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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
10071 Results for "
activators
" in MedChemExpress (MCE) Product Catalog:
Products (10071)
10071 Results for "activators" in MCE Product Catalog:
Cat. No.: HY-181102
CAS No.: 3081614-92-5
Research Areas:
TGR5 agonist 10 is a selective, allosteric and orally active Takeda G protein coupled receptor 5 (TGR5) agonist with EC50s of 0.8 μM and 0.6 μM for human TGR5 and mouse TGR5, respectively. TGR5 agonist 10 demonstrates selectivity for TGR5 over FXR. TGR5 agonist 10 activates hTGR5 and mTGR5 to induce cAMP accumulation, and positively modulates lithocholic acid functional activity and potency at hTGR5, with higher selectivity for cAMP formation over β-arrestin2 recruitment. TGR5 agonist 10 exerts glucose-lowering effects in Mus musculus oral glucose tolerance tests. TGR5 agonist 10 can be used for the research of diabetes .
Cat. No.: HY-181488
CAS No.: 3097745-69-9
Research Areas:
NLRP3-IN-87 is a selective and orally active NLRP3 inhibitor with a Kd of 0.23 μM. NLRP3-IN-87 binds directly to the NLRP3 NACHT domain, disrupts NLRP3-NEK7 and NLRP3-ASC interactions, inhibits ASC oligomerization, and blocks inflammasome assembly. NLRP3-IN-87 suppresses caspase-1 activation and IL-1β secretion. NLRP3-IN-87 exhibits anti-inflammatory and analgesic activity, reducing joint swelling, inflammation, and pain in an MSU (HY-B2130A)-induced acute gout mouse model. NLRP3-IN-87 can be used for the research of gout .
Cat. No.: HY-181533
Target:
Research Areas:
IAP ligand 9 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 9 selectively targets cIAP1-BIR3, XIAP-BIR3, exhibits extremely weak binding affinity for XIAP-BIR2, with a KD of 100 nM for cIAP1-BIR3 and 10 nM for XIAP-BIR2. IAP ligand 9 can be used to synthesize IAP-recruiting protein degraders (IPD), and can calibrate the cell permeability and cellular-level target binding assays of the IPD molecule SNIPER (TEAD)-1 (HY-181607). IAP ligand 9 and its series of degraders can be used in the research of solid tumors such as malignant pleural mesothelioma associated with abnormal activation of the Hippo pathway .
Cat. No.: HY-181655
CAS No.: 3127060-85-6
Target:
Research Areas:
Anti-hepatic fibrosis agent 3 is an orally active anti-hepatic fibrosis compound targeting Cathepsin D. Anti-hepatic fibrosis agent 3 shows an IC50 of 53.18 μM against COL1A1-promoter and a Kd of 8.86 μM for binding to Cathepsin D. Anti-hepatic fibrosis agent 3 directly binds to and promotes the degradation of Cathepsin D, with no significant effect on Cathepsin B or Cathepsin L. Anti-hepatic fibrosis agent 3 inhibits hepatic stellate cell activation and reduces extracellular matrix deposition and inflammatory cytokine expression. Anti-hepatic fibrosis agent 3 exhibits remarkable anti-fibrotic activity in rat BDL and mouse CDAHFD-induced hepatic fibrosis models. Anti-hepatic fibrosis agent 3 can be used for the study of hepatic fibrosis .
Cat. No.: HY-181838
CAS No.: 3064485-73-7
CIRc-014 is an orally active Cyclin A/B inhibitor with a Cyclin A IC50 of 0.05 μM, Cyclin A Kd of 2.7 nM, Cyclin B IC50 of less than 0.02 μM and Cyclin B Kd of 1.0 nM. CIRc-014 activates the spindle assembly checkpoint and promotes the formation of a complex between Cyclin B and CDK2 by blocking the RxL interaction of Cyclin A/B. CIRc-014 can induce replication stress, DNA damage, mitotic arrest and apoptosis in tumor cells. CIRc-014 showed tumor growth inhibition and regression in NCI-H69 and NCI-H446 small cell lung cancer xenograft models. CIRc-014 can be used for the research of small-cell lung cancer .
Cat. No.: HY-182067
Research Areas:
anti-TNBC agent-15 is a platinum (IV) complex with anti-triple-negative breast cancer activity. anti-TNBC agent-15 inhibits cancer cell viability. anti-TNBC agent-15 reverses the resistance of triple-negative breast cancer cells to Cisplatin (HY-17394), increases intracellular uptake, and effectively triggers apoptosis by inducing DNA damage, enhancing intracellular ROS accumulation and activating the mitochondrial pathway. anti-TNBC agent-15 enhances lipid peroxidation, interferes with the signal transduction of the cystine/glutamate transporter-glutathione peroxidase axis, and induces ferroptosis. anti-TNBC agent-15 significantly inhibits tumor growth in triple-negative breast cancer/Cisplatin xenograft models. anti-TNBC agent-15 can be used for the research of triple-negative breast cancer .
