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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
3417 Results for "
mSWI/SNF complex
" in MedChemExpress (MCE) Product Catalog:
Products (3417)
3417 Results for "mSWI/SNF complex" in MCE Product Catalog:
YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a Kd of 35 nM. YX-02-030 recruits the VHL E3 ligase to form a ternary complex, leading to ubiquitination and proteasome-mediated degradation of MDM2. YX-02-030 inhibits MDM2-p53 and VHL-HIF1α binding with IC50 values of 63 and 1350 nM. YX-02-030 activates TAp73, upregulates p53 family target genes and induces apoptosis. YX-02-030 demonstrates on-target efficacy in TNBC xenograft-bearing mice, extending survival without normal cell toxicity .
Cat. No.: HY-163709
PROTAC FAK degrader 2 is an orally active PROTAC FAK degrader with a DC50 of 60.10 nM. PROTAC FAK degrader 2 forms a ternary complex with FAK and CRBN E3 ubiquitin ligase, driving proteasome-mediated degradation of total and phosphorylated FAK. PROTAC FAK degrader 2 inhibits phosphorylation of AKT and ERK, suppressing their downstream signaling pathways. PROTAC FAK degrader 2 reduces cancer cell viability, adhesion, migration, and invasion. PROTAC FAK degrader 2 exerts anti-tumor activity in HCT8/T tumor xenografts in mice. PROTAC FAK degrader 2 can be used for the research of breast cancer, colorectal cancer, lung cancer .
Cat. No.: HY-168016
CAS No.: 3058483-58-9
PROTAC YAP degrader-1 is a VHL-recruiting PROTAC degrader (DC50=8.2 μM) and antiproliferative agent that targets YAP. PROTAC YAP degrader-1 recruits the E3 ligase VHL and binds to VHL to form a ternary complex containing YAP. PROTAC YAP degrader-1 inhibits the nuclear localization of YAP in cancer cells, reduces YAP/TEAD-mediated transcription, and induces TAZ protein degradation. PROTAC YAP degrader-1 reduces the oncogenic activity of YAP and exerts antiproliferative effects in the Huh7 xenograft mouse model. PROTAC YAP degrader-1 can be used for the research of hepatocellular carcinoma and mesothelioma .
Cat. No.: HY-168892
CAS No.: 380636-64-6
LC3B recruiter 2 (34R) is an LC3B recruiter and a component of the autophagy-lysosome pathway degradation system (ATTEC, Autophagy-Tethering Compounds), which directly binds to LC3B. LC3B recruiter 2 binds to CDK9 inhibitor SNS-032 (HY-10008) through a linker, forming an ATTEC that targets the degradation of the CDK9 and Cyclin T1 complex (with inhibitory effects on both). Therefore, LC3B recruiter 2 exerts activity through the LC3B-dependent autophagy-lysosome pathway, interfering with the cell cycle of cancer cells, thus exhibiting antitumor activity .
Cat. No.: HY-169072
CAS No.: 3103327-20-1
Research Areas:
PROTAC MLKL Degrader-2 is an orally active and highly selective mixed lineage kinase domain-like pseudokinase (MLKL) PROTAC degrader with a DC50 of 0.012 μM. PROTAC MLKL Degrader-2 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, leading to ubiquitination of MLKL and its degradation via a proteasome-dependent pathway. PROTAC MLKL Degrader-2 inhibits necroptosis, reduces ROS production, restores mitochondrial function, and ameliorates lysosomal dysfunction induced by necroptotic stimuli. PROTAC MLKL Degrader-2 degrades MLKL in xenograft mouse models. PROTAC MLKL Degrader-2 can be used in cancer-related research .
Cat. No.: HY-169135
Target:
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PROTAC 20S proteasome subunit β5 degrader 2 is a PROTAC degrader targeting the 20S proteasome subunit β5, with a DC50 of 0.16 μM. PROTAC 20S proteasome subunit β5 degrader 2 forms a ternary complex with the CRBN E3 ligase, induces ubiquitination of the 20S proteasome subunit β5, and promotes its degradation via the proteasome. PROTAC 20S proteasome subunit β5 degrader 2 exerts antiproliferative effects in cancer cells and exhibits antitumor activity both in vitro and in vivo. It can be used for the research of pharyngeal cancer and drug-resistant multiple myeloma .
