Scientific Reviews
Product Guides
Blogs
Topics
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
32 Results for "
displacement
" in MedChemExpress (MCE) Product Catalog:
Products (32)
32 Results for "displacement" in MCE Product Catalog:
5
5 Cited Publications
Cat. No.: HY-D1594
CAS No.: 217190-24-4
4
2
2 Cited Publications
Target:
Research Areas:
JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
2
1
1 Cited Publications
Target:
Research Areas:
Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
Cat. No.: HY-P5908F
Target:
Research Areas:
Dextranase, Trichoderma reesei belongs to glycoside hydrolase family 49. It catalyzes the hydrolysis of α-1,6-glycosidic linkages in dextran via a single-displacement reaction, ultimately releasing shorter isomaltooligosaccharides. Dextranase, Trichoderma reesei reduces the molecular size of dextran, inhibits the formation of insoluble dextran and dental plaque, and decreases the viscosity of dextran-contaminated sugar juice. Dextranase, Trichoderma reesei can be used in relevant research in fields such as chemical production, including beer manufacturing, feed additives, and toothpaste formulations .
Cat. No.: HY-N8723
CAS No.: 51095-86-4
Category:
Target:
Synonyms: AZD-3355 hydrochloride
Target:
Research Areas:
Lesogaberan (AZD-3355) hydrochloride is a potent and selective GABAB receptor agonist with an EC50 of 8.6 nM for human recombinant GABAB receptor. The affinity (Kis) of Lesogaberan hydrochloride for rat GABAB and GABAA receptors, as measured by displacement of [ 3H]GABA binding in brain membranes: 5.1 nM and 1.4 μM, respectively. Lesogaberan hydrochloride inhibits transient lower esophageal sphincter relaxation through a peripheral mode of action .
Cat. No.: HY-W013330
CAS No.: 3608-58-0
Synonyms: Guanosine, 3'-deoxy-
Research Areas:
3′-Deoxyguanosine (Guanosine, 3'-deoxy-) is a derivative of Guanosine (HY-N0097). 3′-Deoxyguanosine interacts with human purine nucleoside phosphorylase via hydrogen bonding with residues such as Glu201 and Asn243. 3′-Deoxyguanosine exhibits moderate displacement activity for [ 3H]-guanosine in rat meninges. 3′-Deoxyguanosine is useful for studying the mechanism of guanosine receptors and purine metabolism .
Cat. No.: HY-DY1076
CAS No.: 217190-24-4
Solvent and concentration: DMSO: 2 mM
Target:
Research Areas:
JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
Cat. No.: HY-18164
CAS No.: 945725-50-8
Target:
Research Areas:
TASP0277308 is a highly selective S1P1 antagonist. TASP0277308 possesses immunomodulatory activities, including lymphopenia, a block in T cell egress from the thymus, marginal zone B cell displacement, and the upregulation of CD69 expression on lymphocytes. TASP0277308 can be used for the research of collagen-induced arthritis in mice .
Cat. No.: HY-125209A
CAS No.: 2253744-57-7
Target:
Research Areas:
TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .
Cat. No.: HY-W009722A
CAS No.: 20624-25-3
Synonyms: Ditiocarb sodium trihydrate, ACS, 99.0%
Cat. No.: HY-117167
CAS No.: 219691-94-8
Target:
Research Areas:
KB-141 is a potent and selective TRβ agonist. The IC50 values are 23.9 nM and 3.3 nM for binding affinities from displacement of T3 from hTRα1 and hTRβ1, respectively. KB-141 has anti-obesity, anti-diabetic, and lipid-lowering effects?and can be used as an anti-cholesteremic agent in vivo .
Cat. No.: HY-179109
Research Areas:
EIF2B-IN-1 (Compound A) is an eIF2B inhibitor. EIF2B-IN-1 binds eIF2B. EIF2B-IN-1 stabilises the eIF2B decamer and favours inhibitory eIF2B:eIF2(αP) complex formation. EIF2B-IN-1 exhibits weak displacement of ISRIB. EIF2B-IN-1 can be used in the research of integrated stress responses .
Cat. No.: HY-124308
CAS No.: 1221964-50-6
PS315, a derivative of PS48 (HY-15967), is an allosteric PKC inhibitor by binding to the PIF-pocket of aPKC and inducing a displacement of the active site residue Lys111. PS315 inhibits the full-length and catalytic domain constructs of PKCζ (IC50=10 μM) and PKCη (IC50=30 μM). PS315 has anti-cancer activity .
Cat. No.: HY-N17676
CAS No.: 72424-02-3
Category:
Target:
- 1
- 2
-
-
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
