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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
48 Results for "
LBD
" in MedChemExpress (MCE) Product Catalog:
Products (48)
48 Results for "LBD" in MCE Product Catalog:
12
12 Publications Verification
Synonyms: Amodiaquin dihydrochloride dihydrate
Research Areas:
Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
12
Research Areas:
Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
12
12 Publications Verification
Synonyms: Amodiaquin dihydrochloride
Research Areas:
Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine dihydrochloride is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
4
4 Cited Publications
Synonyms: (R)-Flurbiprofen; MPC7869
Research Areas:
Infection Neurological Disease Inflammation/Immunology Cancer
Tarenflurbil ((R)-Flurbiprofen) is the R-enantiomer of the racemate NSAID Flurbiprofen, Tarenflurbil ((R)-Flurbiprofen) inhibits the binding of [ 3H]9-cis-RA to RXRα LBD with IC50 of 75 μM. Tarenflurbil can be used for Alzheimer's disease research.
2
2 Cited Publications
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UT-155 is a selective and potent androgen receptor (AR) antagonist, with a Ki of 267 nM for UT-155 binding to AR-LBD.
1
1 Cited Publications
Cat. No.: HY-W017113
CAS No.: 149-30-4
1
1 Cited Publications
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4A7C-301 is a blood-brain barrier-permeable Nurr1 agonist, with IC50 values of 48.22 nM and 107.71 nM for binding to Nurr1-LBD in the [ 3H]-CQ competition assay and TR-FRET assay, respectively. The EC50 of 4A7C-301 for activating Nurr1 transcriptional activity is 6.53 μM, and its EC50 in N27-A dopaminergic cells is approximately 0.2 μM. 4A7C-301 binds directly to Nurr1-LBD, enhances the transcriptional function of Nurr1, and restores the reduction of Nurr1 protein induced by MPP + or αSyn. 4A7C-301 alleviates oxidative stress and mitochondrial dysfunction, protects midbrain dopaminergic neurons, inhibits microglial activation, and restores impaired autophagic flux. 4A7C-301 can be used in studies related to neuroprotection and Parkinson's disease .
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DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
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UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
Cat. No.: HY-P3717
CAS No.: 3031514-44-7
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XY018 is a potent ROR-γ-selective antagonist. XY018 inhibits ROR-γ constitutive activity in 293T cells with high potency (EC50, 190 nM). XY018 binds to the ROR-γ hydrophobic ligand binding domain (LBD) .
Cat. No.: HY-W677684
CAS No.: 742058-34-0
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Nurr1 agonist 2 (Compound 7) is a Nurr1 agonist (EC50: 0.07 μM). Nurr1 agonist 2 binds to the recombinant Nurr1 ligand binding domain (LBD) with a Kd value of 0.14 μM. Nurr1 agonist 2 increases the Nurr1-regulated genes tyrosine hydroxylase (TH) and vesicular amino acid transporter 2 (VMAT2) mRNA expression .
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DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
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HBT1 is an effective AMPA receptor AMPA-R potentiator. HBT1 specifically binds to the ligand-binding domain (LBD) of AMPAR and enhances receptor activity only when AMPA is present., HBT1 has almost no agonistic effect (i.e., reaching the optimal concentration, and then the efficacy decreases as the concentration continues to increase) compared with traditional AMPA-R potentiator, avoiding the bell-shaped reaction of brain-derived neurotrophic factor (BDNF) production in primary neurons. HBT1 can be applicable to a wider range of neurological and psychiatric diseases (such as depression, Alzheimer's disease, etc.) .
Cat. No.: HY-164552
CAS No.: 920915-26-0
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ZNU-IMB-Z15 is a bifunctional, selective androgen receptor (AR) antagonist and degrader. ZNU-IMB-Z15 directly binds to the ligand-binding domain (LBD) and transactivation function 1 (AF1) of AR, with an IC50 of 63.3 nM for competitive binding to AR LBD and a KD of 0.93 μM for AR AF1. ZNU-IMB-Z15 inhibits AR transcriptional activity and promotes the degradation of AR and ARV7 via the ubiquitin-proteasome pathway. ZNU-IMB-Z15 can be used for the research of castration-resistant prostate cancer .
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THPN is a potent Nur77 agonist. THPN specifically binds the LBD of Nur77 (TR3) but not that of retinoic acid receptor α and PPARγ with a Kd of 270 nM. THPN leads to Nur77 translocation to the mitochondria to induce autophagic cell death in melanoma .
Cat. No.: HY-170851
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GL392 is a senolytic agent that selectively delivers the potent senolytic compound Dasatinib (HY-10181) to senescent cells. GL392 targets lipofuscin in senescent cells via the LBD domain and is linked to Dasatinib through an ester bond. Upon internalization in senescent cells, Dasatinib is released, inducing apoptosis of the senescent cells. GL392 in micelle encapsulation (mGL392) enables selective delivery to senescent cells, achieving selective senescent cell elimination in vitro and in vivo. GL392 can be used for the research of melanoma .
Cat. No.: HY-164373
CAS No.: 1898232-70-6
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SC428 is an androgen receptor (AR) inhibitor that targets the N-terminal domain. SC428 potently decrease the transactivation of (AR)-V7, (AR)v567es, as well as full-length ( AR ) (AR-FL) and its LBD mutants, substantially. SC428 inhibits androgen-stimulated (AR)-FL nuclear translocation, chromatin binding, and (AR) -regulated gene transcription. SC428 inhibits the proliferation of tumor cells in vitro. SC428 inhibits tumor cell growth by inducing apoptosis in mice transplanted with 22RV1 .
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Amodiaquine (dihydrochloride dihydrate) (Standard) is the analytical standard of Amodiaquine (dihydrochloride dihydrate). This product is intended for research and analytical applications. Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect .
Cat. No.: HY-P11035
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APY-d3 is a highly selective EphA4 receptor inhibitor, with an IC50 value of 17-56 nM for human EphA4, an IC50 value of 20 nM for mouse EphA4, and a Kd value of 138 nM for EphA4-LBD. APY-d3 binds to EphA4, blocks its interaction with ephrin ligands, inhibits tyrosine phosphorylation of EphA4, prevents growth cone collapse, and does not induce EphA4 phosphorylation in primary cortical neurons. APY-d3 adopts a β-hairpin conformation stabilized by an N-terminal to C-terminal disulfide bond. APY-d3 can be used in research related to amyotrophic lateral sclerosis, Alzheimer's disease, stroke, neurodegenerative diseases and cancer .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
