36 Results for "

region selectivity

" in MedChemExpress (MCE) Product Catalog:
Products (36)

36 Results for "region selectivity" in MCE Product Catalog:

  • Targets Recommended:
7
7 Publications Verification
Cat. No.: HY-120088
CAS No.: 1632250-49-7
Target:  

PCSK9

Research Areas:  

Cardiovascular Disease

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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3
3 Cited Publications
Cat. No.: HY-112299
CAS No.: 1661854-97-2
Purity:  99.81%
Synonyms: TAS6417; CLN-081
Target:  

EGFR Apoptosis

Research Areas:  

Cancer

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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2
2 Cited Publications
Cat. No.: HY-113294
CAS No.: 484-78-6
Purity:  99.90%
Synonyms: 3-Hydroxy-DL-kynurenine
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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1
1 Cited Publications
Cat. No.: HY-P99014
CAS No.: 1864871-20-4
Synonyms: ARGX-110

Research Areas:  

Inflammation/Immunology Cancer

Cusatuzumab (ARGX-110) is a selective competitive blocker targeting CD70 (with an equilibrium dissociation constant of 17 pM for binding to human CD70). Cusatuzumab also possesses enhanced antibody-dependent cell-mediated cytotoxicity (ADCC) activity. It is a humanized IgG1 monoclonal antibody, artificially synthesized through humanization and genetic engineering modifications (CH2 region mutation to enhance effector function). Cusatuzumab has a dual mechanism of action: firstly, it competitively blocks the interaction between CD70 and CD27, inhibiting the CD27-NF-κB signaling pathway, reducing regulatory T cell (Treg) activation and tumor cell proliferation; secondly, by enhancing binding to FcγRIIIa, it mediates ADCC and antibody-dependent cellular phagocytosis (ADCP), directly lysing CD70-positive tumor cells. Cusatuzumab can efficiently eliminate leukemia stem cells (LSCs), induce tumor cell differentiation and apoptosis, restore immune surveillance, and target CD70-positive tumors. Cusatuzumab is used in the study of acute myeloid leukemia (AML) .
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1
1 Cited Publications
Cat. No.: HY-W040129
CAS No.: 7059-24-7
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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1
1 Cited Publications
Cat. No.: HY-110374
CAS No.: 1992047-61-6
Purity:  99.40%
Research Areas:  

Cancer

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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Cat. No.: HY-173432
CAS No.: 3111845-07-6
Target:  

ACSL Family Ferroptosis

Research Areas:  

Neurological Disease Cancer

LIBX-A401 is a selective long-chain acyl-CoA synthetase 4 (ACSL4) inhibitor with a human IC50 values of 0.38 μM and a Kd of 0.72 μM. LIBX-A401 binds to ACSL4 in an ATP-dependent manner, stabilizes the C-terminal domain, alters the fatty acid gate region, and interacts with residues A329 and Q302 within the fatty acid binding site. LIBX-A401 exhibits anti-ferroptosis properties in cells. LIBX-A401 can be used for the researches of cancer and parkinson's disease .
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Cat. No.: HY-P990109

Target:  

Amyloid-β

Research Areas:  

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 .
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Cat. No.: HY-W010041
CAS No.: 488-59-5
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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Cat. No.: HY-P99258
CAS No.: 1447814-75-6
Synonyms: OMP 52M51; Anti-Human NOTCH1 Recombinant Antibody

Target:  

Notch

Research Areas:  

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 .
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Cat. No.: HY-12854
CAS No.: 868169-64-6
Purity:  99.43%
Synonyms: GRN163L
Target:  

Telomerase Apoptosis

Research Areas:  

Cardiovascular Disease Cancer

Imetelstat (GRN163L) is a 13-mer oligonucleotide and competitive Telomerase inhibitor. Imetelstat binds with high affinity to the template region of the RNA component of human telomerase. Imetelstat induces Apoptosis. Imetelstat is capable of selectively eliminating myelofibrosis hematopoietic stem cells. Imetelstat leads to the loss of a cancer cell's ability to maintain telomere length, resulting in the inhibition of cell proliferation .
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Cat. No.: HY-159834
CAS No.: 2249696-72-6
Synonyms: SLC-D011
Target:  

DNA/RNA Synthesis

Research Areas:  

Others

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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Cat. No.: HY-112373
CAS No.: 879127-16-9
Purity:  99.05%
Target:  

Aurora Kinase

Research Areas:  

Others

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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Cat. No.: HY-147259
CAS No.: 1637658-98-0
Purity:  98.28%
Target:  

c-Met/HGFR

Research Areas:  

Cancer

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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Cat. No.: HY-151523
Purity:  96.24%
Target:  

Ras

Research Areas:  

Cancer

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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Cat. No.: HY-170505
CAS No.: 2254752-21-9
Research Areas:  

Others

Icafolin-methyl is a herbicide and plant β-tubulin (Microtubule/Tubulin) inhibitor. Icafolin-methyl binds to the β-tubulin region of the Colchicine (HY-16569) binding site, thereby blocking the polymerization of plant tubulin. As a non-selective herbicide, Icafolin-methyl exhibits post-emergence activity against weeds in both cool-season and warm-season cropping systems, including resistant ryegrass and darnel biotypes. Icafolin-methyl can be used for herbicide research .
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Cat. No.: HY-164552
CAS No.: 920915-26-0
Research Areas:  

Cancer

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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Cat. No.: HY-P99382A

Target:  

Inhibitory Antibodies

Research Areas:  

Cancer

Vopratelimab (Mouse IgG2a) is a agonist 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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Cat. No.: HY-117865
CAS No.: 2101957-05-3
Purity:  99.81%
Research Areas:  

Cancer

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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Cat. No.: HY-P1996
CAS No.: 178823-49-9
Synonyms: NBI-5788
Target:  

Peptides

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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