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
488 Results for "
Conformational constraint
" in MedChemExpress (MCE) Product Catalog:
Products (488)
488 Results for "Conformational constraint" in MCE Product Catalog:
1
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Simufilam (PTI-125) is an orally active FLNA modulator. Simufilam restores NMDAR signaling and Arc expression. Simufilam inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tau protein hyperphosphorylation.
Simufilam can be used for research of Alzheimer's disease .
1
1 Cited Publications
Synonyms: PTI-125 hydrochloride
Target:
Research Areas:
Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Simufilam hydrochloride (PTI-125 hydrochloride) is an orally active FLNA modulator. Simufilam hydrochloride restores NMDAR signaling and Arc expression. Simufilam hydrochloride inhibits overactive mTOR signaling by restoring the normal conformation of FLNA, improves insulin sensitivity, reduces Aβ42-induced neuroinflammation and tau protein hyperphosphorylation. Simufilam hydrochloride can be used for research of Alzheimer's disease .
1
1 Cited Publications
Research Areas:
BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen I and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease .
1
1 Cited Publications
Target:
Research Areas:
NVP-DKY709 is an orally active and selective IKZF2 molecular glue degrader with the Dmax and DC50 of 53% and 4 nM, respectively. In addition, NVP-DKY709 can degrade IKZF4 (DC50: 13 nM) and SALL4 (DC50: 2 nM). NVP-DKY709 exerts anti-tumor activity by binding with CRBN to change conformation and recruit and degrade IKZF2 .
1
1 Cited Publications
DS12881479 is a selective non-ATP-competitive MNK1 inhibitor with an IC50 value of 387 nM. DS12881479 stabilizes MNK1 in its autoinhibited DFD-out conformation, blocks eIF4E phosphorylation, suppresses tumor cell proliferation and induces weak apoptosis. DS12881479 also inhibits FLT3 and DYRK1a kinase activity at high concentrations. DS12881479 can be used for the research of cancer, such as leukemia .
1
1 Cited Publications
FzM1 is a negative allosteric modulator (NAM) of Frizzled receptor FZD4. FzM1 reduces WNT5A-dependent WNT responsive element (WRE) activity (log EC50inh=?6.2). FzM1 binds to an allosteric binding site located in intracellular loop 3 (ICL3) of FZD4 and alters the conformation of the receptor, ultimately inhibiting the WNT/β-catenin cascade .
1
1 Cited Publications
Target:
Research Areas:
TH-257 is a potent inhibitor of LIMK1 and LIMK2 with IC50 values of 84 nM and 39 nM for LIMK1 and LIMK2, respectively, and it can be used as a chemical probe for LIMK1 and LIMK2. TH-257 is an allosteric inhibitor targeting a binding pocket induced by an αC and DFG-out conformation. TH257 is exquisitely selective and no significant activity against the wider kinome has been observed in the KINOMEscan assay at 1 μM .
1
1 Cited Publications
Target:
Research Areas:
APOL1-IN-1 is a natural product antibiotic and selective FabF inhibitor discovered in Streptomyces platensis. Platensimycin exhibits IC50 values of 48 nM and 160 nM against Staphylococcus aureus and Escherichia coli FabF, respectively. Platensimycin preferentially recognizes the acyl-enzyme conformation of FabF, occupies the malonyl-binding subsite, and competes with malonyl-ACP, thereby inhibiting bacterial fatty acid elongation. Platensimycin is useful for research on bacterial fatty acid biosynthesis and Gram-positive bacterial infections .
1
1 Cited Publications
Target:
Research Areas:
Complement C5-IN-1 is a Complement C5 inhibitor with an IC50 of less than 0.005 μM in serum inhibition assays. Complement C5-IN-1 stabilizes the α-helical conformation, thereby burying the cleavage site and preventing cleavage of C5 by C5 convertase. Complement C5-IN-1 inhibits membrane attack complex deposition in human serum and whole blood complement activation assays. Complement C5-IN-1 can be used in research related to complement-mediated diseases, such as paroxysmal nocturnal hemoglobinuria .
1
1 Cited Publications
Synonyms: ANSA; 8-Anilino-1-naphthalenesulfonic acid
1
1 Cited Publications
PIN1 inhibitor API-1 is a specific Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) inhibitor (API-1) with an IC50 of 72.3 nM. PIN1 inhibitor API-1 directly and specifically binds to the Pin1 peptidyl-prolyl isomerase (PPIase) domain and potently inhibits Pin1 cis-trans isomerizing activity. PIN1 inhibitor API-1 retains the active conformation of pXPO5 and restores the ability of pXPO5 to transport pre-miRNAs from nucleus to cytoplasm, thus up-regulating the anticancer miRNA biogenesis to suppress both in vitro and in vivo hepatocellular carcinoma development .
1
1 Cited Publications
Cat. No.: HY-160406
CAS No.: 2332803-84-4
Target:
Research Areas:
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 .
1
1 Cited Publications
Synonyms: 8-Bromoadenosine 5'-monophosphate; 8-Bromoadenylic acid
Research Areas:
8-Bromo-AMP (8-Bromoadenosine 5'-monophosphate) is an AMP analog. 8-Bromo-AMP inhibits ADP-dependent glucokinase (ADPGK). 8-Bromo-AMP competitively inhibits ADPGK by binding to the nucleotide-binding site, inducing conformational changes, and acting on catalytic residues. 8-Bromo-AMP non-competitively inhibits rat adenylate kinase isozymes AK-M, AK II, and AK III. 8-Bromo-AMP inhibits T cell activation-induced ROS production and ROS-dependent IL-2 and IκB expression. 8-Bromo-AMP is used in research on cancer and myocardial ischemia-reperfusion injury .
1
1 Cited Publications
Cat. No.: HY-W017113
CAS No.: 149-30-4
Cat. No.: HY-P99415
CAS No.: 2098724-83-3
Synonyms: MAA868
Target:
Research Areas:
Category:
Human Gut Microbiota Metabolites Natural Products Other Diseases Endogenous metabolite Disease Research Fields
Target:
Synonyms: PK4C9
Target:
Research Areas:
Homocarbonyltopsentin (PK4C9) is a small-molecule TSL2-binding compound, binds to pentaloop conformations of TSL2 and promotes a shift to triloop conformations that display enhanced SMN2 exon 7 (E7) splicing with EC50 value of 16 μM .
Cat. No.: HY-W019033
CAS No.: 4016-63-1
Target:
Research Areas:
8-Bromoguanosine is a purine nucleoside, a brominated derivative of guanosine. 8-Bromoguanosine can reduce the conformational heterogeneity of RNA to enhance its function .
Cat. No.: HY-P10856
CAS No.: 3085809-95-3
Target:
Research Areas:
Cat. No.: HY-18343A
CAS No.: 1217195-61-3
CP-31398 dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53 .
-
-
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
