98 Results for "

Burden

" in MedChemExpress (MCE) Product Catalog:
Products (98)

98 Results for "Burden" in MCE Product Catalog:

45
45 Publications Verification
Cat. No.: HY-N0176
CAS No.: 71939-50-9
Synonyms: Dihydroqinghaosu; β-Dihydroartemisinin; Artenimol
Dihydroartemisinin is an orally active metabolite of rtemisinin (HY-B0094) and antimalarial agent. Dihydroartemisinin induces Autophagy by inhibiting NF-κB activation. Dihydroartemisinin promotes ROS accumulation. Dihydroartemisinin exhibits anticancer activity in esophageal cancer cells. Dihydroartemisinin shows schistosomicidal activity against juvenile and adult worms of Schistosoma japonicum, reduces worm burden, and displays antiparasitic activity. Dihydroartemisinin can be used in research related to multiple myeloma, promyelocytic leukemia, esophageal cancer, and Schistosoma japonicum infection .
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24
24 Cited Publications
Cat. No.: HY-13032B
CAS No.: 1895049-20-3
Purity:  97.04%
Synonyms: GSK 525762C; I-BET 762 besylate
Research Areas:  

Cancer

Molibresib besylate (GSK 525762C; I-BET 762 besylate) is an orally active pan-BET inhibitor that targets and binds to BRD2, BRD3, BRD4 and BRDT. By competitively occupying acetylated lysine binding sites, Molibresib besylate disrupts the interaction between BET proteins and chromatin, thereby effectively inhibiting MYC expression and target gene transcription. Molibresib besylate exhibits broad antiproliferative activity, which not only inhibits cancer cell growth and induces growth arrest, but also downregulates mitosis-related genes and upregulates the level of p-ERK1/2. When combined with MEK inhibitors, Molibresib besylate shows a significant synergistic effect, reduces tumor burden in mouse models of leukemia, modulates the immune microenvironment and prolongs survival. Molibresib besylate is widely applicable to research related to acute myeloid leukemia, multiple myeloma, triple-negative breast cancer, small-cell lung cancer and various advanced refractory solid tumors .
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5
5 Cited Publications
Cat. No.: HY-N0430A
CAS No.: 1198398-71-8
Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
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2
2 Cited Publications
Cat. No.: HY-141429A
CAS No.: 3115178-55-4
Purity:  99.15%
Research Areas:  

Cancer

AS-99 TFA is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity. AS-99 TFA blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
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2
2 Cited Publications
Cat. No.: HY-141429
CAS No.: 2323623-93-2
Research Areas:  

Cancer

AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 µM, Kd= 0.89 µM) with anti-leukemic activity. AS-99 blocks cell proliferation, induces apoptosis and differentiation, downregulates MLL fusion target genes, and reduces the leukemia burden in vivo .
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1
1 Cited Publications
Cat. No.: HY-A0169A
CAS No.: 79416-27-6
Research Areas:  

Cancer

Methyl aminolevulinate hydrochloride is a sensitizer used in photodynamic therapy (PDT). Methyl aminolevulinate hydrochloride penetrates the skin and induces the production of photoactive porphyrins including protoporphyrin IX in cells; upon exposure to appropriate light, it generates ROS, which triggers cellular oxidation and cell death. Methyl aminolevulinate hydrochloride acts as a photo-damage reversing agent through epidermal reconstruction, cytokine-mediated activation of dermal fibroblasts, elastin breakdown, new collagen formation, and compression of dilated capillaries. Methyl aminolevulinate hydrochloride reduces the expression of the proliferation marker Ki-67 and the early skin carcinogenesis marker TP53. Methyl aminolevulinate hydrochloride delays the onset of ultraviolet-induced skin tumors and reduces tumor burden in hairless mice. Methyl aminolevulinate hydrochloride is applicable to research related to actinic keratosis and basal cell carcinoma .
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1
1 Cited Publications
Cat. No.: HY-132182
CAS No.: 383418-30-2
Purity:  99.4%
Research Areas:  

