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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
133 Results for "
Allosteric site
" in MedChemExpress (MCE) Product Catalog:
Products (133)
133 Results for "Allosteric site" in MCE Product Catalog:
38
38 Publications Verification
BMS-345541 is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
38
38 Publications Verification
BMS-345541 hydrochloride is a selective inhibitor of the catalytic subunits of IKK (IKK-2 IC50=0.3 μM, IKK-1 IC50=4 μM). BMS-345541 binds at an allosteric site of IKK.
15
15 Cited Publications
Cat. No.: HY-A0005
CAS No.: 123318-82-1
Research Areas:
Clofarabine, a nucleoside analogue for research of cancer, is a potent inhibitor of ribonucleotide reductase (IC50=65 nM) by binding to the allosteric site on the regulatory subunit .
12
12 Cited Publications
JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages .
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6
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Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM .
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6 Cited Publications
Cat. No.: HY-18601
CAS No.: 1416258-16-6
Target:
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(±)-BI-D is a potent ALLINI (allosteric integrase inhibitor). (±)-BI-D binds integrase at the LEDGF/p75 binding site. (±)-BI-D inhibits HIV-Luc infection in cells (IC50: 0.16 μM in Psip1 knockout E9 mouse embryonic fibroblasts, 2.9 μM in wild-type E9 mouse embryonic fibroblasts) .
3
Bithionol is an antibacterial, anthelmintic, and algaecide agent. Bithionol is also a potent inhibitor of soluble adenylyl cyclase through binding to the allosteric activator site (IC50: 4 μM) .
2
2 Cited Publications
Target:
Research Areas:
CCG-50014 is the most potent against the regulator of G-protein signaling protein type 4 (RGS4) (IC50 =30 nM) and is >20-fold selective for RGS4 over other RGS proteins. CCG-50014 binds covalently to the RGS, forming an adduct on two cysteine residues located in an allosteric regulatory site . CCG50014, reduces nociceptive responses and enhances opioid-mediated analgesic effects in the mouse formalin test .
2
2 Cited Publications
Target:
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FHT-1015 is a selective SMARCA4 (IC50 = 4 nM) and SMARCA2 (IC50 = 5 nM) (also known as BRG1 and BRM) inhibitor. FH-1015 is an allosteric inhibitor that causes conformation change in the BRG1/BRM protein upon interaction with an allosteric site, inhibiting ATPase activity. FH-1015 interferes with tumor cell growth and migration. FH-1015 can be studied in research for uveal melanoma and hematologic cancer .
2
2 Cited Publications
Synonyms: AVL-3288; UCI-4083
Target:
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CCMI (AVL-3288) is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction .
2
2 Cited Publications
VCP Activator 1 is a VCP activator that dose-dependently stimulates VCP ATPase activity. VCP Activator 1 binds an allosteric pocket near the C-terminus. In addition, VCP Activator 1 binding site can also be occupied by a phenylalanine residue in the VCP C-terminal tail .
1
1 Cited Publications
Target:
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EZ-482, a novel ligand of apolipoprotein (apoE), binds to sites on apoE in the C-terminal domain with Kds of 5-10 μM for apoE3 and apoE4. EZ-482 binds to apoE4 by a unique N-terminal allosteric effect. EZ482 has the potential for Alzheimer’s diseas .
1
1 Cited Publications
PD318088 is a potent, allosteric and non-ATP competitive MEK1/2 inhibitor, an analog of PD184352 (HY-50295). PD318088 binds simultaneously with ATP in a region of the MEK1 active site that is adjacent to the ATP-binding site. PD318088 can be used for cancer research .
1
1 Cited Publications
FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=?6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade .
1
1 Cited Publications
Research Areas:
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
1
1 Cited Publications
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AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
1
1 Cited Publications
β-catenin-IN-3 (Compound C2) is a selective β-catenin inhibitor. β-catenin-IN-3 binds to allosteric site on the surface of β-catenin with K D calculated at 54.96 nM. β-catenin-IN-3 selectively inhibits β-catenin via targeting a cryptic allosteric modulation site, lowers its cellular load. β-catenin-IN-3 significantly reduces viability of β-catenin driven cancer cells, and triggers β-catenin degradation via proteasome system in β-catenin-overexpressing cancer cells .
1
1 Cited Publications
Target:
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AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
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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
