8798 Results for "

C"-D loop binding

" in MedChemExpress (MCE) Product Catalog:
Products (8798)

8798 Results for "C"-D loop binding" in MCE Product Catalog:

Art. -Nr.: HY-109061A
CAS. Nr.: 2411549-88-5
Synonyms: YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
Forschungsgebiete:  

Cancer

Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
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Art. -Nr.: HY-164729
FZ-AD005 is a DLL3-targeting antibody-drug conjugate (ADC) with high selectivity, composed of the anti-DLL3 antibody FZ-A038 (HY-P990896), a dipeptide linker (Val-Ala), and DXd (HY-13631D). The Kd value of FZ-AD005 for human DLL3 ranges from 13.29 to 58.3 pmol/L. After binding to DLL3 on the cell surface, FZ-AD005 mediates endocytosis, and the payload DXd is released via cleavage by lysosomal cathepsins. DXd inhibits topoisomerase TopI to induce double-strand DNA breaks, cell cycle arrest and apoptosis, and FZ-AD005 exhibits bystander killing activity against adjacent DLL3-negative cells. FZ-AD005 shows stable circulation in vivo, has good tolerance and acceptable pharmacokinetic profiles in rats and cynomolgus monkeys, and effectively inhibits the growth of DLL3-expressing tumor cells. FZ-AD005 serves as a promising candidate molecule for research on small cell lung cancer and human neuroendocrine prostate cancer .
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Art. -Nr.: HY-169385
CAS. Nr.: 2925060-81-5
Forschungsgebiete:  

Cancer

ATC-324 is an bivalent AR (Androgen Receptor) degrader based on the protein degradation technology platform AUTOphagy-TArgeting Chimera (AUTOTAC). ATC-324 induces the formation of AR/p62 complex, leading to autophagy-lysosomal degradation of AR. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa . ATC-324 is composed of target-binding ligand (TBL) Enzalutamide (HY-70002) and p62/SQSTM1 autophagy-targeting ligand (ATL) YT 6-2 analog-1 (HY-169386), connected by Boc-NH-PEG4-CH2CH2NH2 (HY-W008352). Among them, the active control of the target protein ligand is Enzalutamide carboxylic acid (HY-70002B), and the conjugate composed of the autophagy-targeting ligand and the linker is YT 6-2-PEG3-C2-NH2 (HY-169387).
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Art. -Nr.: HY-B0110S
CAS. Nr.: 1542211-40-4
Synonyms: SHB 331-d6; WL 70-d6
Gestodene-d6 (SHB 331-d6; WL 70-d6) is the deuterated-labeled Gestodene (HY-B0110). Gestodene is an orally active synthetic progestogen compound of the 19-nortestosterone class. Gestodene binds with high affinity to the progesterone receptor, inhibits 5α-reductase, binds to androgen and aldosterone receptors, and inactivates CYP3A. Gestodene acts as a positive allosteric modulator of PAR1, enhances PAR1-mediated signaling pathways, and is capable of increasing the activation potency of PAR1-AP toward PAR1, thereby promoting ERK1/2 phosphorylation, receptor internalization, cell morphological changes, and human platelet aggregation. Gestodene and its A-ring reduced metabolites promote the proliferation, differentiation, and mineralization of neonatal rat osteoblasts. Gestodene itself has no binding capacity for estrogen receptors, and this osteogenic activity depends on intracellular metabolism to generate A-ring reduced products with estrogen-like agonistic activity. Gestodene is useful for research on diseases related to progesterone secretion and diseases related to thrombosis .
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Art. -Nr.: HY-N2593R
CAS. Nr.: 32507-66-7
Isorhapontigenin (Standard) is the analytical standard of Isorhapontigenin (HY-N2593). This product is intended for research and analytical applications. Isorhapontigenin is an orally active dietary polyphenol. Isorhapontigenin acts as a potent antioxidant that reduces the production of reactive oxygen species (ROS). Isorhapontigenin promotes the binding of JUN to the AP-1 site on the SESN2 promoter, induces SESN2 transcription, triggers MAPK8-dependent JUN activation, and upregulates the expression of PPAR-α, PGC-1α and CPT-1A to facilitate fatty acid oxidation. Isorhapontigenin induces autophagy, apoptosis and preadipocyte differentiation; it inhibits tumor growth, cell invasion, NF-κB transcriptional activity, the PI3K/Akt signaling pathway, STAT1 phosphorylation and MMP-2 expression. Isorhapontigenin alleviates oxidative stress, inflammatory cytokine release and triglyceride accumulation; it increases intracellular ATP levels and promotes Nrf2 nuclear translocation. Isorhapontigenin improves insulin sensitivity in adipose tissue and glucose tolerance, and reduces postprandial blood glucose, insulin and free fatty acid levels. Isorhapontigenin is applicable to research on bladder cancer, liver injury, chronic obstructive pulmonary disease, acute lung injury and type 2 diabetes.
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Art. -Nr.: HY-W753897
Synonyms: SHB 331-d7; WL 70-d7
Gestodene-d7 (SHB 331-d7; WL 70-d7) is the deuterated-labeled Gestodene (HY-B0110). Gestodene is an orally active synthetic progestogen compound of the 19-nortestosterone class. Gestodene binds with high affinity to the progesterone receptor, inhibits 5α-reductase, binds to androgen and aldosterone receptors, and inactivates CYP3A. Gestodene acts as a positive allosteric modulator of PAR1, enhances PAR1-mediated signaling pathways, and is capable of increasing the activation potency of PAR1-AP toward PAR1, thereby promoting ERK1/2 phosphorylation, receptor internalization, cell morphological changes, and human platelet aggregation. Gestodene and its A-ring reduced metabolites promote the proliferation, differentiation, and mineralization of neonatal rat osteoblasts. Gestodene itself has no binding capacity for estrogen receptors, and this osteogenic activity depends on intracellular metabolism to generate A-ring reduced products with estrogen-like agonistic activity. Gestodene is useful for research on diseases related to progesterone secretion and diseases related to thrombosis .
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Art. -Nr.: HY-L950
2,787 compounds