Neurological Disease Cancer

HPA-12 is a blood-brain barrier-permeable small-molecule inhibitor of ceramide transfer protein (CERT) with four stereoisomers (the (1R,3R)-stereoisomer exhibits the highest activity). HPA-12 blocks the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus by binding to the START domain of CERT, leading to intracellular ceramide accumulation and inhibition of sphingomyelin (SM) synthesis. HPA-12 induces endoplasmic reticulum stress via the GRP78/ATF6/CHOP axis and activates mitochondrial autophagy, thereby inhibiting cell growth and inducing apoptosis. In in vivo experiments, HPA-12 significantly reduces the leukemia burden and splenomegaly in mouse models of acute myeloid leukemia (AML) and prolongs survival. HPA-12 is applicable for the research of lipid metabolism in acute myeloid leukemia and Alzheimer's disease .
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1
1 Cited Publications
Cat. No.: HY-148422
CAS No.: 1139253-73-8
Purity:  99.40%
Research Areas:  

Cancer

Rohinitib is a potent and specific eIF4A inhibitor. Rohinitib induces cell apoptosis of acute myeloid leukemia (AML) cell lines and reduces the leukemia burden of AML xenograft model. Rohinitib can be used for the research of AML .
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Cat. No.: HY-P10761
CAS No.: 2941391-49-5
DPI-4452 is a CAIX-targeting cyclic peptide with a DOTA cage, and can be chelated with radionuclide for CAIX-expressing tumor PET-CT imaging and study. DPI-4452 specifically and selectively binds CAIX without interaction with an in vitro off-target receptor panel of 55 targets (IC50 for recombinant hCAIX: 130 nM). Radiolabeled DPI-4452 inhibits tumor growth in HT-29 and SK-RC-52 xenograft mouse models . DPI-4452 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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Cat. No.: HY-159520
CAS No.: 2731294-23-6
Synonyms: Ofirnoflast; HT-6184
Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia .
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Cat. No.: HY-156794
CAS No.: 2412555-70-3
Purity:  99.88%
Synonyms: DSP-5336
Research Areas:  

Cancer

Enzomenib (DSP-5336) is an orally active Menin inhibitor (IC50=1.4 nM, Kd=6.0 nM). Enzomenib disrupts the interaction between Menin and KMT2A/MLL fusion proteins, specifically inhibits the expression of leukemia driver genes such as HOX/MEIS1, and upregulates ITGAM. Enzomenib effectively induces cell differentiation, inhibits tumor cell proliferation, and suppresses primitive cell colony formation. Enzomenib reduces disease burden and prolongs survival, but causes adverse reactions including differentiation syndrome and QTc interval prolongation. Enzomenib is used for research on relapsed/refractory acute myeloid leukemia, acute lymphoblastic leukemia, and other hematologic malignancies with mixed lineage leukemia (MLL) rearrangements or NPM1 mutations .
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Cat. No.: HY-W025784
CAS No.: 143-66-8
Synonyms: Sodium tetraphenylborate; Tetraphenylboron sodium
Kalibor (Sodium tetraphenylborate; Tetraphenylboron sodium) is a boron-based salt and antibacterial agent. Kalibor exerts activity against Neisseria meningitidis and Neisseria gonorrhoeae. Kalibor facilitates boron uptake by Neisseria meningitidis cells. Kalibor reduces bacterial burden in a mouse model of Neisseria meningitidis bacteremia. Kalibor can be used for the research of bacterial infection, such as meningococcal bacteremia .
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Cat. No.: HY-P9983
CAS No.: 166089-32-3
Synonyms: SGN-33; HuM-195; GLK-33 Antibody
Lintuzumab (HUM-195) is an anti-CD33 humanized monoclonal antibody. Lintuzumab reduces the production of TNFα-induced pro-inflammatory cytokines and chemokines by AML cells. Lintuzumab promotes tumor cell killing through antibody-dependent cellular cytotoxicity (ADCC) and phagocytosis (ADCP) activities against MDR and MDR+ AML cell lines and primary AML patient samples. Lintuzumab enhances survival and reduces tumor burden in mice .
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Cat. No.: HY-162596
CAS No.: 1973494-16-4
Synonyms: BA-1049 free base
Target:  

