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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
16 Results for "
massive
" in MedChemExpress (MCE) Product Catalog:
Products (16)
16 Results for "massive" in MCE Product Catalog:
1
1 Cited Publications
PIK5-12d is a PROTAC PIKfyve degrader (DC50 = 1.48 nM). PIK5-12d induces massive cytoplasmic vacuolization and blocks autophagic flux in multiple prostate cancer cells. PIK5-12d inhibits prostate cancer cell proliferation. PIK5-12d significantly suppresses tumor proliferation in mice bearing LTL-331R human prostate cancer PDX tumors. PIK5-12d can be used for the study of prostate cancer .
Cat. No.: HY-N6723
CAS No.: 116355-84-1
Category:
Infection Human Gut Microbiota Metabolites Antibiotics Microorganism Disease Research Antibacterial Endogenous metabolite Disease Research Fields Other Antibiotics
Target:
(E/Z)-E64FC26 is a mixture of the stereoisomers E-E64FC26 and Z-E64FC26, in which E-E64FC26 is the active component and acts as a potent PDI inhibitor. The IC50 values of E64FC26 (E-E64FC26) for PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6 are 0.6, 4.8, 33.1, 12.1, and 5.7 μM, respectively. By inhibiting PDI, (E/Z)-E64FC26 causes massive intracellular accumulation of misfolded polyubiquitinated proteins, thereby triggering strong endoplasmic reticulum stress and oxidative stress responses, which in turn induce apoptosis. (E/Z)-E64FC26 is used in research on multiple myeloma, ovarian cancer, and breast cancer .
Cat. No.: HY-175381
CAS No.: 3058911-16-0
Research Areas:
DeFer-2 is a Ferritin PROTAC degrader with a Kd value of 17.1 μM. DeFer-2 recruits the VHL E3 ligase to induce targeted degradation of ferritin via the ubiquitin-proteasome system, triggers iron overload stress in cancer cells, and further activates caspase 3-GSDME-mediated pyroptosis through massive ROS production. DeFer-2 can be used for research related to melanoma .
Target:
Aldose Reductase Glutathione Reductase (GR) p38 MAPK ERK JNK Reactive Oxygen Species (ROS) Apoptosis Drug Intermediate
Research Areas:
Cardiovascular Disease Neurological Disease Metabolic Disease
Glyoxal (40% w/w in water) is an α-oxoaldehyde that inhibits Aldose Reductase, Glutathione Reductase, and NADPH synthase. Glyoxal (40% w/w in water) exhibits cytotoxicity, triggers oxidative stress, induces ROS accumulation, lipid peroxidation, mitochondrial membrane potential collapse, DNA damage, apoptosis, and massive production of advanced glycation end products (AGEs). Glyoxal (40% w/w in water) depletes glutathione and activates MAPK phosphorylation. It has lower toxicity as a fixative than paraformaldehyde (PFA) and serves as a precursor for the synthesis of oxalates and dietary carcinogens. Glyoxal (40% w/w in water) is suitable for research related to calcium oxalate kidney stones, diabetes, atherosclerosis, cardiovascular diseases, retinopathy, and cataracts .
Cat. No.: HY-P3095
CAS No.: 65988-34-3
Synonyms: α-LTX
Target:
Research Areas:
α‑Latrotoxin (α-LTX) is a neurotoxin found in the genus Latrodectus. α-Latrotoxin binds to presynaptic receptors such as neurexin and latrophilin-1, inserts into the cell membrane to form non-selective cation channels, and induces massive exocytosis of neurotransmitters and hormones through dual mechanisms of receptor dependence and pore formation, triggering calcium signaling disturbances and electrophysiological alterations. α-Latrotoxin can be used in research related to synaptic vesicle exocytosis and neurotransmitter release .
Cat. No.: HY-149348
CAS No.: 3052259-89-6
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DiPT-4 is a dual TOP1/PARP1 inhibitor that induces massive DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells. DiPT-4 has the potential to overcome cancer drug resistance .
Target:
Cat. No.: HY-P1142
CAS No.: 195262-56-7
Cat. No.: HY-162311
CAS No.: 2767204-90-8
Research Areas:
Anticancer agent 194 (compound 10p) is a ferroptosis and autophagy inducer. Anticancer agent 194 arrests colon cancer cell cycle at G2/M phase, but can't induce cell apoptosis. Anticancer agent 194 independently triggeres cell ferroptosis and autophagy through the massive accumulation of ROS .
Cat. No.: HY-P5172
Target:
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Cat. No.: HY-P1142S
Target:
Research Areas:
Cat. No.: HY-P1142S1
Target:
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Cat. No.: HY-184665
CAS No.: 1638811-35-4
Target:
Research Areas:
Dedimethyl MitoCur-1 is a mitochondria-targeted curcuminoid derived from MitoCur-1 (HY-150228) with anticancer activity. MitoCur-1 induces massive reactive oxygen species production in cancer cells, reduces mitochondrial membrane potential, and triggers cell cycle arrest and apoptosis. Meanwhile, MitoCur-1 inhibits the phosphorylation of Akt and STAT3, enhances ERK phosphorylation, and upregulates the expression of the pro-apoptotic protein BNIP3. Dedimethyl MitoCur-1 can be used in research related to breast cancer, cervical cancer, prostate cancer, and neuroblastoma .
Cat. No.: HY-LD002
100 billion compounds
The discovery of hit molecule is a cornerstone of drug development. Among the diverse tools available, DNA-encoded libraries have emerged a revolutionary platform for high-throughput screening. Compared with traditional HTS, DEL features shorter screening processes, lower costs, simpler assays, and larger library capacities.
DEL Construction utilizes split-and-pool synthesis, a combinatorial chemistry approach that involves iterative splitting, reaction, and pooling. This strategy enables rapid, exponential assembly of fragments in minimal steps without the need for individual compound synthesis andassoicicated isolation or purification steps, thus greatly reducing overall costs. The technology enables simultaneous affinity screeningof massive compound collections to target proteins in a single step. By coupling chemical structures with unique DNA barcodes, each compound is tagged with a distinct DNA sequence for convenient tracking and decoding.DELs readily enable the construction and efficient screening of libraries containing millions to billions of compounds. As a result, DEL screening combines the dual advantages of high efficiency and low cost, making DEL a transformative technology in modern drug discovery.
The DEL kit consists of 50 independent libraries with a total scale of 100 billion compounds. It is constructed through stepwise combinatorial chemistry strategies involving 2-, 3-, and 4-round synthesis. By employing diverse scaffolds and flexible linking strategies, it encompasses various ring systems, linear frameworks, and heterocyclic structures. Screening can be achieved solely through affinity, independent of target-specific activity detection methods. This library is suitable for DEL screening against a wide range of targets.
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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