Seven-membered rings are privileged medium-sized scaffolds with distinct twist-chair conformations and greater 3D diversity than five- and six-membered rings. Their flexible conformations allow induced-fit protein binding and precise pharmacophore positioning. They also modulate Fsp³, pKa and logP to enhance solubility and permeability. Azepanes, oxepanes and benzodiazepines serve as bioisosteres for hit discovery against GPCRs, ion channels and kinases.

Widely found in plant and microbial alkaloids, seven-membered heterocycles show excellent biocompatibility and target affinity. They underpin many approved drugs for CNS, cancer and infectious diseases, including diazepam, imipramine and carbamazepine. Clinical candidates further highlight their unique value. However, high transannular strain and synthetic difficulty limit their availability, leaving them rare in standard screening libraries.

MCE 7 Membered Scaffold Library contains 2,792 structurally diverse, lead-like molecules covering azepanes, oxepanes, benzodiazepines and dibenzazepines. With varied substitutions, chiral centers and synthetic accessibility, it fills the shortage of medium-ring scaffolds. Ideal for HTS, virtual screening and SAR studies, these novel, patent-clear compounds offer a distinctive starting point for drug discovery in CNS disorders, oncology, antivirals and challenging targets such as PPIs.

Art. -Nr.: HY-L018
458 compounds

The transforming growth factor beta (TGF-β) signaling pathway is involved in many cellular processes in both the adult organism and the developing embryo including cell growth, cell differentiation, apoptosis, cellular homeostasis and other cellular functions. The TGF-β superfamily comprises TGF-βs, bone morphogenetic proteins (BMPs), activins and related proteins. Signaling begins with the binding of a TGF beta superfamily ligand to a TGF beta type II receptor. The type II receptor is a serine/threonine receptor kinase, which catalyzes the phosphorylation of the Type I receptor. The type I receptor then phosphorylates receptor-regulated SMADs (R-SMADs) which can now bind the coSMAD (e.g. SMAD4). R-SMAD/coSMAD complexes accumulate in the nucleus where they act as transcription factors and participate in the regulation of target gene expression. Deregulation of TGF-β signaling contributes to developmental defects and human diseases, including cancers, some bone diseases, chronic kidney disease, etc.

MCE designs a unique collection of 458 TGF-beta/Smad signaling pathway compounds. TGF-beta/Smad Compound Library acts as a useful tool for TGF-beta/Smad-related drug screening and disease research.