ROCK

Research Areas:  

Neurological Disease

NRL-1049 (BA-1049 (free base)) is an orally available and selective ROCK2 inhibitor with IC50 values of 0.59 µM for ROCK2 and 26 µM for ROCK1, respectively. NRL-1049 modulates ROCK signaling, preserves blood-brain barrier integrity, reduces edema, seizures and hemorrhage, and alleviates cerebral cavernous malformation lesion burden. NRL-1049 can be used for the study of acute brain injury, ischemic stroke, and cerebral cavernous malformations .
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Cat. No.: HY-P991621
Synonyms: EOS-215

Target:  

TREM receptor

Research Areas:  

Cancer

EOS006215 (EOS-215) is a humanized monoclonal antibody targeting TREM-2. EOS006215 competes with TREM2 ligands, prevents TREM2 multimerization, and blocks downstream signaling. EOS006215 inhibits efferocytosis, reprograms transcriptomic profiles of monocyte-derived macrophages, alters metabolism and immune response genes, and increases pro-inflammatory marker secretion. EOS006215 reduces metastasis burden, delays tumor growth, and reprograms the tumor microenvironment to overcome anti-PD-1 resistance. EOS006215 can be used for the research of triple negative breast cancer and colorectal cancer .
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Cat. No.: HY-B1073
CAS No.: 26155-31-7
Target:  

Parasite

Research Areas:  

Infection

Morantel tartrate is an anthelmintic agent. Sustained-release three-layer composite tablets of Morantel tartrate are administered orally and release after exposure to rumen fluid. Morantel tartrate reduces the fecal egg output and worm burden of gastrointestinal nematodes in Hereford calves. Morantel tartrate is used in research related to gastrointestinal nematode infections .
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Cat. No.: HY-108894
CAS No.: 722492-56-0
Purity:  95.00%
Ferumoxytol is an FDA-approved ultrasmall superparamagnetic iron oxide preparation and iron replacement agent that exerts selective activity against leukemia cells with low ferroportin expression. Ferumoxytol increases intracellular iron levels, induces reactive oxygen species (ROS) production via the Fenton reaction, and triggers oxidative stress and cell death. Ferumoxytol reduces disease burden in mouse models and patient-derived leukemia models. As an MRI contrast agent, Ferumoxytol enables imaging of vascular lesions, tumors and lymph nodes. Ferumoxytol can be used in research related to acute myeloid leukemia and blast-phase chronic myeloid leukemia .
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Cat. No.: HY-N0176R
CAS No.: 71939-50-9
Synonyms: Dihydroqinghaosu (Standard); β-Dihydroartemisinin (Standard); Artenimol (Standard)
Dihydroartemisinin (Standard) (Dihydroqinghaosu (Standard)) is the analytical standard of Dihydroartemisinin (HY-N0176). This product is intended for research and analytical applications. Dihydroartemisinin is an orally active metabolite of rtemisinin (HY-B0094) and antimalarial agent. Dihydroartemisinin induces Autophagy by inhibiting NF-κB activation. Dihydroartemisinin promotes ROS accumulation. Dihydroartemisinin exhibits anticancer activity in esophageal cancer cells. Dihydroartemisinin shows schistosomicidal activity against juvenile and adult worms of Schistosoma japonicum, reduces worm burden, and displays antiparasitic activity. Dihydroartemisinin can be used in research related to multiple myeloma, promyelocytic leukemia, esophageal cancer, and Schistosoma japonicum infection .
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Cat. No.: HY-N0430
CAS No.: 3486-66-6
Synonyms: Coptisin
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
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Cat. No.: HY-P990078
CAS No.: 2571940-41-3
Synonyms: LY3372993

Target:  

Amyloid-β

Research Areas:  

Neurological Disease

Remternetug (LY3372993) is a monoclonal antibody that targets pyroglutamylated amyloid β fibrils (N3pG-Aβ). Remternetug specifically binds to N3pG-Aβ, thereby clearing amyloid plaques in the brain and reducing amyloid burden. Remternetug can be used in research related to Alzheimer's disease .
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