Search Result
Results for "
region selectivity
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-113294
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3-Hydroxy-DL-kynurenine
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Endogenous Metabolite
Apoptosis
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Neurological Disease
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3-Hydroxykynurenine, a metabolite of tryptophan, is a potential endogenous neurotoxin whose increased levels have been described in several neurodegenerative disorders. 3-Hydroxykynurenine induces neuronal apoptosis .
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- HY-P99258
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OMP 52M51; Anti-Human NOTCH1 Recombinant Antibody
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Notch
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Cancer
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Brontictuzumab (OMP 52M51) is a monoclonal antibody (MAb) that inhibits Notch1 signal. Brontictuzumab selectively binds the negative regulatory region of the Notch1. Brontictuzumab inhibits tumor cell proliferation. Brontictuzumab can be used in the research of leukemia and lymphoma .
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- HY-112299
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TAS6417; CLN-081
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EGFR
Apoptosis
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Cancer
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Zipalertinib (TAS6417; CLN-081) is a highly effective, orally active and pan-mutation-selective EGFR tyrosine kinase inhibitor with a unique scaffold fitting into the ATP-binding site of the EGFR hinge region, with IC50 values ranging from 1.1-8.0 nM .
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- HY-112373
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Aurora Kinase
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Others
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Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket .
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- HY-121638A
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Apoptosis
DGK
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Cancer
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(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
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- HY-117865
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Epigenetic Reader Domain
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Cancer
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GNE-886 (Compound 21) is a potent and selective inhibitor of Cat eye syndrome chromosome region candidate 2 bromodomain (CECR2) (BRD) with an IC50 value of 0.016 µM and an EC50 value of 370 nM. GNE-886 also inhibits BRD9 with an IC50 value of 1.6 µM .
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- HY-P990109
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Amyloid-β
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Neurological Disease
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Aducanumab (Mouse IGG2a) is a monoclonal antibody that selectively targets aggregated amyloid-beta (Aβ). The variable region of Aducanumab (Mouse IGG2a) is consistent with that of Aducanumab (HY-P9967), while the constant region is of Mouse IGG2a sequence. Aducanumab (Mouse IGG2a) has strong selectivity for Aβ fibrils with EC50s of >1 μM and 0.2 nM for monomeric Aβ1-40 and fibrillar Aβ1-42, respectively. Aducanumab (Mouse IGG2a) can be used for Alzheimer's disease (AD) research .
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- HY-120088
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PCSK9
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Cardiovascular Disease
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PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 directly and selectively inhibits translation of PCSK9 by stalling the 80S ribosome in the proximity of codon region .
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- HY-146384
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CRM1
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Cancer
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CRM1 degrader 1 (1l) is a low toxic chromosome region maintenance 1 (CRM1) degrader. CRM1 is the sole nuclear exporter of several tumor suppressor, a growth regulatory protein as an attractive cancer agent target. CRM1 degrader 1 induces the apoptosis in gastric carcinoma and selectively inhibits proliferation of gastric cancer .
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- HY-121638
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Apoptosis
DGK
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Inflammation/Immunology
Cancer
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CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
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- HY-147259
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c-Met/HGFR
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Cancer
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Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .
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- HY-164523
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Checkpoint Kinase (Chk)
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Cancer
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PV1162 is a selective Chk2 inhibitor with an IC50 of 0.29 nM. PV1162 inhibits ATP binding to Chk2 by targeting the gatekeeper-dependent hydrophobic pocket, which is specific to Chk2 and located behind the ATP-binding site (adenine-binding region), thereby inhibiting the phosphorylation activity of Chk2. PV1162 holds potential application value in the field of cancer therapy .
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- HY-401209
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α-synuclein
DNA/RNA Synthesis
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Neurological Disease
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Synucleozid-2.0 is a small-molecule inhibitor targeting the iron-responsive element (IRE) structure in the 5' untranslated region (5'UTR) of SNCA mRNA. Synucleozid-2.0 inhibits ribosome assembly onto SNCA mRNA and selectively reduces α-synuclein protein translation. Synucleozid-2.0 is promising for research of Parkinson's disease (PD) and related α-synucleinopathies .