Cat. No.: HY-170952
CAS No.: 3053857-55-6
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LYG-409 is a highly potent, selective, and orally active GSPT1 molecular glue degrader. LYG-409 induces GSPT1 degradation in KG-1 cells with a DC50 of 7.87 nM. LYG-409 binds to Cereblon with an IC50 of 191 nM, promotes the formation of the CRBN-GSPT1 ternary complex, and induces proteasome-dependent degradation of GSPT1. LYG-409 exhibits broad antiproliferative and GSPT1-degrading activities in a variety of hematologic and solid tumor cells. LYG-409 can be used for studies related to GSPT1-targeted protein degradation, acute myeloid leukemia, and prostate cancer .
Cat. No.: HY-173364
CAS No.: 3114073-95-6
Synonyms: BAK-04-212
EB-TCIP (BAK-04-212) is a proof-of-concept tool specifically designed for Ewing sarcoma research, serving as an EWSR1::FLI1 binder tagged with BCL6 and FKBP12 F36V. EB-TCIP forms a ternary complex with the tagged fusion protein, specifically recruits EWSR1::FLI1 to BCL6-bound DNA loci, and induces rapid chromatin remodeling and relocalization. By mediating relocalization, EB-TCIP remodels the transcriptional machinery and activates the expression of BCL6 target genes that are originally repressed. EB-TCIP is used in studies related to novel epigenetic therapies for Ewing sarcoma .
Cat. No.: HY-175252
PROTAC EGFR degrader 14 is a EGFR PROTAC degrader, with a DC50 of 2.9 nM against EGFR L858R/T790M/C797S. PROTAC EGFR degrader 14 forms a stable ternary complex by bridging the ATP-binding pocket of the target protein EGFR with VHL E3 ubiquitin ligase, induces efficient and specific degradation of EGFR mutants via the ubiquitin-proteasome system, and ultimately induces cell cycle arrest and apoptosis. PROTAC EGFR degrader 14 can be used in studies related to non-small cell lung cancer carrying the EGFR C797S drug-resistant mutation .
Cat. No.: HY-175321
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PROTAC c-Met degrader-6 is an orally active c-Met PROTAC degrader with DC50 values of 0.52 nM (EBC-1) and 0.45 nM (Hs746T), respectively. PROTAC c-Met degrader-6 induces potent targeted degradation of c-Met via the ubiquitin-proteasome system by bridging the target protein c-Met and the Cullin-CRBN E3 ubiquitin ligase to form a ternary complex, thereby inducing tumor cell cycle arrest and apoptosis. PROTAC c-Met degrader-6 can be used in the research of various MET-driven cancers (such as gastric cancer, liver cancer, non-small cell lung cancer, etc.) .
Cat. No.: HY-181075
Research Areas:
Antibacterial agent 318 is an antibacterial agent that binds to bacterial DNA, blocks its replication, and forms supramolecular complexes. Antibacterial agent 318 acts as an oxidative stress inducer, elevating intracellular reactive oxygen species (ROS) levels, oxidizing glutathione (GSH) to glutathione disulfide (GSSG), depleting cellular GSH reserves, and inducing bacterial cell death through oxidative damage. Antibacterial agent 318 disrupts the bacterial cell membrane and reduces bacterial metabolic activity. Antibacterial agent 318 exhibits rapid bactericidal activity, inhibits bacterial biofilm formation, and displays minimal cytotoxicity toward non-cancerous mammalian cells. Antibacterial agent 318 is applicable in research on drug-resistant bacterial infections .
Cat. No.: HY-181762
Research Areas:
Multitarget AD-IN-6 (Compound 39) is a multi-target inhibitor, with an IC50 of 15.54 μM against PDE4B, 15.15 μM against PDE7A, 8.39 μM against PDE3A, and a Kd of 37.7 μM against CHIT1. Multitarget AD-IN-6 acts as a TRPA1 antagonist, reduces the level of the NLRP3 inflammasome multiprotein complex to inhibit its activation, while inhibiting PDE4B, PDE7A and CHIT1, and decreasing the phosphorylation of NF-κB. Multitarget AD-IN-6 improves the pathology of elastase-induced emphysema in mice. Multitarget AD-IN-6 is applicable for the research of chronic obstructive pulmonary disease .
