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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
2438 Results for "
decrease
" in MedChemExpress (MCE) Product Catalog:
Products (2438)
2438 Results for "decrease" in MCE Product Catalog:
Synonyms: AT-752 free base
Áreas de investigación:
Arbemnifosbuvir (AT-752 free base) is an orally active inhibitor of DENV NS5 RdRp and MTase, and is also a guanosine nucleotide analog prodrug. Arbemnifosbuvir forms the active triphosphate metabolite AT‑9010 (HY-139165) in peripheral blood mononuclear cells, which competes with GTP to terminate RNA synthesis and binds to the GTP/RNA-cap site to inhibit 2'-O-methylation. Arbemnifosbuvir reduces viremia, improves survival, prevents weight loss, and decreases viral load in a mouse model of dengue virus. Arbemnifosbuvir can be used for research related to viral infections .
Referencia número: HY-157936
No. CAS: 3034593-10-4
Target:
Áreas de investigación:
GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke .
Referencia número: HY-159595
No. CAS: 1233353-86-0
Áreas de investigación:
PCSK9-IN-29 is a lipid-lowering agent. PCSK9-IN-29 can increase low-density lipoprotein receptor (LDLR) protein expression and decrease PCSK9 protein expression in hepG2 cells. PCSK9-IN-29 can reduce the levels of serum LDL-C, TC, and liver enzyme ALT in crab eating macaques fed a high-fat diet, lower body weight and fat, and increase bone mineral content. PCSK9-IN-29 can be used for research on non-alcoholic fatty liver disease and obesity .
Referencia número: HY-161966
No. CAS: 3046428-94-5
Áreas de investigación:
VEGFR-2-IN-52 (compound 14d) is a potent VEGFR-2 inhibitor with an IC50 value of 191.1 nM. VEGFR-2-IN-52 decreases the protein expression of p-VEGFR-2, MMP9, p-ERK1/2 and p-MEK1. VEGFR-2-IN-52 shows cytotoxicity. VEGFR-2-IN-52 induces apoptosis and cell cycle arrest at G0/G1 phase. VEGFR-2-IN-52 increases the levels of ROS .
Referencia número: HY-162350
No. CAS: 3057216-63-1
Target:
Áreas de investigación:
TDI-11055 is a selective and orally active eleven-nineteen leukemia (ENL) inhibitor, which displaces ENL from chromatin by blocking its YEATS domain interaction with acylated histones. TDI-11055 inhibits ENL and AF9 YEATS domains with IC50 values of 50 nM and 70 nM, respectively, and no activity against GAS41 or YEATS2. TDI-11055 decreases chromatin occupancy of ENL-associated complexes, impairs transcription elongation, suppresses key oncogenic gene expression programs, and induces differentiation. TDI-11055 can be used for the research of acute myeloid leukemia .
Referencia número: HY-162353
No. CAS: 3056570-19-2
Áreas de investigación:
AZ'9567 is an orally active MAT2a inhibitor with a pIC50 of 9.1. AZ'9567 binds to MAT2a allosterically, reduces the synthesis of SAM, decreases SDMA levels, and exerts antiproliferative effects on MTAP-knockout cells. AZ'9567 depletes SAM, causes methionine accumulation in plasma and tissues, triggers adaptive disorders in one-carbon metabolism, transsulfuration metabolism and lipid metabolism, and induces oxidative stress, hepatic steatosis and lipid homeostasis imbalance. AZ'9567 can be used in studies related to MTAP-deficient/deleted cancers .
Referencia número: HY-163783
No. CAS: 3105428-74-5
Target:
Áreas de investigación:
CSNK2-IN-1 is a potent and selective CSNK2 inhibitor with IC50 of 1.7 nM and 0.66 nM for CSNK2A1 and CSNK2A2, respectively. CSNK2-IN-1 has antiviral activity against beta-coronaviruses such as SARS-CoV-2 and MHV. CSNK2-IN-1 has good solubility, metabolic stability, and low cytotoxicity, but its plasma concentration in vivo decreases rapidly and is insufficient to achieve pharmacological effects. CSNK2-IN-1 can be used in the research of antiviral drug development .
