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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
187 Results for "
E3 ligase complex
" in MedChemExpress (MCE) Product Catalog:
Products (187)
187 Results for "E3 ligase complex" in MCE Product Catalog:
26
Research Areas:
Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
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9 Cited Publications
Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis .
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6 Cited Publications
Synonyms: ARV-471; PF-07850327
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Vepdegestrant (ARV-471) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM .
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6 Cited Publications
Cat. No.: HY-145514D
CAS No.: 2451573-86-5
dTAGV-1 is a selective FKBP12 F36V PORTAC degrader. dTAGV-1 induces rapid degradation of FKBP12 F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 is applicable to functional validation studies of cancer and undegradable oncoproteins .
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6 Cited Publications
dTAGV-1 TFA is a selective FKBP12 F36V PORTAC degrader. dTAGV-1 TFA induces rapid degradation of FKBP12 F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 TFA is applicable to functional validation studies of cancer and undegradable oncoproteins .
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6 Cited Publications
dTAGV-1 hydrochloride is a selective FKBP12 F36V PORTAC degrader. dTAGV-1 hydrochloride induces rapid degradation of FKBP12 F36V-tagged oncogenic fusion proteins, triggering collapse of downstream cellular signaling pathways, reduced proliferative capacity of cancer cells, and decreased levels of target proteins. dTAGV-1 hydrochloride is applicable to functional validation studies of cancer and undegradable oncoproteins .
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3 Cited Publications
Synonyms: NX-5948; BTK-IN-24
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Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
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2 Cited Publications
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VZ185 is a BRD9 and BRD7 PROTAC degrader, with DC50 values of 1.76 nM and 4.5 nM, respectively, in RI-1 cells; and DC50 values of 4 nM and 34 nM, respectively, in HEK293 cells. VZ185 hijacks the CRL2 VHL E3 ubiquitin ligase complex to induce ubiquitination and subsequent proteasomal degradation of BRD9 and BRD7. VZ185 can be used in research related to acute myeloid eosinophilic leukemia and malignant rhabdoid tumors .
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2 Cited Publications
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BETd-246 is a BRD2/3/4 PROTAC degrader targeting the BET family. BETd-246 induces ubiquitination and proteasomal degradation of BRD2, BRD3 and BRD4 by recruiting the CUL4-RBX1-DDB1-CRBN E3 ubiquitin ligase complex; it also inhibits TRAT1 expression and depletes BET proteins. BETd-246 suppresses cancer cell proliferation and invasion, disrupts the cell cycle and induces apoptosis. BETd-246 is applicable to research related to triple-negative breast cancer and T-cell acute lymphoblastic leukemia .
1
Zelebrudomide is an orally active BTK-targeting PROTAC degrader, with DC50 values of 4.5 nM and 31 nM against wild-type BTK and BTK C481S mutant, respectively. Zelebrudomide recruits the cereblon E3 ubiquitin ligase complex to mediate the degradation of BTK. Zelebrudomide also acts as a molecular glue to bind the cereblon E3 ubiquitin ligase complex, mediating the degradation of IKZF1 and IKZF3. Zelebrudomide can be used in the research of B-cell malignancies .
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1 Cited Publications
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CRBN-6-5-5-VHL is a potent and selective VHL E3 ligand-based Cereblon (CRBN) PROTAC degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL forms a heterotrimeric complex with CRBN and VHL E3 ligase, thereby promoting CRBN ubiquitination and proteasomal degradation without inducing VHL degradation. CRBN-6-5-5-VHL protects myeloma from the toxic effects of IMiDs. CRBN-6-5-5-VHL can be used in the research of multiple myeloma .
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1 Cited Publications
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KH-4-43 is an inhibitor of E3 CRL4. KH-4-43 inhibits E3 CRL4's core ligase complex and exhibits anticancer activity. KH-4-43 has a binding Kd to E3 ROC1-CUL4A CTD or the highly related ROC1-CUL1 CTD at 83 nM or 9.4 μM, respectively .
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1 Cited Publications
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CFT8634 is an orally active BRD9 PROTAC degrader with a DC50 of 0.003 μM (HEK293T.166). CFT8634 recruits the CRBN E3 ubiquitin ligase to form a ternary complex, triggering CRBN-catalyzed BRD9 polyubiquitination and 26S proteasome-mediated degradation. CFT8634 induces sustained tumor regression and inhibits tumor growth in mouse models. CFT8634 can be used in research related to synovial sarcoma, SMARCB-1-deficient cancers, acute myeloid leukemia, malignant rhabdoid tumors, and multiple myeloma .