Cat. No.: HY-182331
CAS No.: 3059574-58-9
WCF-598 is a RXRγ (Kd: 234.2 nM) PROTAC degrader. WCF-598 induces RXRγ degradation via the ubiquitin-proteasome pathway and binds directly to RXRγ. WCF-598 indirectly induces AR-V7 degradation, impairs the stability of the RXRγ-AR-V7 complex, downregulates AR-V7 levels, and inhibits the transcription of downstream target genes of AR-V7. WCF-598 induces tumor cell apoptosis, inhibits cell proliferation, activates the p53 signaling pathway, and suppresses cell cycle progression. WCF-598 can be used for the research of prostate cancer .
Cat. No.: HY-183105
CAS No.: 2133291-32-2
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DC551040 is an orally active and selective lysine demethylase 1 (LSD1) inhibitor with a human IC50 of 2.14 nM. DC551040 binds to LSD1 via π-π stacking with Trp552, polar interactions with Phe538, and covalent adduct formation with FAD, and disrupts the LSD1-GFI1B-CoREST complex. DC551040 induces H3K4me2 accumulation, apoptosis, and cell differentiation, activates STAT5, NF-κB, AKT, and IL6-STAT3 pathways, and upregulates IL6 expression. DC551040 can be used for the research of acute myeloid leukemia .
Cat. No.: HY-187102
CAS No.: 19866-38-7
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Research Areas:
2-Hydrazinyl-3-methylbutanoic acid is a diamine oxidase (DAO) inhibitor. 2-Hydrazinyl-3-methylbutanoic acid acts as a non-competitive inhibitor of diamine oxidase (with histamine as the substrate), achieving an inhibition rate of up to 76%. This inhibition can be prevented by pre-incubation with 2-Ketoglutaric acid (HY-W013636) to form a non-inhibitory complex. 2-Hydrazinyl-3-methylbutanoic acid also inhibits glutamate decarboxylase and 5-hydroxytryptophan decarboxylase, and exhibits moderate inhibitory activity against monoamine oxidase. 2-Hydrazinyl-3-methylbutanoic acid can be used in studies related to amino acid metabolic enzymes .
Cat. No.: HY-189151
CAS No.: 3057302-21-0
PROTAC HDAC8 Degrader-5 is a selective HDAC8 PROTAC degrader that mediates ubiquitination and proteasomal degradation through the formation of a ternary complex. PROTAC HDAC8 Degrader-5 degrades HDAC8 with a DC50 of 1.8 nM in MDA-MB-231 cells and a DC50 of 4.7 nM in Jurkat cells. PROTAC HDAC8 Degrader-5 inhibits cancer cell migration and proliferation, induces apoptosis through caspase 3/7 activation, and increases acetylated SMC3 and α-tubulin. PROTAC HDAC8 Degrader-5 is useful for cancer-related research, such as leukemia, triple-negative breast cancer, etc. .
Cat. No.: HY-D3125
Target:
Research Areas:
NtHzBtd is a fluorescent probe for detecting Fe 3+. NtHzBtd is applicable to the selective fluorescent detection of Fe 3+ ions and live cell imaging studies. NtHzBtd can selectively coordinate with Fe 3+ to form a 1:1 complex, triggering chelation enhanced quenching (CHEQ) and intramolecular charge transfer (ICT) processes, which result in fluorescence turn-off, thereby enabling sensitive detection of Fe 3+ and live cell fluorescence imaging. After binding to Fe 3+, NtHzBtd reduces fluorescence intensity, exhibits a rapid response property, with a limit of detection of 0.036 μM and a response time of approximately 55 s. The detection wavelengths are Ex/Em = 334/401 nm (solution system) .
Cat. No.: HY-DY2024
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0.5% Evans Blue Staining Solution is an azo dye solution that strongly binds to serum albumin to form a high-molecular-weight tracer complex. 0.5% Evans Blue Staining Solution can passively leak with albumin and produce color when the blood-brain barrier or vascular barrier is damaged in vivo, and it is used for permeability assessment. 0.5% Evans Blue Staining Solution is excluded by living cells but enters dead cells to stain them in vitro due to the loss of membrane integrity in dead cells. 0.5% Evans Blue Staining Solution can be used for studies related to the identification of dead/necrotic cells and blood-brain barrier (BBB) permeability .
Cat. No.: HY-P990610
Cat. No.: HY-P992382
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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