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- HY-151523
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Ras
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Cancer
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KRas G12R inhibitor 1 is a covalent inhibitor targeting the common oncogenic mutant KRas G12R with selectivity for the mutant arginine. KRas G12R inhibitor 1 possesses an α,β-diketoamide and exploits strong nucleophilicity of the mutant cysteine and irreversibly binds in the Switch II region of KRas. KRas G12R inhibitor 1 can be researched for K-Ras (G12R)-driven cancer such as pancreatic ductal adenocarcinoma (PDAC) .
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- HY-171776
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MMP
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Cancer
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OPB-3206 is a selective matrix metalloproteinase (MMP) inhibitor. OPB-3206 inhibits interstitial collagenase, gelatinase A (MMP-2), gelatinase B (MMP-9) and stromelysin with IC50 values of 7×10 -7 M, 5×10 -6 M, 5×10 -7 M and 2×10 -6 M, respectively. OPB-3206 reversibly binds to the zinc-binding region of MMPs, preventing the activation of MMP-9 and reducing extracellular matrix degradation to inhibit tumor lung metastasis. OPB-3206 is promising for research of lung metastasis of osteosarcoma .
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- HY-110374
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Epigenetic Reader Domain
Apoptosis
|
Cancer
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NVS-CECR2-1, a non-BET family Bromodomain (BRD) inhibitor, is a potent and selective cat eye syndrome chromosome region, candidate 2 (CECR2) inhibitor. NVS-CECR2-1 binds to CECR2 BRD with high affinity (IC50=47 nM; KD=80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis against various cancer cells by targeting CECR2 as well as via CECR2-independent mechanism . NVS-CECR2-1 is a chemical probe.
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- HY-W010041R
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α-synuclein
Amyloid-β
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Neurological Disease
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Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .
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- HY-W010041
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|
α-synuclein
Amyloid-β
|
Neurological Disease
|
Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .
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- HY-W707693
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Isotope-Labeled Compounds
Amyloid-β
α-synuclein
|
Neurological Disease
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Scyllo-Inositol-d6 is the deuterium labeled Scyllo-Inositol (HY-W010041). Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .
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- HY-W040129
-
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Apoptosis
Caspase
|
Infection
Neurological Disease
Cancer
|
Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg 2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe .
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- HY-159834
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SLC-D011
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DNA/RNA Synthesis
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Others
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Progerinin (SLC-D011) is an orally active progerin-lamin A binding inhibitor. Progerinin selectively binds to the C-terminal region of progerin, disrupting its interaction with lamin A and promoting progerin degradation while sparing wild-type lamin A, B, and C. Progerinin ameliorates nuclear deformation, increases H3K9me3 levels, and reduces progerin expression in HGPS patient-derived fibroblasts. Progerinin extends lifespan in Lmna G609G/G609G mice and Lmna G609G/+ mice, improves body weight, hair morphology, cardiac function, and histological phenotypes. Progerinin can be used for the study of Hutchinson-Gilford progeria syndrome (HGPS) .
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- HY-164552
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Apoptosis
Androgen Receptor
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Cancer
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ZNU-IMB-Z15 (Compound Z15) is an antagonist of the androgen receptor (AR) and also a selective degrader of AR and ARV7. ZNU-IMB-Z15 can directly bind to the ligand-binding domain (LBD) and activation function-1 region of AR, and promote AR degradation through the proteasome pathway. ZNU-IMB-Z15 effectively inhibits the transcriptional activity of AR, AR mutants, and AR splice variants (ARVs), downregulating the mRNA and protein levels of AR downstream target genes, thereby overcoming the resistance to second-generation antiandrogen drugs induced by AR LBD mutations, AR amplification, and ARVs in castration-resistant prostate cancer (CRPC). ZNU-IMB-Z15 can inhibit the proliferation of AR-positive CRPC cell lines and induce their apoptosis, demonstrating anticancer activity both in vivo and in vitro .