Art. -Nr.: HY-P75830
Reinheit:  ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: IL13RA2; IL-13R Subunit Alpha-2; Interleukin 13 Receptor Subunit Alpha 2; IL-13R-Alpha-2; CD213a2; IL-13RA2; IL-13R; Interleukin-13 Receptor Alpha 2 Variant; IL13BP; Interleukin 13 Receptor Alpha 2 Chain; CT19; Interleukin 13 binding Protein; Interleukin-
Species:  
Mouse
Source:  
HEK293
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Art. -Nr.: HY-P75832
Reinheit:  ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: IL13RA2; IL-13R Subunit Alpha-2; Interleukin 13 Receptor Subunit Alpha 2; IL-13R-Alpha-2; CD213a2; IL-13RA2; IL-13R; Interleukin-13 Receptor Alpha 2 Variant; IL13BP; Interleukin 13 Receptor Alpha 2 Chain; CT19; Interleukin 13 binding Protein; Interleukin-
Species:  
Mouse
Source:  
HEK293
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Art. -Nr.: HY-P75833
Reinheit:  ≥ 95%, as determined by Bis-Tris PAGE.
Synonyms: IL13RA2; IL-13R Subunit Alpha-2; Interleukin 13 Receptor Subunit Alpha 2; IL-13R-Alpha-2; CD213a2; IL-13RA2; IL-13R; Interleukin-13 Receptor Alpha 2 Variant; IL13BP; Interleukin 13 Receptor Alpha 2 Chain; CT19; Interleukin 13 binding Protein; Interleukin-
Species:  
Rat
Source:  
HEK293
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Art. -Nr.: HY-P75834
Reinheit:  ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: IL13RA2; IL-13R Subunit Alpha-2; Interleukin 13 Receptor Subunit Alpha 2; IL-13R-Alpha-2; CD213a2; IL-13RA2; IL-13R; Interleukin-13 Receptor Alpha 2 Variant; IL13BP; Interleukin 13 Receptor Alpha 2 Chain; CT19; Interleukin 13 binding Protein; Interleukin-
Species:  
Rat
Source:  
HEK293
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Art. -Nr.: HY-P76989
Reinheit:  ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: IL13RA2; IL-13R Subunit Alpha-2; Interleukin 13 Receptor Subunit Alpha 2; IL-13R-Alpha-2; CD213a2; IL-13RA2; IL-13R; Interleukin-13 Receptor Alpha 2 Variant; IL13BP; Interleukin 13 Receptor Alpha 2 Chain; CT19; Interleukin 13 binding Protein; Interleukin-
Species:  
Canine
Source:  
HEK293
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Art. -Nr.: HY-P76990
Reinheit:  ≥ 95%, as determined by reducing SDS-PAGE.
Synonyms: IL13RA2; IL-13R Subunit Alpha-2; Interleukin 13 Receptor Subunit Alpha 2; IL-13R-Alpha-2; CD213a2; IL-13RA2; IL-13R; Interleukin-13 Receptor Alpha 2 Variant; IL13BP; Interleukin 13 Receptor Alpha 2 Chain; CT19; Interleukin 13 binding Protein; Interleukin-
Species:  
Canine
Source:  
HEK293
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Art. -Nr.: HY-P701809
Reinheit:  ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: MARK4; FLJ90097; Prev. MARKL1; Non-Specific Serine/Threonine Protein Kinase; MAP/Microtubule Affinity-Regulating Kinase 4; Epididymis Secretory Sperm binding Protein; KIAA1860; MARK4 Serine/Threonine Protein Kinase; PAR-1D; MARKL1L; MAP/Microtubule Affinity-Regulating Kinase Like 1; MARK4L; Nbla00650; MARK4S; Microtubule Affinity Regulating Kinase 4; MAP/Microtubule Affinity-Regulating Kinase-Like 1
Species:  
Human
Source:  
E. coli
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Art. -Nr.: HY-P85607
Synonyms: Bag 1; BAG family molecular chaperone regulator 1; BAG-1; BAG1; BAG1_HUMAN; BCL 2 Associated Athanogene 1; BCL 2 associated athanogene; BCL 2 binding athanogene 1; Bcl-2-associated athanogene 1; BCL2 associated athanogene 1; BCL2 associated athanogene; Glucocorticoid receptor-associated protein RAP46; HAP1; Haptoglobin; RAP 46; RAP46.

