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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:
製品番号: HY-17357
CAS 番号: 78281-72-8
別名: AHR 9434; AL 6515
Target:
Nepafenac (AHR 9434; AL 6515), a nonsteroidal anti-inflammatory agent, is a topically administered COX-2 inhibitor with an IC50 of 0.12 μM. Nepafenac exhibits only weak COX-1 inhibitory activity (IC50 = 64.3 μM). Nepafenac possesses unique prodrug properties, which enable it to rapidly convert into the active metabolite Amfenac (HY-17479) in the ocular tissues, thereby achieving high concentrations in the retina and choroid. Nepafenac reduces inflammation and pain by inhibiting the activity of cyclooxygenase (COX) enzymes and thereby decreasing the production of prostaglandin PGE₂. Nepafenac can delay the metastasis of uveal melanoma (UM) in rabbit eyes. Nepafenac is mainly used for pain management and inflammation control after ophthalmic surgeries .
製品番号: HY-174423
CAS 番号: 1994348-72-9
別名: NC-656
Iptriazopyrid is a 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitor, with a Ki value of 24.3 nM against Arabidopsis thaliana and 33.3 nM against Oryza sativa. Iptriazopyrid binds to the active pocket of HPPD, occupies the catalytic site, inhibits carotenoid biosynthesis, prevents chloroplast formation, and induces albino and chlorotic symptoms in sensitive plants. Used as a herbicide, Iptriazopyrid can control barnyardgrass when applied alone, and its efficacy does not decrease when mixed with labeled residual herbicides. When Iptriazopyrid is mixed with 2,4-D or triclopyr, its barnyardgrass control effect shows an antagonistic effect. Iptriazopyrid is a triazole carboxamide herbicide that exhibits selectivity for Oryza sativa over Echinochloa crus-galli, and has partial tank-mix compatibility with synthetic auxin herbicides registered for rice .
製品番号: HY-174499
Cas9 Nickase D10A mRNA expresses a version of the Streptococcus pyogenes SF370 Cas9 protein (CRISPR Associated Protein 9) that contains a D10A amino acid substitution. This mRNA also contains a C-terminal nuclear localization signal followed by a HA tag.Cas9 functions as part of the CRISPR (clustered regularly interspaced short palindromic repeats) genome editing system. In the CRISPR system, an RNA guide sequence targets the site of interest and the Cas9 protein is employed to perform the DNA cleavage. While wild-type Cas9 creates a double-stranded break at the target site, Cas9 nickase creates a single-stranded break. This favors homology-directed repair and decreases the occurrence of non-homologous end joining.
製品番号: HY-175496
CAS 番号: 2907705-12-6
Target:
研究分野:
Acid Ceramidase-IN-3 is a acid ceramidase (aCDase) inhibitor. Acid Ceramidase-IN-3 inhibits the enzymatic activity of aCDase with a pIC 50 of 8.5 in enzymatic assays and 6.8 in A375 melanoma cellular assays. Acid Ceramidase-IN-3 promotes HSC inactivation, as measured by a dose-dependent
reduction in COL1A1 and ACTA2. Acid Ceramidase-IN-3 inhibits aCDase activity in HSCs, promotes HSC inactivation and suppresses YAP/TAZ nuclear localization. Acid Ceramidase-IN-3 increases Dynein/Kinesin (NDE1, NDEL1.
KIF3B, KIF15) while decreases several proteins involved with signaling pathway (SARM1, RGAP1,
PDGF-D,PDGFR-B). Acid Ceramidase-IN-3 can be used for the study of fibrotic diseases .
製品番号: HY-178018
CAS 番号: 1269110-12-4
別名: iOXCT1
Target:
研究分野:
D574-0246 is a dual-activity inhibitor of OXCT1, inhibiting both the ketolytic and succinyltransferase activities of OXCT1. D574-0246 reduces substrate-specific (LACTB K284) and global protein succinylation and decreases OXCT1 ketolytic activity in HepG2 cells. D574-0246 inhibits the viability of HCC cells (IC50: 16.49 μM in PLC cells, 6.656 μM in HepG2 cells). D574-0246 exerts anti-tumor efficacy in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors. D574-0246 can be used for the study of hepatocellular carcinoma (HCC) .
