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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
862 Results for "
6.3
" in MedChemExpress (MCE) Product Catalog:
Products (862)
862 Results for "6.3" in MCE Product Catalog:
86
86 Publications Verification
Cat. No.: HY-42110A
Target:
Research Areas:
Deschloroclozapine dihydrochloride, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [ 11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging .
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Target:
Research Areas:
Deschloroclozapine, a metabolite of Clozapine, is a highly potent muscarinic DREADDs agonist, with blood-brain barrier permeability. Deschloroclozapine binds to DREADD receptor subtypes hM3Dq and hM4Di with Ki of 6.3 and 4.2 nM, respectively. [ 11C]-Deschloroclozapine is developed as a promising PET tracer for DREADD imaging .
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38
Target:
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Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC50s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.
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37 Cited Publications
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R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 reduces immune complex-mediated inflammation . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
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37 Cited Publications
Research Areas:
R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation . R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
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35 Cited Publications
Synonyms: DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride
Research Areas:
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor . 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor [6]. 3-Deazaneplanocin A hydrochloride also has anti-orthopoxvirus and anti-variola activities .
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I-BET151 (GSK1210151A) is a BET bromodomain inhibitor which inhibits BRD4, BRD2, and BRD3 with pIC50 of 6.1, 6.3, and 6.6, respectively .
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20 Cited Publications
Synonyms: ITMN-191; R7227; RO5190591; RG7227
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Research Areas:
Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC50 of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC50 higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC50s=0.2-0.4 nM) as well as 2b and 3a (IC50s=1.6, 3.5 nM) . Danoprevir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 0.05 μM .
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Branaplam (LMI070; NVS-SM1) is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .
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16 Cited Publications
Cat. No.: HY-19620A
CAS No.: 1562338-39-9
Synonyms: LMI070 hydrochloride; NVS-SM1 hydrochloride
Target:
Research Areas:
Branaplam (LMI070; NVS-SM1) hydrochloride is a highly potent, selective and orally active survival motor neuron-2 (SMN2) splicing modulator with an EC50 of 20 nM for SMN. Branaplam hydrochloride inhibits human-ether-a-go-go-related gene (hERG) with an IC50 of 6.3 μM. Branaplam hydrochloride elevates full-length SMN protein and extends survival in a severe spinal muscular atrophy (SMA) mouse model .
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Fostamatinib (R788) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
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16 Cited Publications
Synonyms: R788Disodium
Research Areas:
Fostamatinib Disodium (R788 Disodium) is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
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16 Cited Publications
Synonyms: R788 disodium hexahydrate
Research Areas:
Fostamatinib (R788) disodium hexahydrate is the oral proagent of the active compound R406 . R406 is an orally available and competitive Syk/FLT3 inhibitor with a Ki of 30 nM and an IC50 of 41 nM . R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM) .
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13 Cited Publications
Synonyms: α-Cyano-4-hydroxycinnamate
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α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications .
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Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC50 values of 0.8 nM and 4 nM against Abl1 WT and Abl1 T315I, respectively. Rebastinib potently inhibits CYP2C8 (IC50 = 0.0533 μM) and CYP2C9 (IC50 = 2.54 μM). Rebastinib allosterically inhibits Tie2 with an IC50 of 0.63 nM. Rebastinib inhibits the transcriptional activity of FoxO1. Rebastinib inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib induces Apoptosis. Rebastinib exerts anti-tumor activity in breast cancer. Rebastinib exerts anti-angiogenic effects. Rebastinib increases myotube diameter and improves reduced contractility. Rebastinib can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia .
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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