Host:  

Mouse

Application:  

WB

Reactivity:  

Human, Mouse

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Art. -Nr.: HY-P705931
Reinheit:  ≥ 90%, as determined by reducing SDS-PAGE.
Synonyms: DUSP22; JNK-Stimulatory Phosphatase-1; Dual Specificity Phosphatase 22; MAP Kinase Phosphatase X; JKAP; LMW-DSP2; JSP1; LMWDSP2; MKPX; MKP-X; Low Molecular Weight Dual Specificity Phosphatase 2; JSP-1; JNK Pathway Associated Phosphatase; Homolog Of Mouse Dual Specificity Phosphatase LMW-DSP2; VHX; Epididymis Secretory Sperm binding Protein; Mitogen-Activated Protein Kinase Phosphatase X; JNK-Stimulating Phosphatase 1; Dual Specificity Protein Phosphatase 22
Species:  
Human
Source:  
E. coli
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Art. -Nr.: HY-P812030A
Synonyms: MED27; Mediator Complex Subunit 27; CRSP34; TRAP37; CRSP8; MED3; Cofactor Required For Sp1 Transcriptional Activation, Subunit 8, 34kDa; Mediator Of RNA Polymerase II Transcription Subunit 27; Transcriptional Coactivator CRSP34; P37 TRAP/SMCC/PC2 Subunit; CRSP Complex Subunit 8; Cofactor Required For Sp1 Transcriptional Activation Subunit 8; Epididymis Secretory Sperm binding Protein; NEDSCAC; CRAP34

Host:  

Mouse

Application:  

WB

Reactivity:  

Human, Mouse, Rat

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Art. -Nr.: HY-P84973
Synonyms: BLR1; MDR15; BLR 1 antibody; BLR1 antibody; Burkitt lymphoma receptor 1 antibody; Burkitt lymphoma receptor 1 GTP binding protein antibody; Burkitt lymphoma receptor 1; GTP binding protein; chemokine; C-X-C motif; receptor 5; antibody; C X C chemokine receptor type 5 antibody; C-X-C chemokine receptor type 5 antibody; CD 185 antibody; CD185 antibody; CD185 antigen antibody; Chemokine; C-X-C motif; receptor 5 antibody; Chemokine C X C motif receptor 5 antibody; Chemokine CXC motif receptor 5 antibody; Chemokine receptor 5 antibody; CXC chemokine receptor type 5 antibody; CXC R5 antibody; CXC-R5 antibody; CXCR 5 antibody; CXCR-5 antibody; Cxcr5 antibody; CXCR5_HUMAN antibody; MDR 15 antibody; MDR-15 antibody; MDR15 antibody; MGC117347 antibody; Monocyte derived receptor 15 antibody; Monocyte-derived receptor 15 antibody;
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Art. -Nr.: HY-P85022
Synonyms: BLR1; MDR15; BLR 1 antibody; BLR1 antibody; Burkitt lymphoma receptor 1 antibody; Burkitt lymphoma receptor 1 GTP binding protein antibody; Burkitt lymphoma receptor 1; GTP binding protein; chemokine; C-X-C motif; receptor 5; antibody; C X C chemokine receptor type 5 antibody; C-X-C chemokine receptor type 5 antibody; CD 185 antibody; CD185 antibody; CD185 antigen antibody; Chemokine; C-X-C motif; receptor 5 antibody; Chemokine C X C motif receptor 5 antibody; Chemokine CXC motif receptor 5 antibody; Chemokine receptor 5 antibody; CXC chemokine receptor type 5 antibody; CXC R5 antibody; CXC-R5 antibody; CXCR 5 antibody; CXCR-5 antibody; Cxcr5 antibody; CXCR5_HUMAN antibody; MDR 15 antibody; MDR-15 antibody; MDR15 antibody; MGC117347 antibody; Monocyte derived receptor 15 antibody; Monocyte-derived receptor 15 antibody;

Host:  

Mouse

Application:  

FC, ELISA

Reactivity:  

Human

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