製品番号: HY-178912
Anti-MRSA agent 39 is an orally active ClpX modulator that binds Staphylococcus aureus caseinolytic protease X (SaClpX) with high affinity (Kd = 3.6 μM). Anti-MRSA agent 39 exerts antibacterial effects through temperature-dependent inhibition of cell division. Anti-MRSA agent 39 elicits profound metabolic dysregulation in methicillin-resistant Staphylococcus aureus (MRSA), manifesting as significantly reduced ATP levels, elevated reactive oxygen species (ROS), and decreased NAD+/NADH ratio, and accelerates bacterial lysis rates in MRSA ATCC 33591. Anti-MRSA agent 39 significantly increases the proportion of MRSA cells in the mitotic phase, and the cells exhibit obvious morphological abnormalities. Anti-MRSA agent 39 can be used for the study of invasive MRSA infections .
製品番号: HY-179177
CAS 番号: 1081122-55-5
Target:
研究分野:
AO-365/43472821 is a selective, brain-penetrant Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC50 = 0.29 μM) and shows a significant inhibitory effect on (CDC-like kinase 1) CLK1 (IC50 = 0.08 μM). AO-365/43472821 could protect the human neuroblastoma cell line SH-SY5Y from Okadaic acid (HY-N6785) (OA)-induced injury. AO-365/43472821 decreased tau (pSer396)/tau and Aβ1-42 protein expression. AO-365/43472821 can be used for the study of Alzheimer's disease .
製品番号: HY-179550
研究分野:
Avanafil metabolite M4 (Compound M-4ii) is a metabolite of Avanafil (HY-18252). Avanafil is a selective Phosphodiesterase-5 (PDE-5) inhibitor with IC50s of 5.2, 630, 5700, 6200, 12000, 27000, 51000 and 53000 nM for PDE-5, PDE-6, PDE-4, PDE-10, PDE-8, PDE-7, PDE-2 and PDE-1, respectively. Avanafil activates NO/cGMP/PKG signaling-pathway to decrease loss in BMD, bone atrophy, and oxidative stress. Avanafil inhibits cGMP hydrolysis and thus increases cGMP levels. Avanafil can be used for the research of erectile dysfunction and osteoporosis .
製品番号: HY-180242
EGFR/CDK2-IN-5 is a potent dual EGFR and CDK2 inhibitor with IC50s of 17.30 and 212.10 nM, respectively. EGFR/CDK2-IN-5 also inhibits EGFR T790M with an IC50 of 123.8 nM. EGFR/CDK2-IN-5 exhibits potent anticancer activity. EGFR/CDK2-IN-5 induces G1 and S cell cycle arrest and apoptosis, accompanied by increased levels of caspase-3/9 and Bax, as well as decreased Bcl-2 levels. EGFR/CDK2-IN-5 can be used for the research of cancers, such as lung cancer, breast cancer, and leukemia .
製品番号: HY-180271
研究分野:
Xanthine oxidase-IN-21, a Genipin (HY-17389) derivative, is an orally active mixed competitive xanthine oxidase (XOD) inhibitor with an IC50 of 0.68 μM. Xanthine oxidase-IN-21 reduces renal fibrosis by decreasing α-SMA expression and suppresses pro-inflammatory cytokines IL-1β, IL-6, and TNF-α through NF-κB pathway regulation. Xanthine oxidase-IN-21 also inhibits URAT1 and GLUT9 expression, promoting uric acid excretion and lowering serum uric acid levels. Xanthine oxidase-IN-21 shows significantly hepatorenal protection activity. Xanthine oxidase-IN-21 can be used for the research of hyperuricemia .
製品番号: HY-180400
CAS 番号: 1426293-61-9
Target:
研究分野:
PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC50: 39 μM, rat α7 nAChR EC50: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC50 = 174 μM) and CaV2.2 channel (IC50 = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain .
製品番号: HY-180965
CAS 番号: 3057939-64-4
研究分野:
Pro-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research .
製品番号: HY-181040
CAS 番号: 3049710-19-9
Target:
研究分野:
Factor B-IN-8 (Compound (3R ,4R )-15) is a potent, selective and orally active factor B inhibitor with an IC50 of 10.2 nM. Factor B-IN-8 can effectively inhibit the binding of factor B to C3b and the subsequent formation of C3 convertase (C3bBb). Factor B-IN-8 can inhibit the deposition of membrane attack complex (MAC) mediated by alternativepathway with an IC50 of 59.3 nM. Factor B-IN-8 can reduce the cleavage of factor B protein and decrease the deposition of complement C3d in the glomeruli and renal tubules. Factor B-IN-8 can be used for researches of arthritis and paroxysmal nocturnal hemoglobinuria (PNH) .
