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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
3492 Results for "
Competitive
" in MedChemExpress (MCE) Product Catalog:
Products (3492)
3492 Results for "Competitive" in MCE Product Catalog:
Referencia número: HY-180155
No. CAS: 3105470-83-2
Target:
Keap1-Nrf2 Cholinesterase (ChE) Interleukin Related TNF Receptor Reactive Oxygen Species (ROS) Heme Oxygenase (HO) Quinone Reductase
Áreas de investigación:
Keap1/Nrf2/ARE activator 2 is an activator of Keap1/Nrf2/ARE pathway and non-competitively inhibits AChE with an IC50 of 14.79 μM and a Ki of 1.35 μM. Keap1/Nrf2/ARE activator 2 promotes Nrf2 nuclear translocation, leading to antioxidant gene upregulation and enhanced cellular defense against oxidative stress. Keap1/Nrf2/ARE activator exhibits robust neuroprotection against both H2O2- and Scopolamine (SCA) (HY-N0296)-induced injury in PC12 cells. Keap1/Nrf2/ARE activator 2 ameliorates memory impairment and the neuro-inflammation associated with SCA-initiated cognitive dysfunction in a zebrafish model. Keap1/Nrf2/ARE activator 2 can be used for the research of Alzheimer's disease .
Referencia número: HY-182354
No. CAS: 861877-12-5
VEGFR2-IN-84 is an orally active, multi-targeted tyrosine kinase inhibitor based on a naphthalene ring scaffold. VEGFR2-IN-84 inhibits VEGFR2 with sub-nanomolar affinity and broadly targets kinases including Kit, FGFR, PDGFR, and Ret. By competitively binding to the ATP-binding pocket, VEGFR2-IN-84 blocks the phosphorylation of VEGFR2 and its downstream AKT/ERK signaling pathway, thereby significantly inhibiting endothelial cell proliferation, migration, and tumor angiogenesis. VEGFR2-IN-84 exhibits broad-spectrum antiproliferative activity against various solid tumors such as liver cancer, lung cancer, and renal cancer, shows weak toxicity to normal cells, and has superior potency to Lenvatinib (HY-10981). VEGFR2-IN-84 possesses favorable pharmacokinetic properties and high safety (LD50>2000 mg/kg), and can be used in related studies of various malignant tumors .
Referencia número: HY-184044
No. CAS: 13112-05-5
Target:
Áreas de investigación:
P2X2R antagonist-1 (compound 66) is a P2X2 receptor antagonist derived from Reactive Blue 4 (HY-125815). P2X2R antagonist-1 shows high selectivity for P2X4, P2X7, P2Y2, P2Y4, P2Y6 and P2Y12 receptors, moderate selectivity for P2X1 and P2X3 receptors, and exhibits higher potency toward homomeric P2X2 receptors than heteromeric P2X2/3 receptors. P2X2R antagonist-1 competitively inhibits ATP-mediated currents. P2X2R antagonist-1 can be used in research related to pain and urinary incontinence .
Synonyms: Citronic acid (Standard); Methylfumaric acid (Standard)
Synonyms: DHEA sulfate sodium (Standard); Prasterone sulfate sodium (Standard)
Category:
Referencia número: HY-N3097
No. CAS: 18836-52-7
Referencia número: HY-N3097R
No. CAS: 18836-52-7
Referencia número: HY-W778236
No. CAS: 1346603-47-1
Synonyms: SAN 9789-13C,d3
Áreas de investigación:
Norflurazon- 13C,d3 (SAN 9789- 13C,d3) is the d3, 13C-labeled Norflurazon (HY-114849). Norflurazon (SAN 9789) is a pre-emergence Herbicide. Norflurazon non-competitively inhibits phytoene desaturase by competing with the enzyme cofactor and disrupts carotenoid biosynthesis, thereby leading to chlorophyll photodegradation and chlorosis. Norflurazon inhibits MGDG synthase, CDP-choline phosphotransferase, Omega-3 FAD7 desaturase, and PG delta-3-trans desaturase, and activates LysoPC-acyltransferase and Omega-3 FAD3 desaturase. Norflurazon inhibits photosynthetic membrane organization, mitochondrial respiration, ATP production, PI3K signaling, and ERK1/2 phosphorylation. Norflurazon activates MAPK P38 phosphorylation and ER stress signaling. Norflurazon induces morphological malformations and cardiovascular effects in zebrafish embryos .
Target:
PROTACs CDK AAK1 Cyclin G-associated Kinase (GAK) Salt-inducible Kinase (SIK) LIM Kinase (LIMK) Wee1 SnRK
Áreas de investigación:
RSS0680 is a small noncoding RNA (sRNA) targeting the mRNA ribosome binding site (RBS) and a PROTAC. RSS0680 competitively binds to RBS through the conserved CCUCCUCCC anti-Shine-Dalgarno (aSD) sequence and inhibits the translation initiation of target genes. RSS0680 can interact with the DUF1127 protein CcaF1, regulate its own stability and participate in bacterial oxidative stress defense, enhancing the host's resistance to heat shock and oxidative damage by affecting pathways such as C1 metabolism and pyruvate dehydrogenase complex. RSS0680 degrades AAK1, CDK1, CDK16, CDK2, CDK4, CDK6, EIF2AK4, GAK, LATSl, LIMK2, MAPK6, MAPKAPK5, MARK2, MARK4, MKNK2, NEK9, RPS6KB1, SIK2, SNRK, STK17A, STK17B, STK35, and WEEl. RSS0680 can be used to study diseases or disorders mediated by aberrant kinase activity and regulatory mechanisms of noncoding RNAs in α-proteobacteria[1][2].
