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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
216 Results for "
protein-protein interaction inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (216)
216 Results for "protein-protein interaction inhibitors" in MCE Product Catalog:
34
34 Publications Verification
Cat. No.: HY-19991
CAS No.: 1675201-83-8
Synonyms: PD-1/PD-L1 inhibitor 1
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BMS-1 is an inhibitor of the PD-1/PD-L1 protein/protein interaction (IC50 between 6 and 100 nM) .
34
34 Publications Verification
K-975 is a potent, selective and orally active TEAD inhibitor, with a strong inhibitory effect against protein-protein interactions between YAP1/TAZ and TEAD. K-975 covalently binds to Cys359 located in the palmitate-binding pocket of TEAD via an acrylamide structure. K-975 exhibits antitumor activity on malignant pleural mesothelioma .
23
23 Cited Publications
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KI696 is a selective KEAP1/NRF2 protein-protein interaction inhibitor with a human Kd value of 1.3 nM. KI696 acts by competitively occupying the NRF2-binding pocket of the KEAP1 Kelch domain. KI696 blocks KEAP1-mediated ubiquitination and degradation of NRF2, promotes the translocation of NRF2 to the nucleus, activates the expression of downstream antioxidant genes, increases intracellular glutathione levels, and alleviates oxidative stress-induced cell damage and inflammatory cell infiltration in the lungs. KI696 reduces ozone-induced pulmonary oxidative damage and inflammatory cell accumulation in rats, and upregulates pulmonary antioxidant genes. KI696 can be used in research related to chronic obstructive pulmonary disease, oxidative stress and inflammation .
22
Lenacapavir (GS-6207) is an HIV-1 capsid inhibitor. Lenacapavir binds to the interface between capsid hexamers and CA monomers, disrupts capsid assembly and viral maturation, inhibits nuclear translocation of HIV-1 DNA, interferes with CA-mediated protein-protein interactions, reduces the formation of 2-LTR circles and pre-integration proviruses, induces aberrant capsids, and decreases the production of mature HIV-1. Lenacapavir exhibits activity against a variety of HIV-1 subtypes and clinical isolates. Lenacapavir is applicable to research related to human immunodeficiency virus type 1 (HIV-1) infection .
22
Lenacapavir (GS-6207) sodium is an HIV-1 capsid inhibitor. Lenacapavir sodium binds to the interface between capsid hexamers and CA monomers, disrupts capsid assembly and viral maturation, inhibits nuclear translocation of HIV-1 DNA, interferes with CA-mediated protein-protein interactions, reduces the formation of 2-LTR circles and pre-integration proviruses, induces aberrant capsids, and decreases the production of mature HIV-1. Lenacapavir sodium exhibits activity against a variety of HIV-1 subtypes and clinical isolates. Lenacapavir sodium is applicable to research related to human immunodeficiency virus type 1 (HIV-1) infection .
19
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Bazedoxifene acetate (TSE-424 acetate) is an oral, nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene acetate can be used for the research of osteoporosis. Bazedoxifene acetate also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
19
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Bazedoxifene (TSE-424) is an oral, BBB-penetrant nonsteroidal selective estrogen receptor modulator (SERM), with IC50s of 23 nM and 99 nM for ERα and ERβ, respectively. Bazedoxifene can be used for the research of osteoporosis. Bazedoxifene also acts as an inhibitor of IL-6/GP130 protein-protein interactions and can be used for the research of pancreatic cancer .
12
Limantrafin (CB-103) is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. Limantrafin has anti-tumor activity .
12
12 Cited Publications
TED-347 is a potent, irreversible, covalent and allosteric inhibitor at YAP-TEAD protein-protein interaction with an EC50 of 5.9 μM for TEAD4⋅Yap1 protein-protein interaction. TED-347 specifically and covalently bonds with Cys-367 within the central pocket of TEAD4 with a Ki of 10.3 μM. TED-347 blocks TEAD transcriptional activity and has antitumor activity .
6
6 Cited Publications
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A2ti-1 is a selective and high-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 24 μM . A2ti-1 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-1 prevents human papillomavirus type 16 (HPV16) infection .
5
5 Cited Publications
Cat. No.: HY-19541
CAS No.: 1640282-31-0
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I-CBP112, a chemical probe, is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.
4
4 Cited Publications
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A-395, a chemical probe, is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM .
4
4 Cited Publications
Synonyms: CX05168; CX04328
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LEDGIN6 (CX05168) is a quinoline-based protein-protein interaction inhibitor of LEDGF/p75 and HIV integrase .
4
4 Cited Publications
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BRD5529 is an effective dose-dependent CARD9-TRIM62 protein–protein interaction (PPI) inhibitor with an IC50 value of 8.6 μM. BRD5529 has potency and complete inhibition of CARD9 ubiquitinylation in vitro, also has favorable solubility. BRD5529 can be used for the research of inflammatory bowel disease (IBD) such as Crohn’s disease (CD) and ulcerative colitis (UC) .
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3 Cited Publications
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IPR-803 is a potent inhibitor of the uPAR·uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity .
3
3 Cited Publications
RAS inhibitor Abd-7, a potent RAS-binding compound (Kd=51 nM), is a RAS-effector protein-protein interaction (PPI) inhibitor. RAS inhibitor Abd-7 interacts with RAS inside the cells, prevents RAS-effector interactions and inhibits endogenous RAS-dependent signaling. RAS inhibitor Abd-7 impairs the PPI of various mutant KRAS proteins with PI3K, CRAF and RALGDS as well as NRAS Q61H and HRAS G12V .
3
3 Cited Publications
BRCA1-IN-2 (compound 15) is a cell-permeable protein-protein interaction (PPI) inhibitor for BRCA1 with an IC50 of 0.31 μM and a Kd of 0.3 μM, which shows antitumor activities via the disruption of BRCA1 (BRCT)2/protein interactions .
3
3 Cited Publications
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DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 μM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 μM and 4.5 μM, respectively .
3
3 Cited Publications
Cat. No.: HY-162289
CAS No.: 3036029-78-1
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FAZ-3780 is an inhibitor that binds to the NTF2L domain of G3BP1/2. FAZ-3780 binds to the NTF2L nsP3 of G3BP1 with high affinity, with a Kd of 0.15 μM and a Pep-FRET IC50 of 0.7 μM. FAZ-3780 targets the protein-protein interaction domain of G3BP1/2, and specifically inhibits the co-condensation of G3BP1, caprin 1 and RNA in vitro. FAZ-3780 inhibits stress granule formation and disassembles pre-formed stress granules. FAZ-3780 can be used in studies related to cancer and neurodegenerative diseases .
2
2 Cited Publications
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MRTX0902 is a potent, selective, brain-penetrant, and orally active SOS1 inhibitor with a Ki of 1.9 nM. MRTX0902 disrupts the SOS1:KRASG12C protein-protein interaction (PPI). MRTX0902 can be used in research on pancreatic ductal adenocarcinoma .
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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
