2 is the 13C- and 15N-labeled Alpha Feto Protein.
    Alpha Feto Protein, Arg-13C6,15N4, Lys-13C6,15N2
  • HY-164445

    STAT Cancer
    STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
    STAT3-IN-32
  • HY-174575

    mRNA Cancer
    Human MYOD1 mRNA encodes the human myogenic differentiation 1 (MYOD1) protein, a nuclear protein that belongs to the basic helix-loop-helix family of transcription factors and the myogenic factors subfamily. MYOD1 acts as a transcriptional activator that promotes transcription of muscle-specific target genes and plays a role in muscle differentiation.
    Human MYOD1 mRNA
  • HY-174568

    mRNA Inflammation/Immunology
    Human NFKB2 mRNA encodes the human nuclear factor kappa B subunit 2 (NFKB2) protein, a subunit of the transcription factor complex nuclear factor-kappa-B (NFkB). The NFkB complex is expressed in numerous cell types and functions as a central activator of genes involved in inflammation and immune function. NFKB2 can function as either a transcriptional activator or repressor depending on its dimerization partner.
    Human NFKB2 mRNA
  • HY-N6747

    c-Myc Autophagy Cancer
    Stauprimide is a staurosporine analog that promotes embryonic stem cell (ESC) differentiation. Stauprimide is a non-broad spectrum inhibitor that binds to the MYC transcription factor NME2 and blocks its nuclear localization in ESCs, which results in down-regulation of MYC transcription .
    Stauprimide
  • HY-111498A
    RGX-104
    2 Publications Verification

    Abequolixron

    LXR Inflammation/Immunology Cancer
    RGX-104 is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
    RGX-104
  • HY-174577

    mRNA Cancer
    Human MYC mRNA encodes the human MYC proto-oncogene, bHLH transcription factor (MYC) protein, a nuclear phosphoprotein that plays a role in cell cycle progression, apoptosis and cellular transformation.
    Human MYC mRNA
  • HY-174505

    mRNA Cancer
    Human YAP1 mRNA encodes the human Yes1 associated transcriptional regulator (YAP1) protein, a downstream nuclear effector of the Hippo signaling pathway which is involved in development, growth, repair, and homeostasis. YAP1 is known to play a role in the development and progression of multiple cancers as a transcriptional regulator of this signaling pathway and may function as a potential target for cancer treatment.
    Human YAP1 mRNA
  • HY-135572

    Orphan Nuclear Receptor Neurological Disease Cancer
    TLX agonist 1 (ccrp2) is an orphan nuclear receptor tailless (TLX, NR2E1) modulator (EC50=1μM; Kd= 650 nM). TLX agonist 1 potentiates TLX transcriptional repressive activity .
    TLX agonist 1
  • HY-144745

    NF-κB Cancer
    HSR1304 (Compound 5d) is a potent inhibitor of NFκB. The multifunctional transcription factor, nuclear factor-κB (NF-κB), is broadly involved in multiple human diseases, such as cancer and chronic inflammation. HSR1304 has the potential for the research of cancer diseases .
    HSR1304
  • HY-W019721

    Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A . Cyclosporin A is a potent immunosuppressant agent, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc) .
    Cyclosporin D
  • HY-P5458

    Mineralocorticoid Receptor Others
    SRC-1 (686-700) is a biological active peptide. (This peptide is amino acids 686 to 700 fragment containing the second LXXLL motif, derived from NR box II of steroid receptor coactivator (SRC1). Coactivator proteins interact with nuclear receptors in a ligand-dependent manner and augment transcription.)
    SRC-1 (686-700)
  • HY-107494AR

    all-trans 4-Keto Retinoic Acid (Standard)

    Reference Standards Endogenous Metabolite Metabolic Disease
    all-trans-4-Oxoretinoic acid (Standard) is the analytical standard of all-trans-4-Oxoretinoic acid. This product is intended for research and analytical applications. all-trans-4-Oxoretinoic acid, an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).
    all-trans-4-Oxoretinoic acid (Standard)
  • HY-107404

    Orphan Receptor Endocrinology
    SID 7969543 is a selective SF-1 (steroidogenic factor 1, NR5A1) inhibitor with an IC50 of 760 nM. SID 7969543 inhibits SF-1-triggered luciferase expression with IC50 of 30 nM. SF-1 is a transcription factor belonging to the nuclear receptor superfamily .
    SID 7969543
  • HY-P4101

    HIV Infection
    Cys(Npys)-TAT (47-57) is a peptide fragment of TAT peptide and it is able to interact with plasmid DNA electrostatically. Cys(Npys)-TAT (47-57) is corresponding to the transduction domain of TAT with an activated cysteine residue C. TAT is a small nuclear transcriptional activator protein encoded by HIV-1 .
    Cys(Npys)-TAT (47-57)
  • HY-144339
    AhR agonist 2
    1 Publications Verification