Cat. No.: HY-18252S1
Cat. No.: HY-18252S3
Synonyms: TA1790-13C5
Cat. No.: HY-183070
CXJ2080 is a selective PROTAC-based CDK7 degrader with a DC50 of 0.88 nM. CXJ2080 recruits VHL E3 ligase to induce ubiquitin-proteasome-dependent CDK7 degradation, disrupts the CDK7-cyclin H-MAT1 complex, suppresses CDK7-dependent phosphorylation of RNA polymerase II CTD Ser5, CDK1 Thr161, and CDK2 Thr160. CXJ2080 activates the p53-p21 axis, suppresses MYC-driven signaling, induces leukemia cell cycle arrest, apoptosis, and differentiation, reduces CD117 expression, spares platelets and normal PBMCs, maintains sustained CDK7 degradation post-washout. CXJ2080 can be used for the research of acute leukemia .
Cat. No.: HY-183784
Target:
Research Areas:
P2X7R antagonist-1 is an orally active P2X7 receptor antagonist with an IC50 of 3.57 μM. P2X7R antagonist-1 inhibits the proliferation, invasion and metastasis abilities of cancer cells. P2X7R antagonist-1 downregulates the expression of FAK and MMP-9. P2X7R antagonist-1 suppresses tumor growth and metastasis in a mouse breast cancer model. P2X7R antagonist-1 promotes the activation of CD4 and CD8 T cells. P2X7R antagonist-1 can be used in breast cancer-related research .
Cat. No.: HY-184324
CAS No.: 2975573-18-1
Target:
NF-κB p38 MAPK Reactive Oxygen Species (ROS) Interleukin Related TNF Receptor COX IKK ERK JNK
Research Areas:
Anti-inflammatory agent 116 is an anti-inflammatory agent. Anti-inflammatory agent 116 inhibits the abnormal activation of the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 116 binds to the p50 subunit and impairs the DNA-binding ability of the p65-p50 heterodimer. Anti-inflammatory agent 116 inhibits LPS-induced production of NO and MtROS, secretion of IL-1β and TNF-α, expression of iNOS and COX-2, phosphorylation of IKK, IκB, p65, p38, ERK and JNK, as well as nuclear translocation of p65. Anti-inflammatory agent 116 alleviates sepsis-associated acute liver injury in mice. Anti-inflammatory agent 116 can be used for the research of sepsis-associated acute liver injury .
Cat. No.: HY-184897
CAS No.: 312724-83-7
Target:
Research Areas:
YS-01 is an inhibitor of pendrin (SLC26A4) with pulmonary protective activity. YS-01 inhibits pendrin-mediated anion exchange activity, reduces pendrin expression, and suppresses the activation of NF-κB and the production of proinflammatory cytokines. YS-01 alleviates lipopolysaccharide-induced and ventilator-induced lung injury. YS-01 attenuates ovalbumin-induced airway hyperresponsiveness, inflammatory infiltration, epithelial thickening and goblet cell hyperplasia, and reduces eosinophil and neutrophil counts. YS-01 decreases MUC5AC transcription levels induced by IL-4, reverses the reduction of airway surface liquid volume, and inhibits the increase of apical SCN − concentration in epithelial cells. YS-01 can be used in studies related to lung injury and allergic asthma .
Cat. No.: HY-185899
CAS No.: 72052-96-1
Synonyms: 5-Aza-2'-deoxycytidine-5′-triphosphate
5-Aza-dCTP (5-Aza-2'-deoxycytidine-5′-triphosphate) is a nucleotide analog that acts as a substrate for mammalian DNA polymerase α (Km = 3.0 μM) and a weak competitive inhibitor of this enzyme (Ki = 4.3 μM). 5-Aza-dCTP inhibits DNA polymerase α via incorporation into DNA through Watson-Crick base pairing, inhibits DNA methyltransferases via incorporation into hemimethylated DNA, and induces mutations in HIV-1 via incorporation into viral DNA during synthesis. 5-Aza-dCTP reverses the inhibitory effect of dTTP on dCMP deaminase, and allosterically activates dCMP deamination to the same extent as dCTP. 5-Aza-dCTP is applicable to research related to leukemia and type 1 human immunodeficiency virus infection .