Referencia número: HY-164895
No. CAS: 3080918-50-6
PIN1 degrader-1 is a covalent PIN1 degrader with an IC50 of 21.5 nM. PIN1 degrader-1 induces a decrease in the thermal stability of PIN1, and triggers PIN1 degradation in a concentration- and time-dependent manner across various cancer cells. PIN1 degrader-1 also reduces the viability of pancreatic cancer, breast cancer, prostate cancer and lung cancer cells. PIN1 degrader-1 can be used for research on pancreatic cancer, breast cancer, prostate cancer and non-small cell lung cancer .
Referencia número: HY-165316
No. CAS: 13699-45-1
Target:
NOD-like Receptor (NLR) Interleukin Related Reactive Oxygen Species (ROS) Caspase TNF Receptor Apoptosis
Áreas de investigación:
Myristoyllysophosphatidylcholine is a NLRP3 inflammasome inhibitor with multiple activities including anti-inflammatory and antioxidant effects. Myristoyllysophosphatidylcholine inhibits LPS-induced NLRP3 inflammasome activation, reduces pro-inflammatory cytokine secretion, decreases ROS and MDA levels, alleviates lung tissue and cell damage, and mediates apoptosis. Myristoyllysophosphatidylcholine serves as a myristate donor for myristoylation of the Glucose-6-Phosphate Isomerase (GPI) anchor in Trypanosoma brucei and undergoes hydrolysis. Myristoyllysophosphatidylcholine acts as a biomarker for the severity of community-acquired pneumonia. Myristoyllysophosphatidylcholine can be used in research related to diseases such as community-acquired pneumonia and acute lung injury .
Referencia número: HY-168086
No. CAS: 2992690-04-5
Target:
Áreas de investigación:
LSD1-IN-35 (Compound Z-1) is a selective LSD1 Inhibitor (IC50: 108 nM). LSD1-IN-35 inhibits the demethylation on H3K4me1/2. LSD1-IN-35 is an immunomodulator. LSD1-IN-35 promotes response of gastric cancer cells to T-cell killing effect by decreasing PD-L1 expression and further attenuates the PD-1/PD-L1 interaction .
Referencia número: HY-168087
No. CAS: 1893340-21-0
Target:
Áreas de investigación:
GSK3335103 is an orally active non-peptidic αvβ6 integrin inhibitor with a pIC50 of 8 and a pKi of 9.96. GSK3335103 blocks αvβ6 integrin-mediated cell adhesion and TGF-β1 activation, induces integrin internalization, recycling and lysosomal degradation, attenuates TGFβ signaling and reduces collagen deposition. GSK3335103 decreases the level of pSmad2 in BAL cells and collagen deposition in lung tissues in a mouse model of pulmonary fibrosis. GSK3335103 can be used in research related to pulmonary fibrosis .
Referencia número: HY-171336
No. CAS: 357625-50-4
Target:
Áreas de investigación:
TRC4186 is a potent advanced glycation end-product (AGE) breaker . TRC4186 breaks advanced glycation end-products, reduces their tissue accumulation, and decreases AGE burden. TRC4186 improves endothelial and myocardial function, preserves cardiac function, retards renal dysfunction, and reduces renal dysfunction severity. TRC4186 downregulates brain natriuretic peptide and IL-6 expression. TRC4186 can be used for the research of diabetic macro- and microvascular complications, diabetic heart failure, diabetic renal failure, hypertension, diabetes, diabetic cardiomyopathy, and diabetic nephropathy .
Referencia número: HY-171900
Target:
Áreas de investigación:
Lipid 114 is an ionizable cationic lipid with a pKa of approximately 6.8. Lipid 114 can be used to generate lipid nanoparticles (LNP) to deliver siRNA in vitro as well as in vivo. Lipid 114 LNPs encapsulating siRNA that targets IL-1β can reduce IL-1β expression in macrophages. Lipid 114 LNPs encapsulating siRNA that targets IL-1β also reduces hepatic and renal expression of IL-1β, as well as decreasing hepatic inflammation in mouse model with LPS-induced acute liver failure .
