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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
10 Results for "
active conformational state
" in MedChemExpress (MCE) Product Catalog:
Products (10)
10 Results for "active conformational state" in MCE Product Catalog:
1
1 Cited Publications
Cat. No.: HY-160406
CAS No.: 2332803-84-4
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SNX281 is a selective STING agonist, with IC50 values of 4.1, 4.5, 10.7, and 3.7 μM against human, mouse, rat, and monkey STING, respectively. SNX281 undergoes homodimerization at the STING binding site, triggering a conformational shift of STING from an inactive open state to an active closed state, thereby driving downstream STING-dependent signaling pathways. SNX281 induces type I interferons, IFN-β, TNF-α, IL-6, cytokine release, T cell responses, and long-lasting immune memory. SNX281 exhibits anti-tumor activity and is applicable to research related to colorectal cancer, melanoma, advanced solid tumors, lymphoma, and ovarian cancer .
Cat. No.: HY-173521
CAS No.: 3026520-19-1
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JNJ-9676 is an orally active Coronavirus M protein inhibitor and selective Sarbecovirus inhibitor. JNJ-9676 binds to the M protein dimer and forces the protein into an alternative conformational state with a compound-induced binding pocket. JNJ-9676 demonstrates in vitro nanomolar antiviral activity against SARS-CoV-2, SARS-CoV and Sarbecovirus strains from bat and pangolin zoonotic origin .
Cat. No.: HY-177425
CAS No.: 152674-95-8
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AM11542 is a cannabinoid receptor 1 (CB1) agonist with a human CB1 Ki of 0.11 nM. AM11542 stabilizes the active conformational state of the CB1 receptor. AM11542 can be used for the research of obesity .
Cat. No.: HY-186310
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ISRACT-02 is a eIF2B modulator. The Kd values of ISRACT-02 for eIF2B WT and eIF2B Δ-latch are 174 nM and 385 nM, respectively. Depending on the conformation of its amide bond (trans or cis), ISRACT-02 binds to and stabilizes the inactive conformation (I-state) or active conformation (A-state) of eIF2B, respectively. ISRACT-02 can be used in studies related to leukodystrophy, Alzheimer's disease, traumatic brain injury, and Down syndrome .
Cat. No.: HY-Z20873
CAS No.: 84210-35-5
MK-4815 is an orally active small-molecule allosteric inhibitor of Falcilysin (FLN) with antimalarial activity. MK-4815 inhibits the viability of Plasmodium falciparum NF54 and Dd2 strains with IC50 values of 38 and 40 ng/mL, respectively. MK-4815 preferentially accumulates in erythrocytes containing mature trophozoite/schizont-stage parasites. MK-4815 preferentially binds to the partially closed conformation of FLN, shifting the FLN conformational equilibrium toward the partially closed state and restricting the hinge region-mediated transition from the partially closed state to the open state, thereby interfering with the catalytic cycle of FLN. MK-4815 can be used for malaria-related research .
Cat. No.: HY-189244
CAS No.: 3103996-88-6
RSV-IN-14 is an orally active pre-fusion F protein inhibitor of respiratory syncytial virus (RSV), with a Kd of 5.0 μM, and exhibits lung-targeted distribution properties. RSV-IN-14 binds to the central cavity of the trimeric pre-fusion F protein, locks it in the pre-fusion state, and inhibits the conformational changes required for membrane fusion to block viral entry. RSV-IN-14 suppresses respiratory syncytial virus-induced syncytium formation. RSV-IN-14 can be used in studies on respiratory syncytial virus infection .
Cat. No.: HY-P991964
Synonyms: Rendomab-B49
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Cat. No.: HY-P1609
CAS No.: 105116-61-8
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Cat. No.: HY-19896A
CAS No.: 1204956-74-0
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COTI-2 hydrochloride is an orally active thiosemicarbazone anticancer agent and p53 mutant activator. COTI-2 hydrochloride induces Apoptosis. COTI-2 hydrochloride triggers the activation of AMPK and the inhibition of the mTOR pathway. COTI-2 hydrochloride induces DNA damage and replication stress responses. COTI-2 hydrochloride binds to misfolded mutant p53 proteins, thereby inducing conformational changes that restore p53 to its normal state and reactivate its function. COTI-2 hydrochloride acts on a variety of cancer cell lines and xenografts. COTI-2 hydrochloride can be used in research related to colorectal cancer, small cell lung cancer, glioblastoma, breast cancer, and ovarian cancer .
Cat. No.: HY-184501
CAS No.: 486440-74-8
UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2. UE01 activates hULK1 with an EC50 of 695.30 nM and a KD of 114.3 nM for ULK1; it inhibits hERK1 with an IC50 of 179.90 nM and a KD of 114 nM for ERK1; it shows weak binding to ERK2 with a KD of 2.8 mM. UE01 induces the conformational transition of ULK1 from an inactive to an active state, enhances the phosphorylation of ULK1 Ser317 and mAtg13 Ser355, and reduces the phosphorylation of ULK1 Ser757. UE01 competitively occupies the ATP-binding pocket of ERK1, inhibits ERK1 kinase activity, and reduces the activity of the ERK1/2 signaling pathway. UE01 induces complete autophagy flux and apoptosis, upregulates Atg5, Atg7, LC3-II/LC3-I, Bax, cytochrome C (Cyt c), Cleaved-Caspase 3, Cleaved-PARP1 and E-cadherin, downregulates p62, Bcl-2, MMP-2 and MMP-9, reduces the phosphorylation of Exo70 Ser250, and promotes the proteasome-dependent degradation of Cav-1, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation. UE01 can be used in studies related to triple-negative breast cancer .
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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