Referencia número: HY-187396
Target:
Áreas de investigación:
FD1-C10-CB is a PROTAC degrader targeting the BRD4 protein. FD1-C10-CB binds to FEM1B to form a ternary complex with BRD4, achieving FEM1B-dependent degradation of BRD4 via the ubiquitin-proteasome system. FD1-C10-CB binds to CD36 to mediate endocytic cellular delivery, thereby enhancing its degrading activity. FD1-C10-CB mediates protein degradation through the Cullin-dependent ubiquitin-proteasome pathway, rather than the lysosomal autophagy pathway. FD1-C10-CB induces a decrease in BRD4 protein levels, and its degrading activity is competitively inhibited by FL47 or JQ1. FD1-C10-CB can be used in the research of breast cancer and osteosarcoma .
Referencia número: HY-30004
No. CAS: 22059-21-8
Target:
Referencia número: HY-B0364AR
No. CAS: 536-43-6
Synonyms: Dyclocaine hydrochloride (Standard)
Dyclonine hydrochloride (Standard) (Dyclocaine hydrochloride (Standard)) is the analytical standard of Dyclonine hydrochloride (HY-B0364A). This product is intended for research and analytical applications. Dyclonine hydrochloride (Dyclocaine hydrochloride) is an orally active, blood-brain barrier-permeable piperidine phenylacetone small molecule commonly used as a local anesthetic. Dyclonine hydrochloride acts as a highly selective allosteric antagonist of TRPV3; it also reversibly inhibits G9a, ALDH2 and ALDH3A1, non-competitively blocks AChE. Dyclonine hydrochloride activates the Nrf2/ARE pathway, relieves the epigenetic silencing of FXN, blocks Aβ42 aggregation, and promotes remyelination and reparative polarization of microglia. Dyclonine hydrochloride alleviates pruritus via TRPV3 inhibition; it is used in studies of neurodegenerative disease models based on its AChE inhibitory, antioxidant and remyelinating effects; it sensitizes drug-resistant tumors through ALDH inhibition, and combined use with protease inhibitors induces more tumor cell apoptosis; it inhibits Candida albicans in vitro. Dyclonine hydrochloride can be used for research on multiple diseases including neurodegenerative diseases, cancer and pruritic dermatitis .
Referencia número: HY-B0364AS
Synonyms: Dyclocaine-d9 hydrochloride
Referencia número: HY-W011927
No. CAS: 80-09-1
Synonyms: Bisphenol S; Bis(4-hydroxyphenyl) sulfone
Referencia número: HY-W016409R
No. CAS: 3943-89-3
Synonyms: Protocatechuic acid ethyl ester (Standard)
Category:
Referencia número: HY-W154247
No. CAS: 103313-38-8
IP6C is a specific inhibitor and phage sensitizer targeting type II Thoeris systems. IP6C competitively binds to histidine in the catalytic pocket of ThsB, blocks the production of the His-ADPR alarm signal and inhibits ThsA activation, thereby relieving bacterial stasis of phage replication. IP6C selectively resensitizes drug-resistant bacteria carrying type II Thoeris systems (such as Pseudomonas aeruginosa) to phage lysis, without affecting other bacteria, and shows no toxicity to mice and human cell lines. IP6C significantly improves the survival rate of infected mice, and can be used to overcome bacterial phage defense mechanisms and study Pseudomonas aeruginosa infections .
Thoeris system: (named after the Egyptian goddess of fertility and protection), is a widespread anti-phage immune defense system in bacteria and archaea. Thoeris system belongs to the "Abortion Infection (Abi)" mechanism of bacteria: when an individual bacterium detects phage invasion, it initiates a suicide program and dies, thereby blocking phage replication and spread, and protecting the surrounding bacterial population from infection.
Thoeris system: (named after the Egyptian goddess of fertility and protection), is a widespread anti-phage immune defense system in bacteria and archaea. Thoeris system belongs to the "Abortion Infection (Abi)" mechanism of bacteria: when an individual bacterium detects phage invasion, it initiates a suicide program and dies, thereby blocking phage replication and spread, and protecting the surrounding bacterial population from infection.
Referencia número: HY-W748758
Synonyms: NSC 108165-d8; Navan-d8; Navane-d8
Referencia número: HY-W778057
No. CAS: 1330195-40-8
Synonyms: Protocatechuic acid ethyl ester-13C3
Referencia número: HY-118156
No. CAS: 155238-60-1
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
Referencia número: HY-12017C
No. CAS: 1159490-83-1
Target:
Áreas de investigación:
Cardiovascular Disease Neurological Disease Inflammation/Immunology Endocrinology Cancer
PF-04217903 phosphate is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a Ki value of 4.8 nM and a Kd value of 4.5 nM. PF-04217903 phosphate blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 phosphate suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 phosphate retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 phosphate increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 phosphate is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis) .
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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