製品番号: HY-181542
研究分野:
SG-55 is a selective, noncompetitive and orally active AKR1C3 inhibitor with an IC50 of 5 nM and a Ki of 10 nM. SG-55 shows >2000-fold selectivity for AKR1C3 over AKR1C1, AKR1C2, and AKR1C4 (> 10 μM). SG-55 increases the ratio of reduced/oxidized nicotinamide adenine dinucleotide phosphate (NADPH/NADP +), decreases the ratio of reduced/oxidized glutathione (GSH/GSSG), and induces DNA double-strand breaks. SG-55 can overcome Osimertinib (HY-15772) resistance mediated by EGFR C797S triple mutation in non-small cell lung cancer (NSCLC) .
製品番号: HY-181678
研究分野:
DNA-PK/HDAC6-IN-1 is a selcetive and orally active dual DNA-PK and HDAC6 inhibitor with IC50 values of 84.2 and 64.8 nM. DNA-PK/HDAC6-IN-1 suppresses cancer cells proliferation, induces cancer cell cycle G2/M arrest, apoptosis, and decreases the mitochondrial membrane potential. DNA-PK/HDAC6-IN-1 induces DNA damage and elevates γ-H2AX levels. DNA-PK/HDAC6-IN-1 exhibits antitumor efficacy in AML animal mouse model. DNA-PK/HDAC6-IN-1 can be used for the research of acute myeloid leukemia .
製品番号: HY-18252A
CAS 番号: 330784-48-0
別名: TA1790 dibenzenesulfonate
製品番号: HY-18252R
CAS 番号: 330784-47-9
別名: TA1790 (Standard)
Category:
製品番号: HY-182942
CAS 番号: 3112321-20-4
PV-DPD-19 is an autoinducer-2 (AI-2) quorum sensing inhibitor. PV-DPD-19 reduces AI-2 production and inhibits the expression of multiple MSCRAMMs. In co-culture systems with Staphylococcus aureus, PV-DPD-19 decreases the production of pyocyanin and Elastase in Pseudomonas aeruginosa. PV-DPD-19 impairs the adhesion ability of Staphylococcus aureus to lung epithelial cells. PV-DPD-19 inhibits biofilm formation of Pseudomonas aeruginosa (MBIC50 = 27 μg/mL) and Staphylococcus aureus (MBIC50 = 35 μg/mL). PV-DPD-19 shows no cytotoxicity in both in vitro lung epithelial cell models and in vivo Galleria mellonella larva models .
製品番号: HY-183448
CAS 番号: 117666-86-1
研究分野:
ETMTC is an orally active anti-inflammatory and antioxidant agent. ETMTC inhibits IKK-mediated phosphorylation and degradation of IkBα, blocks nuclear translocation and activation of NF-κB, and reduces the expression of ICAM-1, VCAM-1, E-selectin, Th2 cytokines and eosinophil chemokines. ETMTC abrogates neutrophil adhesion to endothelial monolayers and inhibits TNF-α-induced ROS production. ETMTC activates Nrf2, and enhances the activities of mitochondrial complex I and IV. ETMTC reduces lipid peroxidation levels, oxidative DNA damage, cytochrome c and caspase 9 activity, and decreases goblet cell metaplasia and subepithelial fibrosis. ETMTC can be used for the research of inflammatory diseases and asthma .
製品番号: HY-184325
NDM-622 is a Colistin (HY-113678) adjuvant. NDM-622 weakly inhibits IKKβ with an IC50 of 20.40 μM. NDM-622 reduces the minimum inhibitory concentration of colistin against colistin-highly-resistant Acinetobacter baumannii and Klebsiella pneumoniae. NDM-622 decreases bacterial colony-forming units in a mouse peritonitis model infected with colistin-highly-resistant Klebsiella pneumoniae. NDM-622 does not modify bacterial lipid A, induce reactive oxygen species production, or increase bacterial membrane permeability. NDM-622 can be used in the research of extensively drug-resistant Gram-negative bacterial infections, colistin-resistant Acinetobacter baumannii infections, and Klebsiella pneumoniae infections .
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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
