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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
20 Results for "
degradation efficiency
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "degradation efficiency" in MCE Product Catalog:
2
2 Cited Publications
PROTAC TBK1 degrader-2 is a potent PROTAC degrader of serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM) .
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1 Cited Publications
Cat. No.: HY-W019670
CAS No.: 3768-18-1
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Dornase alfa (rhDNase) is a recombinant human deoxyribonuclease I (rhDNase) that can specifically degrade extracellular DNA. Dornase alfa catalyzes the cleavage of DNA released by neutrophils in respiratory mucus, reduces sputum viscosity, thereby improving mucus clearance efficiency, reducing airway obstruction and alleviating inflammatory responses. Dornase alfa can be used to improve lung function (such as FEV_1) in cystic fibrosis (CF), reduce the risk of acute pulmonary exacerbations, and has good in vivo tolerability. Dornase alfa acts locally on the respiratory tract through aerosol inhalation, specifically improving the high viscosity of mucus caused by DNA accumulation and related respiratory symptoms .
Cat. No.: HY-172736
CAS No.: 3005272-36-3
Synonyms: BMS-986458
Toviblideg (BMS-986458) is a highly selective, orally active cereblon-based BCL6 PROTAC degrader and antitumor agent. Toviblideg selectively degrades BCL6 by binding cereblon to the BTB domain of BCL6, thereby regulating the cell cycle, antiproliferative and interferon signaling pathways, and upregulating the expression and distribution of CD20. Toviblideg modulates the phenotype of follicular helper T cells and reduces circulating tumor DNA levels. The combination of Toviblideg with CD20xCD3 bispecific antibody also enhances the efficiency of T cell tumor infiltration and expansion. Toviblideg induces regression of BCL6-positive tumors and prolongs survival, and it is suitable for research related to B-cell non-Hodgkin lymphoma, diffuse large B-cell lymphoma, follicular lymphoma, and relapsed/refractory lymphoma .
KTX-951 is an orally active PROTAC degrader of IRAK4 and IMiD (Ikaros/Aiolos) substrates (Kd = 3.5 nM). KTX-951 induces IRAK4 degradation, and the degradation efficiency is independent of IRAK4 binding affinity. The DC50 values of KTX-951 for IRAK4, Ikaros and Aiolos are 18 nM, 14 nM and 13 nM, respectively. The IC50 of KTX-951 against OCl-Ly10 CTG is 35 nM. KTX-951 exhibits antitumor activity .
Cat. No.: HY-W753593
Cat. No.: HY-172930
CAS No.: 2991021-08-8
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PVTX-405 is a selective and oral active IKZF2 molecular glue degrader with a DC50 of 0.7 nM and a Dmax of 91%. PVTX-405 enhances degradation efficiency, significantly reduces off-target degradation, and alleviates hERG inhibition with IC50 of 48 µM. PVTX-405 significantly inhibits the growth of MC38 tumors, with greater synergistic anti-cancer efficacy in combination with immune checkpoint therapies (ICTs) (anti-PD1 or anti-LAG3) in the MC38 mouse tumor xenograft model using Crbn 391V C57BL/6 mice .
Cat. No.: HY-W019670R
CAS No.: 3768-18-1
Category:
Cat. No.: HY-154818
Synonyms: Bovine Serum Albumin, Acetylated
Cat. No.: HY-179065
CAS No.: 882235-30-5
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VU0494372 is an activator of potassium ion channel KCNQ1. VU0494372 can significantly enhance the cell surface expression and transport efficiency of KCNQ1. VU0494372 does not alter KCNQ1 mRNA levels and protein degradation rate, and has no significant cytotoxicity. VU0494372 can be used for research on cardiovascular conditions .