    Aryl Hydrocarbon Receptor Others
    AhR agonist 2 (Compound 12a) is a potent agonist of aryl hydrocarbon receptor (AhR) with an EC50 of 0.03 nM. AhR agonist 2 induces rapid nuclear enrichment of AhR, triggers the transcription of downstream genes and promote skin barrier repair. AhR agonist 2 has the potential for the research of psoriasis .
    AhR agonist 2
  • HY-13982
    JSH-23
    Maximum Cited Publications
    118 Publications Verification

    NF-κB Metabolic Disease Inflammation/Immunology Cancer
    JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .
    JSH-23
  • HY-30267
    4-Hydroxyphenyl acetate
    2 Publications Verification

    4-HPA; 4-Acetoxyphenol

    Quinone Reductase Endogenous Metabolite Others
    4-Hydroxyphenyl acetate (4-HPA) is a natural antioxidant and protects cells from oxidative stress-induced necrosis. 4-Hydroxyphenyl acetate blocks the increase of cellular ROS induced by oxidative stress, and up-regulates NQO1 and HO-1 genes by stabilizing and inducing the nuclear translocation of NRF2 transcription factor .
    4-Hydroxyphenyl acetate
  • HY-146027

    Androgen Receptor Cancer
    Androgen receptor antagonist 4 (Compound AT2) is an androgen receptor (AR) antagonist with an IC50 of 0.15 μM. Androgen receptor antagonist 4 efficiently antagonizes AR transcriptional activity, suppresses downstream target gene of AR, and blocks the DHT-induced AR nuclear translocation. Androgen receptor antagonist 4 shows anticancer activities .
    Androgen receptor antagonist 4
  • HY-133552

    ROR Inflammation/Immunology
    RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
    RORγt Inverse agonist 10
  • HY-155543

    Androgen Receptor Cancer
    Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models .
    Anticancer agent 135
  • HY-132243

    Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    NFAT Inhibitor-3 (Compound 10) is a factor nuclear factor of activated T cells (NFAT) inhibitor. NFAT Inhibitor-3 inhibits IL-2 production. NFAT Inhibitor-3 binds in a sequence-selective manner directly to DNA. NFAT Inhibitor-3 can be used for the research of transcription factor dysregulation .
    NFAT Inhibitor-3
  • HY-14649
    Retinoic acid
    95+ Cited Publications

    Vitamin A acid; all-trans-Retinoic acid; ATRA

    Organoid RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
    Retinoic acid
  • HY-403733C

    Androgen Receptor Cancer
    JJ-450 is a non-competitive antagonist androgen receptor (AR) that inhibits the transcriptional activity of wild-type AR and mutant AR F876L. JJ-450 has an IC50 of approximately 1-10 μM in inhibiting AR transcriptional activity in PC3 cells. It is selective for AR binding and does not compete with androgens for binding to the ligand binding domain (LBD) of AR. JJ-450 inhibits the transcriptional activity of AR and its splice variants (such as AR F876L) by inhibiting AR nuclear translocation and promoting the degradation of unliganded AR in the nucleus. JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to Enzalutamide (MDV3100) (HY-70003) .
    JJ-450
  • HY-117669

    Androgen Receptor Cancer
    VPC-14228 is an inhibitor that selectively targets androgen receptor DNA binding domain (AR-DBD). VPC-14228 inhibits the interaction between AR and DNA, thereby blocking AR-mediated transcriptional activation. VPC-14228 does not rely on nuclear localization inhibition, but rather inhibits the activity of full-length AR and splice variant AR-V7 by interfering with AR binding to chromatin. And VPC-14228 has high selectivity for other nuclear receptors such as ER and PR. VPC-14228 can be used in the study of prostate cancer [2].
    VPC-14228
  • HY-174132

    CRM1 Inflammation/Immunology
    CW8001 is a covalent XPO1 (Exportin-1) inhibitor with an EC50 value of 1 nM for inhibiting T cell activation. CW8001 prevents nuclear localization of NFAT transcription factors, suppressing expression of inflammatory cytokines like IL-2. CW8001 is promising for research of T cell-driven immune diseases such as graft-versus-host disease (GVHD) .
    CW8001
  • HY-135691

    c-Myc Apoptosis Cancer
    hnRNPK-IN-1 is a heterogeneous nuclear ribonucleoprotein K (hnRNPK) binding ligand with Kd values of 4.6 μM and 2.6 μM measured with SPR and MST, respectively. hnRNPK-IN-1 inhibits c-myc transcription by disrupting the binding of hnRNPK and c-myc promoter. hnRNPK-IN-1 induces Hela cells apoptosis and has strongly anti-tumor activities .
    hnRNPK-IN-1
  • HY-W019721R

