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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
2419 Results for "
decrease
" in MedChemExpress (MCE) Product Catalog:
Products (2419)
2419 Results for "decrease" in MCE Product Catalog:
Cat. No.: HY-179177
CAS No.: 1081122-55-5
Target:
Research Areas:
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 .
Cat. No.: HY-179550
Research Areas:
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 .
Cat. No.: 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 .
Cat. No.: HY-180271
Research Areas:
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 .
Cat. No.: HY-180400
CAS No.: 1426293-61-9
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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 .
Cat. No.: HY-180965
CAS No.: 3057939-64-4
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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 .
Cat. No.: HY-181040
CAS No.: 3049710-19-9
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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) .
Cat. No.: HY-181542
Research Areas:
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) .
Cat. No.: HY-181678
Research Areas:
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 .
Cat. No.: HY-18252A
CAS No.: 330784-48-0
Synonyms: TA1790 dibenzenesulfonate
Cat. No.: HY-18252R
CAS No.: 330784-47-9
Synonyms: TA1790 (Standard)
Category:
Cat. No.: HY-182942
CAS No.: 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 .
Cat. No.: HY-183448
CAS No.: 117666-86-1
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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 .
Cat. No.: 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 .
Cat. No.: HY-185206
CAS No.: 2756388-01-7
BSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines. BSJ-05-037 blocks the activation of the NF-κB/GATA-3 signaling pathway, inhibits PLCγ1 phosphorylation, and reduces the proliferative capacity of T-cell lymphoma cells. BSJ-05-037 enhances the sensitivity of T-cell lymphoma cells to chemotherapy. In mouse models of T-cell lymphoma, BSJ-05-037 induces ITK degradation, reduces GATA-3 expression, decreases tumor volume, and reverses chemotherapy resistance. BSJ-05-037 is applicable to research related to T-cell lymphoma .
Cat. No.: HY-187585
CAS No.: 104639-01-2
Target:
Research Areas:
Fourphit is a dopamine transporter (DAT) inhibitor and phencyclidine (PCP) receptor binding agent. Fourphit irreversibly acylates the DAT [ 3H]methylphenidate binding site, reversibly binds to the PCP receptor, and sensitizes neuronal L-type DHP calcium channels. Fourphit attenuates K +-stimulated 45Ca 2+ uptake at high concentrations, and after its pretreatment, Nifedipine (HY-B0284) effectively inhibits this uptake without affecting resting calcium uptake. Fourphit reduces cocaine-induced hyperactivity, decreases cocaine-induced rearing frequency, enhances cocaine-induced thigmotaxis, elicits an acute increase in locomotor activity, and suppresses dark-cycle activity. Fourphit is used in research related to cocaine abuse and addiction .
Cat. No.: HY-187687
CAS No.: 2740603-37-4
Target:
Ferroptosis Fatty Acid Synthase (FASN) Keap1-Nrf2 Glutathione Peroxidase Reactive Oxygen Species (ROS)
Research Areas:
Anticancer agent 359 is a ferroptosis inducer. Anticancer agent 359 inhibits the proliferation, colony formation and migration of bladder cancer cells in a concentration-dependent manner. Anticancer agent 359 induces ferroptosis by downregulating SREBP1 to inhibit FASN transcription, reducing the expression of NRF2/SLC7A11/GPX4, decreasing GSH, promoting ROS accumulation and lipid peroxidation; this effect is reversible by Ferrostatin-1 (HY-100579). Anticancer agent 359 acts synergistically with Talazoparib (HY-16106). Anticancer agent 359 inhibits tumor growth in vivo without obvious hepatotoxicity or nephrotoxicity. Anticancer agent 359 can be used in the research of bladder cancer .
Cat. No.: HY-187692
CAS No.: 3112339-39-3
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Research Areas:
IRAK4-IN-35 is an orally active IRAK4 inhibitor with an IRAK4 IC50 of 9.88 nM. IRAK4-IN-35 also inhibits JAK3, EGFR, CDK2 with IC50 values of 6.72 nM, 32.35 nM, and 39.08 nM, respectively. IRAK4-IN-35 inhibits the production of proinflammatory cytokines, blocks inflammatory signaling pathways, and reduces serum TNF-α levels and spleen index in mouse models of acute inflammation. IRAK4-IN-35 decreases the disease activity index, paw swelling degree, and spleen index in a collagen-induced arthritis mouse model. IRAK4-IN-35 can be used for the research of rheumatoid arthritis .
Cat. No.: HY-188168
CAS No.: 99630-95-2
Synonyms: FMMT
Research Areas:
MDL 72394 (FMMT) is an orally active, blood-brain barrier-penetrant amino acid-based prodrug compound. MDL 72394 is decarboxylated by aromatic L-amino acid decarboxylase to generate the active metabolite MDL 72392 (HY-182727), which is a covalent irreversible MAO inhibitor. MDL 72394 is transported into the brain and synaptosomes via the L-neutral amino acid transport system and the norepinephrine transporter. MDL 72394 selectively inhibits MAO in noradrenergic and dopaminergic neurons without inhibiting serotonergic neurons. MDL 72394 increases hypothalamic extracellular 5-HT, tissue 5-HT, and pineal melatonin biosynthesis, and decreases 5-HIAA. MDL 72394 can be used in research related to MAO-mediated diseases, such as depression .
Cat. No.: HY-189386
CAS No.: 3081319-75-4
Research Areas:
Pyroptosis inducer-1 is a pyroptosis inducer. Pyroptosis inducer-1 promotes STING phosphorylation, NF-κB activation, caspase-1-dependent pyroptosis, GSDMD cleavage, mitochondrial membrane potential disruption, ROS production, S phase cell cycle arrest, ER stress, calcium release, and immunogenic cell death accompanied by CRT exposure, HMGB1 release, and ATP secretion. Pyroptosis inducer-1 enters cancer cells via endocytosis and accumulates in mitochondria and endoplasmic reticulum. Pyroptosis inducer-1 increases dendritic cells and CD8 + T cells while decreasing regulatory T cells. Pyroptosis inducer-1 can be used for breast cancer research .
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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