Cat. No.: HY-401721
CAS No.: 204852-67-5
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5-CNAC is an orally active enhancer of absorption, with no pharmacological activity on its own. 5-CNAC can significantly enhance the absorption efficiency of the drug (such as Salmon calcitonin (HY-P0090)) when administered together with it in the gastrointestinal tract. 5-CNAC binds reversibly and non-covalently to peptide drugs, protecting them from degradation by gastrointestinal enzymes, increasing their lipid solubility, promoting passive transcellular absorption, and not damaging the integrity of the intestinal epithelium. 5-CNAC can be used in the research of adjuvants for orally administered peptide agents .
Cat. No.: HY-W012935
CAS No.: 50675-20-2
Synonyms: Piperidine-4-carboxaldehyde
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Piperidine-4-carbaldehyde (Piperidine-4-carboxaldehyde) is a PROTAC Linker. Piperidine-4-carbaldehyde can be used to optimize combined with the target protein affinity, thus improve the PROTAC the molecular degradation efficiency. Piperidine-4-carbaldehyde can be used in the CDK2 PROTACs (HY-161708) .
Cat. No.: HY-L151
544 compounds
PROTACs (Proteolysis-targeting chimeras) is a class of molecules that utilize ubiquitin-proteasome system (UPS) to ubiquitinate and degrade target proteins. The PROTACs molecule consists of two ligands joined by a linker. The one-to-one interaction between PROTACs and target proteins determines the high efficiency of PROTACs, making it a potential molecule for targeted protein degradation (TPD) therapy.
MCE supplies a unique collection of 544 PROTACs that effectively degrade target proteins with more powerful screening capability. MCE PROTAC Library is a useful tool for signal pathway research, protein degradation therapy research, drug discovery and drug repurposing, etc.
Cat. No.: HY-L257
0 compounds
Linkers, as key structural units in PROTAC molecules that connect the two functional ends, not only determine the overall molecular conformation and spatial compatibility but also directly influence the stability of the ternary complex, as well as cellular permeability and degradation efficiency. In recent years, with the widespread application of click chemistry in medicinal chemistry, the incorporation of bioorthogonal reactive groups such as azides (-N3) into PROTAC linker design has become an emerging research focus, providing an important tool for modular assembly and rapid structural optimization.
The MCE Azide PROTAC Linker Library contains 0 linkers specifically designed for targeted protein degradation molecule design and optimization. These linkers serve as efficient “click handles,” enabling rapid and highly selective covalent coupling with alkyne reaction partners, thereby facilitating modular assembly and structural diversification of PROTAC molecules. In drug development, this design not only improves the efficiency of molecular construction but also significantly accelerates the screening and optimization of lead compounds. Meanwhile, by tuning linker properties such as length, flexibility, and polarity, the ability to form ternary complexes and degradation activity can be optimized.
Cat. No.: HY-180985
Azo-PROTAC-4C-cis is a BCR-ABL PROTAC degrader, and its degradation efficiency of BCR-ABL is much lower than that of its trans isomer Azo-PROTAC-4C-trans (HY-180983). Azo-PROTAC-4C-cis is the product of the conformational transformation of Azo-PROTAC-4C-trans under ultraviolet (UV) light irradiation. Azo-PROTAC-4C-cis can be converted into highly active Azo-PROTAC-4C-trans under visible light, thereby initiating protein degradation. Azo-PROTAC-4C-cis can be used for the study of myeloid leukemia .
Cat. No.: HY-L259
0 compounds
In PROTAC drug development, linkers are often one of the key variables determining drug-likeness and degradation efficiency. Since PROTAC systems must simultaneously satisfy target protein binding, E3 ligase recruitment, and intracellular spatial conformational matching, their structural design is essentially a multi-parameter optimization problem. Differences in linker rigidity, flexibility, and spatial extension can significantly influence the formation pathway and stability of the ternary complex, leading to substantial variations in degradation activity. Therefore, the development of linker systems with modular tunability and high structural expandability has become an important direction in PROTAC optimization.