    Reference Standards Nuclear Factor of activated T Cells (NFAT) Inflammation/Immunology
    Cyclosporin D (Standard) is the analytical standard of Cyclosporin D. This product is intended for research and analytical applications. Cyclosporin D, a metabolite of Cyclosporin A, is a weak immunosuppressant. Cyclosporin D is used as internal standard for quantification of Cyclosporin A . Cyclosporin A is a potent immunosuppressant agent, suppress T cell activation by inhibiting calcineurin and the calcineurin-dependent transcription factors nuclear factor of activated T cells (NFAc) .
    Cyclosporin D (Standard)
  • HY-W722556

    3α,5α-Androstanol

    GABA Receptor Constitutive Androstane Receptor Metabolic Disease
    5α-Androstan-3α-ol is a γ-aminobutyric acid (GABA) receptor agonist. 5α-Androstan-3α-ol can inhibit the transcriptional activity of the orphan nuclear receptor CAR (constitutive androstane receptor). 5α-Androstan-3α-ol negatively regulates the activity of CAR by binding to CAR and promoting its dissociation from coactivator proteins. 5α-Androstan-3α-ol can be used to study nuclear receptor-mediated hormone metabolism and drug detoxification mechanisms .
    5α-Androstan-3α-ol
  • HY-P1832A
    PTD-p65-P1 Peptide TFA
    3 Publications Verification

    NF-κB Apoptosis Inflammation/Immunology Cancer
    PTD-p65-P1 Peptide TFA is a potent, selective nuclear transcription factor NF-κB inhibitor and derives from the p65 subunit of NF-κB amino acid residues 271-282, which selectively inhibits NF-κB activation induced by various inflammatory stimulation, down-regulate NF-κB-mediated gene expression and up-regulate apoptosis .
    PTD-p65-P1 Peptide TFA
  • HY-117511

    STAT Apoptosis Interleukin Related TGF-beta/Smad Others
    HJC0123 is a STAT3 inhibitor. HJC0123 inhibits the proliferation of hepatic stellate cells and induces cell cycle arrest and apoptosis. HJC0123 reduces the phosphorylation, nuclear translocation and transcriptional activities of STAT3, increases the production of IL-6, inhibits the phosphorylation of Smad2/3 and down-regulates SOCS3. HJC0123 can be used in the study of liver fibrosis .
    HJC0123
  • HY-P1832

    NF-κB Apoptosis Inflammation/Immunology Cancer
    PTD-p65-P1 Peptide is a potent, selective nuclear transcription factor NF-κB inhibitor and derives from the p65 subunit of NF-κB amino acid residues 271-282, which selectively inhibits NF-κB activation induced by various inflammatory stimulation, down-regulate NF-κB-mediated gene expression and up-regulate apoptosis .
    PTD-p65-P1 Peptide
  • HY-162152

    Keap1-Nrf2 Inflammation/Immunology
    biKEAP1 (compound 3) is an inhibitor targeting the dimerKEAP1. biKEAP1 binds to cellular KEAP1 dimers and releases the NRF2 protein sequestered by KEAP1, resulting in immediate activation of NRF2. biKEAP1 also promotes nuclear translocation of NRF2 and directly inhibits proinflammatory cytokine transcription. biKEAP1 can reduce acute inflammation and reduce inflammatory damage in acute inflammation models .
    biKEAP1
  • HY-43515

    Endogenous Metabolite Metabolic Disease
    ESI1 is a small molecule epigenetic silencing inhibitor. ESI1 can trigger the formation of nuclear condensates of key lipid metabolism regulators SREBP1/2, concentrating transcriptional co-activators to drive lipid/cholesterol biosynthesis. ESI1 can promote myelin regeneration in demyelinated animal models and facilitate de novo myelination on regenerating CNS axons, reversing age-related declines in cognitive abilities .
    ESI1
  • HY-403733A

    Androgen Receptor Cancer
    (-)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR). (-)-JJ-450 is more potent than (+)-JJ-450 (HY-403733B) in inhibiting androgen-induced AR activity, and the mechanism of AR inhibition by (+)-JJ-450 is different from that of Enzalutamide (MDV3100) (HY-70003), which may target the ligand binding domain (LBD) of AR. (-)-JJ-450 inhibits the transcriptional activity of wild-type AR and mutant AR F876L by inhibiting AR nuclear translocation and promoting nuclear degradation of unbound AR. (-)-JJ-450 can be used in the study of castration-resistant prostate cancer (CRPC) resistant to Enzalutamide .
    (–)-JJ-450
  • HY-14649R
    Retinoic acid (Standard)
    95+ Cited Publications

