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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
367 Results for "
Lead optimisation
" in MedChemExpress (MCE) Product Catalog:
Products (367)
367 Results for "Lead optimisation" in MCE Product Catalog:
657
657 Publications Verification
Synonyms: SB 203580; RWJ 64809
Adezmapimod (SB 203580) is a selective and ATP-competitive p38 MAPK inhibitor with IC50s of 50 nM and 500 nM for SAPK2a/p38 and SAPK2b/p38β2, respectively. Adezmapimod inhibits LCK, GSK3β and PKBα with IC50s of 100-500-fold higher than that for SAPK2a/p38. Adezmapimod can inhibit p38 MAPK and lead to the inhibition of downstream HSP27 phosphorylation. Adezmapimod does not disrupt JNK activity and is an autophagy and mitophagy activator .
61
Ciprofloxacin (Bay-09867) is a potent, orally active topoisomerase IV inhibitor. Ciprofloxacin induces mitochondrial DNA and nuclear DNA damage and lead to mitochondrial dysfunction, ROS production. Ciprofloxacin has anti-proliferative activity and induces apoptosis. Ciprofloxacin is a fluoroquinolone antibiotic, exhibiting potent antibacterial activity .
16
16 Cited Publications
CCG-1423 is an inhibitor of Rho/MRTF/SRF pathway. CCG-1423 shows activities in several cancer cells. CCG-1423 is a promising lead compound for the development of novel pharmacologic tools, and it can be used for the research of cancer and diabetes .
10
Target:
Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology
10
Target:
Research Areas:
Cardiovascular Disease Metabolic Disease Inflammation/Immunology
8
Research Areas:
Lysozyme (Muramidase) is a conserved antimicrobial protein. Lysozyme exerts its bactericidal effect by hydrolyzing bacterial cell wall peptidoglycan (PG). Lysozyme plays an important role in limiting bacterial growth on mucosal surfaces and other sites, not only controlling potential pathogens but also limiting overgrowth of microbiota to prevent dysbiosis. Extracellular lysozyme can also degrade polymeric PG into soluble fragments, activate NOD receptors in mucosal epithelial cells, and lead to the secretion of chemokines and activating factors by neutrophils and macrophages .
7
5
5 Cited Publications
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Research Areas:
A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases .
5
5 Cited Publications
Cat. No.: HY-N0498
CAS No.: 13063-04-2
4
Category:
Triterpenes Plant Terpenoids Panax ginseng C. A. Meyer Extract Disease Research Fields Cancer Araliaceae Extract
Target:
3
Category:
Neurological Disease Metabolic Disease Other Families Extract Endogenous metabolite Indole Alkaloids Infection Alkaloids Human Gut Microbiota Metabolites Plant Disease Research Fields Endocrinology
Target:
3
Target:
Research Areas:
Phenylthiourea (Phenylthiocarbamide) is an inhibitor for phenoloxidase. Phenylthiourea inhibits enzymatic oxidation of DOPA by phenoloxidase (Ki = 0.21 μM). Phenylthiourea is an effective inhibitor for tyrosinase. Phenylthiourea can lead to graying of hair in black rats due to the interference with melanin formation .
3
3 Cited Publications
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Research Areas:
SH-42 is a potent and selective inhibitor of human Δ 24-dehydrocholesterol reductase (DHCR24), with an IC50 of 42 nM. SH-42 can lead to a significant increase in plasma desmosterol levels of mice .
3
3 Cited Publications
Synonyms: 2,2'-Azodiisobutyramidine dihydrochloride
Target:
Research Areas:
AAPH (2,2'-Azodiisobutyramidine dihydrochloride) has an effect of radical generation. AAPH induces oxidative stress and erythrocyte hemolysis . AAPH decomposes at 37°C to generate an alkyl radical, is used as an initiator. In the presence of oxygen, these alkyl radicals will be converted to peroxyl radicals that can cause lipid peroxidation and loss of erythrocyte membrane integrity, which could ultimately lead to hemolysis .
3
3 Cited Publications
Cat. No.: HY-163731
CAS No.: 3077196-25-6
Research Areas:
EGR-1-IN-1 is a EGR-1 inhibitor with an IC50 of 1.86 μM. EGR-1-IN-1 binds to the zinc finger DNA-binding domain of EGR-1 and promotes the dissociation of the EGR-1-DNA complex. EGR-1-IN-1 reduces the mRNA expression levels of EGR-1-regulated inflammatory genes induced by TNFα. EGR-1-IN-1 alleviates atopic dermatitis-like lesions in the ear skin of mice. EGR-1-IN-1 serves as a lead compound for the development of targeted compounds for inflammatory skin diseases. EGR-1-IN-1 can be used in studies related to atopic dermatitis .
2
2 Cited Publications
Synonyms: JNJ-67856633
Safimaltib (JNJ-67856633) is an orally active, first-in-class, potent, selective and allosteric MALT1 protease inhibitor. Safimaltib in some cases lead to tumor stasis .
2
2 Cited Publications
DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity .
2
2 Cited Publications
AN3661, a potent antimalarial lead compound, targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue subunit 3 (PfCPSF3). AN3661 inhibits Plasmodium falciparum laboratory-adapted strains (mean IC50=32 nM), Ugandan field isolates (mean ex vivo IC50=64 nM), and murine P. berghei and P. falciparum infections .
2
2 Cited Publications
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Research Areas:
Glatiramer acetate, a synthetic analogue of myelin basic protein and an immunomodulating agent, inhibits Experimental autoimmune encephalomyelitis (EAE), and can be used for the research of multiple sclerosis. Glatiramer acetate exhibits strong and promiscuous binding to MHC molecules and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression .
2
CID44216842 (Cdc42-IN-1) is a potent Cdc42-selective guanine nucleotide binding lead inhibitor. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 1.0 and 1.2 μM in GTP binding assay, respectively. The EC50s for Cdc42 WT and Cdc42Q61L mutant are 0.3 and 0.5 μM in GDP binding assay, respectively. Use as a molecular probe .
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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
