Scientific Reviews
Product Guides
Blogs
Topics
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
8 Results for "
Non-competitive ligand
" in MedChemExpress (MCE) Product Catalog:
Products (8)
8 Results for "Non-competitive ligand" in MCE Product Catalog:
Target:
Research Areas:
4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection .
Cat. No.: HY-P991243
Cat. No.: HY-164144
CAS No.: 1887195-17-6
Target:
Research Areas:
EPZ033294 is an inhibitor of SYMD2 (IC50 is 3.9 nM). SYMD2 itself has catalytic activity and can methylate the lysine residue of BTF3 to BTF3me1, which was experimentally demonstrated by detecting an IC50 of 2.9 nM for inhibition of BTF3ME1 by SYMD2, indicating an active inhibition of SYMD2 by EPZ033294. EPZ033294 (0-50 µM) has an inhibitory effect on SYMD2 and a concentration-dependent inhibitory effect in 293T .
Cat. No.: HY-403733A
CAS No.: 1998094-23-7
Target:
Research Areas:
(-)-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 .
Cat. No.: HY-403733B
CAS No.: 1998094-24-8
Research Areas:
(+)-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) .
Cat. No.: HY-403733C
CAS No.: 2020353-42-6
Target:
Research Areas:
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) .
Cat. No.: HY-100815
CAS No.: 83654-13-1
Target:
Research Areas:
(R)-AMPA is an inactive AMPA receptor ligand that inhibits the release of excitatory amino acids from neurons. (R)-AMPA is inactive in experiments that enhance the release of [3H]D-aspartate induced by electrical stimulation. (R)-AMPA is inhibited by competitive and noncompetitive AMPA receptor selective antagonists in response to AMPA and glutamate .
Cat. No.: HY-187650
CAS No.: 2507890-46-0
Target:
Research Areas:
LuAF60097 is a serotonin transporter (SERT) ligand. LuAF60097 binds to the extracellular vestibule (S2 site) of SERT with high affinity and to the central binding site (S1) with lower affinity, triggering conformational changes that exert combined competitive and non-competitive inhibitory effects on serotonin reuptake. LuAF60097 is applicable to research related to depression and anxiety disorders .
-
-
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