    Vitamin A acid (Standard); all-trans-Retinoic acid (Standard); ATRA (Standard)

    Reference Standards RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    Retinoic acid (Standard) is the analytical standard of Retinoic acid. This product is intended for research and analytical applications. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
    Retinoic acid (Standard)
  • HY-13982R

    NF-κB Metabolic Disease Inflammation/Immunology Cancer
    JSH-23 (Standard) is the analytical standard of JSH-23. This product is intended for research and analytical applications. JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation .
    JSH-23 (Standard)
  • HY-169007

    STAT Inflammation/Immunology
    STAT3-IN-34 (Compound 15E) is an inhibitor for STAT3, and inhibits the nuclear translocation and transcriptional regulator activity of STAT3. STAT3-IN-34 inhibits the proliferation of cell HaCaT with IC50 of 0.008 μM. STAT3-IN-34 inhibits IL-17A expression and ameliorates Imiquimod (HY-B0180)-induced psoriasis in mice .
    STAT3-IN-34
  • HY-N0167

    Ginsenoside C-Mx1; Gypenoside IX

    p38 MAPK Akt NF-κB COX Interleukin Related NO Synthase Metabolic Disease Inflammation/Immunology
    Gynostemma Extract (Gypenoside IX) is a triterpenoid saponin. Gynostemma Extract can be isolated from Panax notoginseng. Gynostemma Extract reduces NFκB nuclear translocation and transcriptional activity by inhibiting the p38 MAPK/Akt/NFκB signaling pathway. Gynostemma Extract reduces the expression of cytokines (COX-2, IL-6) and the production of NO. Gynostemma Extract has anti-inflammatory activity. Gynostemma Extract can be used in the study of liver injury and neuroinflammation .
    Gynostemma Extract
  • HY-162866

    Autophagy Metabolic Disease
    CXM102 is an autophagy activator. CXM102 can induce autophagy in aged BMSCs, leading to the rejuvenation of BMSCs and preferential differentiation into osteoblasts. CXM102 promotes the nuclear translocation of transcription factor EB (TFEB) and the formation of osteoblasts. CXM102 can stimulate bone synthesis metabolism in middle-aged male mice, reduce bone marrow adipocytes, delay bone loss, lower serum inflammation levels, decrease organ fibrosis, and extend the lifespan of the mice .
    CXM102
  • HY-14649S5

    Vitamin A acid-d3; all-trans-Retinoic acid-d3; ATRA-d3

    Isotope-Labeled Compounds RAR/RXR PPAR Endogenous Metabolite Autophagy Cancer
    Retinoic acid-d3 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha .
    Retinoic acid-d3
  • HY-30267R

    Endogenous Metabolite Others
    4-Hydroxyphenyl acetate (Standard) is the analytical standard of 4-Hydroxyphenyl acetate. This product is intended for research and analytical applications. 4-Hydroxyphenyl acetate (4-HPA) is a natural antioxidant and protects cells from oxidative stress-induced necrosis. 4-Hydroxyphenyl acetate blocks the increase of cellular ROS induced by oxidative stress, and up-regulates NQO1 and HO-1 genes by stabilizing and inducing the nuclear translocation of NRF2 transcription factor .
    4-Hydroxyphenyl acetate (Standard)
  • HY-14649S6

    Vitamin A acid-d3-1; all-trans-Retinoic acid-d3-1; ATRA-d3-1

    Isotope-Labeled Compounds RAR/RXR PPAR Endogenous Metabolite Autophagy Metabolic Disease Cancer
    Retinoic acid-d3-1 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha .
    Retinoic acid-d3-1
  • HY-403733B

    Androgen Receptor Prostaglandin Receptor Cancer
    (+)-JJ-450 is a non-competitive antagonist targeting the androgen receptor (AR) that inhibits AR nuclear localization and transcriptional activity in the absence of androgen. (+)-JJ-450 is less active than (-)-JJ-450 (HY-403733A) in inhibiting prostate-specific antigen (PSA) expression in LN95 cells, possibly because (+)-JJ-450 targets the ligand binding domain (LBD) of AR. (+)-JJ-450 inhibits the transcriptional activity of AR and its splice variants (e.g., ARv7) by promoting the degradation of unliganded AR in the nucleus and reducing the binding of AR to androgen response elements (AREs). (+)-JJ-450 can be used in castration-resistant prostate cancer (CRPC) studies that are resistant to enzalutamide (MDV3100) (HY-70003) .
    (+)-JJ-450

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