Cat. No.: HY-186151
CAS No.: 1372406-51-3
UCI-LC0019 is a mutant p53 reactivator. UCI-LC0019 binds to mutant p53, induces wild-type-like conformational change, restores sequence-specific DNA binding activity, activates p53-dependent transcription programs, and does not act via thiol reactivity or glutathione depletion. UCI-LC0019 inhibits proliferation and induces apoptosis in cancer cells harboring mutant p53, with no significant effect on p53 null or wild-type p53 tumors cells. UCI-LC0019 exhibits anti-tumor activity in xenograft mouse models carrying p53R175H mutant tumors. UCI-LC0019 can be used for the research of cancer, such as ovarian cancer .
Cat. No.: HY-187930
CAS No.: 2965385-11-7
HPK1-IN-72 is an orally active and selective HPK1/MAP4K1 inhibitor with an IC50 of 52.4 nM against human targets. HPK1-IN-72 inhibits HPK1 activation, blocks the negative regulation of T cell receptor signaling, restores T cell receptor signal transduction and enhances T cell function. HPK1-IN-72 suppresses tumor growth, exhibits potent single-agent anti-tumor efficacy, and also produces synergistic effects with anti-PD-1 antibodies or anti-PD-L1/IL-15 immunocytokine prodrugs. HPK1-IN-72 can be used in research related to breast cancer, colorectal cancer and prostate cancer .
Cat. No.: HY-188012
CAS No.: 2975602-21-0
Synonyms: dMGer
Desmethyl germinone (dMGer) is a KL signaling pathway activator that binds to the human HTL/KAI2 receptor with an IC50 of 46.4 nM. Desmethyl germinone induces conformational changes of the receptor by directly binding to the ligand-binding pocket of KAI2/D14L, promotes the interaction of KAI2/D14L with D3/MAX2 and SMAX1, and leads to SMAX1 degradation. Desmethyl germinone induces seed germination and inhibits hypocotyl elongation in an abscisic acid-independent manner in Arabidopsis thaliana, and inhibits mesocotyl elongation and induces the expression of KL-responsive genes in rice. Desmethyl germinone can be used in studies related to seed germination, dormancy, and the KAI2/KL signaling pathway .
Cat. No.: HY-19205B
CAS No.: 205654-37-1
Research Areas:
(2S,5S)-CMI-392 is the absolute configuration of CMI-392 (HY-19205A). CMI-392 is an orally active dual 5-lipoxygenase inhibitor and platelet-activating factor receptor (PAFR) antagonist, with an IC50 of 10 nM for human PAF receptor and an IC50 of 100 nM for rat 5-lipoxygenase. CMI-392 blocks PAF receptor binding, inhibits leukotriene synthesis, attenuates PAF-induced hemoconcentration, and suppresses arachidonic acid- and TPA-induced ear swelling in mice. CMI-392 reduces inflammatory cell infiltration, decreases MPO levels, alleviates ocular inflammation, and improves dextran sulfate sodium-induced colitis. CMI-392 can be used in the research of inflammatory and immune-related diseases such as colitis and atopic dermatitis .
Cat. No.: HY-19882
CAS No.: 941285-15-0
BAL-30072 is a siderophore-bearing monocyclic β-lactam antibiotic with antibacterial activity. BAL-30072 inhibits penicillin-binding proteins 1a, 1b, and 3, thereby disrupting bacterial cell wall synthesis. BAL-30072 inhibits mitochondrial electron transport chain complex II and complex III, while also inhibiting glycolysis and mitochondrial fatty acid β-oxidation. BAL-30072 induces mitochondrial ROS production, cellular ATP depletion, reduces mitochondrial membrane potential, and triggers hepatocyte apoptosis via caspase-3/7 activation. BAL-30072 is a substrate of the hepatic uptake transporters OAT1 and OAT3. BAL-30072 can be used in research related to bacterial infections .
Cat. No.: HY-34464
CAS No.: 136630-39-2
Synonyms: 2,7-DBCZ
Research Areas:
2,7-Dibromocarbazole (2,7-DBCZ) is an orally active AhR agonist and MAOB inhibitor that can cross the blood-brain barrier. 2,7-Dibromocarbazole induces CYP1A/CYP1B1, developmental toxicity and oxidative toxicity, Akt phosphorylation, apoptosis, mitochondrial depolarization, and calcium elevation. 2,7-Dibromocarbazole disrupts dopamine homeostasis, promotes α-synuclein aggregation and transcriptomic dysregulation, leading to hepatic lipid accumulation, liver lesions, brain injury, and angiogenesis/energy metabolism disorders, while activating ERα and inhibiting GRα. 2,7-Dibromocarbazole can be used in research on cardiotoxicity and Parkinson's disease .
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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