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- HY-W040129R
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|
Reference Standards
Bacterial
Fungal
Apoptosis
Antibiotic
|
Infection
Neurological Disease
Cancer
|
Chromomycin A3 (Standard) is the analytical standard of Chromomycin A3 (HY-W040129). This product is intended for research and analytical applications. Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg 2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1996
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NBI-5788
|
Peptides
|
Neurological Disease
Inflammation/Immunology
|
Tiplimotide (NBI-5788) is an altered peptide ligand (APL) designed from an immunodominant region (83-99) of the neuroantigen myelin basic protein (MBP). Tiplimotide can selectively reduce the production of inflammatory cytokines by pathogenic T-cells. Tiplimotide can be used for the research of multiple sclerosis (MS) .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99258
-
OMP 52M51; Anti-Human NOTCH1 Recombinant Antibody
|
Notch
|
Cancer
|
Brontictuzumab (OMP 52M51) is a monoclonal antibody (MAb) that inhibits Notch1 signal. Brontictuzumab selectively binds the negative regulatory region of the Notch1. Brontictuzumab inhibits tumor cell proliferation. Brontictuzumab can be used in the research of leukemia and lymphoma .
|
-
- HY-P99382A
-
|
Inhibitory Antibodies
|
Cancer
|
Vopratelimab (Mouse IgG2a) is a monoclonal antibody that selectively targets Inducible CO-Stimulator of T cells (ICOS). The variable region of Vopratelimab (Mouse IgG2a) is consistent with that of Vopratelimab (HY-P99382), while the constant region is of Mouse IgG2a sequence. Vopratelimab (Mouse IgG2a) has antitumor immune response and enhances combinatorial efficacy with anti-PD-1 (HY-P9902A) therapy .
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- HY-P990109
-
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Amyloid-β
|
Neurological Disease
|
Aducanumab (Mouse IGG2a) is a monoclonal antibody that selectively targets aggregated amyloid-beta (Aβ). The variable region of Aducanumab (Mouse IGG2a) is consistent with that of Aducanumab (HY-P9967), while the constant region is of Mouse IGG2a sequence. Aducanumab (Mouse IGG2a) has strong selectivity for Aβ fibrils with EC50s of >1 μM and 0.2 nM for monomeric Aβ1-40 and fibrillar Aβ1-42, respectively. Aducanumab (Mouse IGG2a) can be used for Alzheimer's disease (AD) research .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-113294
-
-
-
- HY-W010041
-
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
α-synuclein
Amyloid-β
|
Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .
|
-
-
- HY-W040129
-
|
Microorganisms
Source classification
|
DNA Alkylator/Crosslinker
DNA/RNA Synthesis
Apoptosis
Caspase
|
Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg 2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe .
|
-
-
- HY-W010041R
-
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
α-synuclein
Amyloid-β
|
Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .
|
-
-
- HY-W040129R
-
|
Microorganisms
Source classification
|
Reference Standards
Bacterial
Fungal
Apoptosis
Antibiotic
|
Chromomycin A3 (Standard) is the analytical standard of Chromomycin A3 (HY-W040129). This product is intended for research and analytical applications. Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg 2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe .
|
-
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-W707693
-
|
Scyllo-Inositol-d6 is the deuterium labeled Scyllo-Inositol (HY-W010041). Scyllo-Inositol is an inhibitor that targets the aggregation of misfolded proteins (such as α-synuclein and Amyloid-β), is orally effective, and can cross the blood-brain barrier. Scyllo-Inositol can selectively bind to and stabilize non-toxic oligomers, preventing them from converting into toxic fibers, exerting protein homeostasis regulation and neuroprotective activity. Scyllo-Inositol binds to the hydrophobic region of pathogenic proteins, inhibits protein aggregation, and promotes lysosome- and proteasome-mediated degradation pathways, thereby reducing neurotoxicity. Scyllo-Inositol can be used in the study of neurodegenerative diseases such as Parkinson's disease, Alzheimer's disease, and Huntington's disease .
|
-
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