The MCE Alkyne PROTAC Linker Library contains 0 linkers based on terminal and internal alkyne scaffolds, forming a highly derivatizable linker module system. These linkers serve as standardized building blocks for rapid assembly and iterative optimization of PROTAC molecules, and support efficient conjugation with azide-containing functional groups via click chemistry. In practical drug development, this type of structure not only facilitates the construction of diverse linker space libraries, accelerating lead compound screening, but also enables systematic tuning of molecular geometry and physicochemical properties, thereby improving ternary complex stability and targeted protein degradation efficiency.
Cat. No.: HY-W009690
CAS No.: 10543-57-4
Synonyms: Tetraacetylethylenediamine; TAED
Research Areas:
N,N,N',N'-Tetraacetylethylenediamine (Tetraacetylethylenediamine; TAED) is a disinfectant and bleach activator. N,N,N',N'-Tetraacetylethylenediamine is a common bleach activator in phosphorus-free laundry detergent formulations, which acts to activate sodium perborate and improve bleaching efficiency at low temperatures. N,N,N',N'-Tetraacetylethylenediamine reacts with sodium percarbonate in water to produce peracetic acid with strong oxidative bactericidal activity. This reaction is environmentally friendly, and the final degradation products are sodium carbonate, acetic acid, ammonia, carbon dioxide, oxygen and water .
Cat. No.: HY-156957
CAS No.: 300718-75-6
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5-CNAC disodium is an orally active enhancer of absorption, with no pharmacological activity on its own. 5-CNAC disodium can significantly enhance the absorption efficiency of the drug (such as Salmon calcitonin (HY-P0090)) when administered together with it in the gastrointestinal tract. 5-CNAC disodium binds reversibly and non-covalently to peptide drugs, protecting them from degradation by gastrointestinal enzymes, increasing their lipid solubility, promoting passive transcellular absorption, and not damaging the integrity of the intestinal epithelium. 5-CNAC disodium can be used in the research of adjuvants for orally administered peptide agents .
Cat. No.: HY-D3276
Target:
Research Areas:
PE-Cy7 is a tandem dye conjugate based on fluorescence resonance energy transfer (FRET). Composed of phycoerythrin (PE) as the donor and Cy7 as the acceptor fluorescent dye, PE-Cy7 is suitable for multicolor flow cytometry, laser scanning cytometry and immunofluorescence applications. PE-Cy7 can be conjugated to antibodies or used in the biotin-streptavidin system to label cell surface antigens in immunophenotyping and multiparametric cell analysis. PE-Cy7 undergoes photon-induced oxidative degradation, whose rate depends on light intensity and storage conditions, leading to reduced FRET efficiency and increased PE leakage. PE-Cy7 can be excited at wavelengths of 488 nm, 532 nm or ~760 nm, and its emission signal can be detected using 780/60 nm, 810/90 nm or 785/50 nm bandpass filters, with a Stokes shift of 300 nm .
Cat. No.: HY-L140
232 compounds
Withdrawal or delisting drugs refer to drugs that are recalled or discontinued from the market due to low efficiency, serious side effects, financial and regulatory problems and other reasons. Once the drug is withdrawn from the market, it will cause heavy losses to the original research company that invested a lot of time, finance and other costs to develop the drug.
Adverse drug reaction (ADR) is the main reason for drug withdrawal from the market. ADR refers to the unexpected effects caused by the reasons such as the target-directed interaction during the treatment. However, studying the mechanism of these ADRs may just be a breakthrough in finding new indications. For example, thalidomide, the protagonist of the drug damage event that caused numerous "seal babies" deformed infants, was found to be due to the degradation of a transcription factor - SALL4 after delisting, which made thalidomide have a new clinical application. In 1998, it was approved by FDA for the treatment of leprosy nodular erythema, and in 2006, it was approved for the treatment of multiple myeloma. ADR study of delisted drugs can not only avoid the loss of drug development in advance but also bring hope to new indications.
MCE has sorted out 232 drug compounds withdrawn from the market through FDA, EMA and other authoritative platforms. Each compound has withdrawal records in at least one country/market. It is a useful tool for conducting research on drug side effects or drug toxicity mechanisms and discovering new indications of drugs.
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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