1
1 Cited Publications
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MN551 is a covalent modulator of SOCS2 and CISH, with selectivity for SOCS2 and CISH over SOCS4. MN551 covalently modifies Cys111 in the SH2 domain of SOCS2 and Cys144 in the EF loop of the CISH SH2 domain, while only minimally modifying Cys471 in the BG loop of the SOCS6 SH2 domain. MN551 increases the thermal stability of the recombinant SOCS2-ElonginB-ElonginC complex and competitively blocks the binding of SOCS2 to its substrate; when delivered via the prodrug MN714, it blocks the intracellular recruitment of substrates by SOCS2. MN551 can serve as a chemical probe for investigating the biological functions of SOCS2 and its CRL5 complex, and also act as an E3 ligase-binding module in proteolysis-targeting chimeras (PROTACs) .
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1 Cited Publications
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PROTAC MLKL Degrader-1 is a selective MLKL PROTAC degrader with a DC50 of 2.4 μM. PROTAC MLKL Degrader-1 blocks necroptosis without modulating the phosphorylation of RIPK1 or RIPK3, and exhibits a linear correlation between MLKL levels and necroptotic cell death .
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1 Cited Publications
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dBRD9 is a BRD9 PROTAC degrader. dBRD9 reduces the binding of the ISGF3 complex to ISG promoters, decreases the level of ISG induction downstream of IFNAR signaling, and reduces the chromatin binding of BRD4 at BRD9 co-binding sites. dBRD9 can be used in research related to acute myeloid leukemia .
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1 Cited Publications
Cat. No.: HY-117690A
CAS No.: 2341840-98-8
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dBRD9 dihydrochloride is a BRD9 PROTAC degrader. dBRD9 dihydrochloride reduces the binding of the ISGF3 complex to ISG promoters, decreases the level of ISG induction downstream of IFNAR signaling, and reduces the chromatin binding of BRD4 at BRD9 co-binding sites. dBRD9 dihydrochloride can be used in research related to acute myeloid leukemia .
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1 Cited Publications
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DEG-77 is a molecular glue targeting IKZF2 and CK1α, with DC50 values of 15.3 nM and 10 nM, respectively. DEG-77 exhibits significant anti-tumor activity, inducing increased transcriptional levels of the pro-apoptotic protein Bax and the cell cycle arrest protein p21. DEG-77 is applicable to the research of acute myeloid leukemia (AmL), diffuse large B-cell lymphoma and ovarian cancer.
Cat. No.: HY-159641
CAS No.: 3034880-93-5
Synonyms: BAY-3605349
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VVD-130037 (BAY-3605349) is a covalent molecular glue and allosteric NRF2 degrader. VVD-130037 covalently binds to KEAP1 and allosterically enhances the affinity of KEAP1-CUL3, promotes the formation of the active KEAP1-CUL3 E3 ligase complex, and thereby enhances the ubiquitination and degradation of NRF2. VVD-130037 exhibits KEAP1 target-binding activity both in in vitro systems and mouse models, and it can be used in research related to NRF2-dependent cancers, solid tumors harboring KEAP1 nonsense mutations and frameshift mutations, as well as advanced solid tumors .
Cat. No.: HY-159607
CAS No.: 2755761-78-3
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PRT3789 is a selective SMARCA2 PROTAC degrader (DC50 in HeLa cell: 0.72 nM for SMARCA2, 14 nM for SMARCA4). PRT3789 forms a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, induces polyubiquitination at SMARCA2-specific lysine residues, and drives proteasome-dependent SMARCA2 degradation. PRT3789 disrupts SWI/SNF chromatin remodeling complex integrity, induces dissociation of specific subunits, suppresses oncogenic gene expression, reduces chromatin accessibility, and upregulates antigen processing/presentation-related gene expression. PRT3789 induces synthetic lethality, inhibits proliferation and colony formation, and drives tumor growth inhibition and regression in SMARCA4-deficient contexts. PRT3789 can be used for the research of SMARCA4-mutated solid tumors, non-small cell lung cancer, endometrial cancer, colorectal cancer, bladder cancer, esophageal cancer, ovarian cancer, and gastric 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