Referencia número: HY-172533
3’,5’-DiOA-dC is a hydrophobic nucleotide lipid and a ligand for the STING agonist c-di-GMP (CDG). 3’,5’-DiOA-dC can assemble with CDG and form stable cyclic dinucleotide nanoparticles via various supramolecular forces driven by molecular recognition. 3’,5’-DiOA-dC can decrease tumor weight and volume, increase CD8 T cell, neutrophils as well as NK cell counts in tumor microenvironment in combination with CDG. 3’,5’-DiOA-dC also increases the levels of TNF-α and IFN-γ in murine melanoma model .
Referencia número: HY-175512
Áreas de investigación:
Tubulin-IN-53 is a potent Tubulin inhibitor with an IC50 of 6.06 μM. Tubulin-IN-53 inhibits the polymerization of tubulin by targeting the colchicine binding site of tubulin and destroys the microtubule network. Tubulin-IN-53 induces MCF-7 cell cycle arrest in the G2/M phase and apoptosis, and inhibits cell migration accompanied by the decrease of mitochondrial membrane potential and increase the accumulation of ROS. Tubulin-IN-53 destroys the angiogenesis of human umbilical vein endothelial cells.Tubulin-IN-53 can used for the study of cancers such as breast cancer and lung cancer .
Referencia número: HY-176192
Áreas de investigación:
SMU-14a is a selective Toll-like receptor 3 (TLR3) inhibitor wirh an IC50 of 0.18 μM. SMU-14a reduces phosphorylation of p65, ERK, and TBK1 via NF-κB, MAPK, and IRF3 signaling pathways. SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages, downregulates TNF-α in human peripheral blood monocytes and decreases serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used for the research of acute hepatitis .
Referencia número: HY-176284
Target:
Oxidative Phosphorylation Mitochondrial Metabolism Apoptosis Reactive Oxygen Species (ROS) AMPK Keap1-Nrf2
Áreas de investigación:
OXPHOS-IN-2 is an orally active OXPHOS inhibitor. OXPHOS-IN-2 exhibits potent inhibitory activity in PC9 (IC50 = 12.3 nM) and Bxpc-3 cells (IC50 = 250 nM in glucose medium, IC50 = 17.5 nM in galactose medium). OXPHOS-IN-2 decreases the NADH/NAD + ratio and reduces ATP levels. OXPHOS-IN-2 induces tumor cells apoptosis by activating reactive oxygen species (ROS) and downregulating the level of Nrf2. OXPHOS-IN-2 can be used for research on cancer such as non-small cell lung cancer and pancreatic cancer .
Referencia número: HY-179125
Target:
Áreas de investigación:
COX-2-IN-59 is a potent and selective COX-2 inhibitor with an IC50 of 0.052 μM. COX-2-IN-59 exhibits 200-fold selectivity over COX-1 (IC50 = 11.16 μM). COX-2-IN-59 reduces COX-2 levels, induces cell cycle arrest, and triggers apoptosis by increasing Bax expression, decreasing Bcl-2 levels, and activating caspase-3. COX-2-IN-59 can be used for the research of colon cancer .
Referencia número: HY-180779
No. CAS: 2636710-78-4
Áreas de investigación:
SR-1815 is a multi-kinase inhibitor of CLK1 (IC50 446 nM), CLK2 (605 nM), and CLK3 (6.8 μM; weaker). SR-1815 reduces SR protein phosphorylation and Syngap1 toxic exon inclusion, restores SynGAP and postsynaptic PSD95/GluN1 expression, and promotes dendritic spine enlargement and branching. SR-1815 decreases synaptic/circuit hyperexcitability. SR-1815 selectively inhibits cancer cell line proliferation. SR-1815 can be used for research on epileptic encephalopathy .
Referencia número: HY-181669
No. CAS: 3034595-62-2
Target:
Áreas de investigación:
P300-IN-6 is an orally active histone acetyltransferase p300 HAT domain inhibitor with human IC50 values of 7 nM. P300-IN-6 suppresses c-Myc expression, decreases H3K18ac and H3K27ac levels, and inhibits cancer cell proliferation.P300-IN-6 suppresses tumor growth in xenograft mouse models.P300-IN-6 can be used for the research of multiple myeloma .
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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
