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
247 Results for "
VHL E3-ligase
" in MedChemExpress (MCE) Product Catalog:
Products (247)
247 Results for "VHL E3-ligase" in MCE Product Catalog:
20
20 Publications Verification
Research Areas:
CC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer .
18
18 Cited Publications
Research Areas:
VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM. VH-298 leads to HIF-α accumulation inside HeLa cells. VH-298 is an E3 ligase Ligand, and can be used for synthesis of PROTACs .
4
4 Cited Publications
Gefitinib-based PROTAC 3 is a PROTAC degrader targeting EGFR, with a DC50 of 11.7 nM against exon 19 deletion mutants and a DC50 of 22.3 nM against EGFR L858R. Gefitinib-based PROTAC 3 selectively induces the ubiquitin-proteasome degradation of exon 19 deletion-mutant and L858R-mutant EGFR by recruiting the VHL E3 ligase. Gefitinib-based PROTAC 3 can be used for the research of EGFR mutation-positive cancers .
2
2 Cited Publications
Synonyms: VH032-PEG4-NH2 hydrochloride; VHL Ligand-Linker Conjugates 4 hydrochloride; E3 ligase Ligand-Linker Conjugates 7
Research Areas:
(S,R,S)-AHPC-PEG4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
2
2 Cited Publications
Synonyms: VH032-PEG4-N3; VHL Ligand-Linker Conjugates 5; E3 ligase Ligand-Linker Conjugates 4
Research Areas:
(S,R,S)-AHPC-PEG4-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG4-N3 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
2
2 Cited Publications
Synonyms: VH032-PEG4-NH2; VHL Ligand-Linker Conjugates 4 ; E3 ligase Ligand-Linker Conjugates 7 Free Base
Research Areas:
(S,R,S)-AHPC-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 4-unit PEG linker used in PROTAC technology.
2
2 Cited Publications
Research Areas:
PD0325901-O-C2-dioxolane has main portion of MEK inhibitor PD0325901. PD0325901-O-C2-dioxolane and a ligand of VHL or CRBN E3 ligase can be used in the synthesis of MEK1/2 degrader .
2
2 Cited Publications
Cat. No.: HY-132857
CAS No.: 2711006-66-3
Target:
Research Areas:
ZXH-4-130 is a potent and selective Cereblon (CRBN) degrader. ZXH-4-130 recruits the VHL E3 ligase to specifically target CRBN as a substrate for selective degradation as a hetero-PROTAC molecule. ZXH-4-130 can be applied in studies on the biological functions of CRBN and related research of frontotemporal dementia .
2
2 Cited Publications
GSK215 is a potent and selective PROTAC focal adhesion kinase (FAK) degrader with a pDC50 of 8.4. GSK215 is designed by a binder for the VHL E3 ligase and the FAK inhibitor VS-4718. GSK215 induces rapid and prolonged FAK degradation, giving a long-lasting effect on FAK levels and a marked pharmacokinetic/pharmacodynamics (PK/PD) disconnect .
2
2 Cited Publications
Target:
Research Areas:
ZXH-4-130 TFA is a potent and selective Cereblon (CRBN) degrader. ZXH-4-130 TFA recruits the VHL E3 ligase to specifically target CRBN as a substrate for selective degradation as a hetero-PROTAC molecule. ZXH-4-130 TFA can be applied in studies on the biological functions of CRBN and related research of frontotemporal dementia .
2
2 Cited Publications
LC-2 is an orally active PROTAC-class degrader targeting KRAS G12C and a MAPK inhibitor. LC-2 shows higher selectivity for KRAS G12C than wild-type KRAS and other KRAS mutants. LC-2 covalently binds to KRAS G12C via the MRTX849 (HY-130149) warhead, recruits the VHL E3 ligase to form a ternary complex, and induces ubiquitination and degradation of KRAS G12C. Meanwhile, LC-2 inhibits the MAPK signaling pathway, reduces the phosphorylation levels of CRAF and AKT, thereby inducing apoptosis and suppressing cancer cell and tumor growth. LC-2 can be used for the research of KRAS G12C-positive cancers, including non-small cell lung cancer and colorectal cancer .
1
1 Cited Publications
Synonyms: VHL ligand 3; E3 ligase Ligand 19
Target:
Research Areas:
VH032-cyclopropane-F is the VH032-based VHL ligand. VH032-cyclopropane-F can be connected to the ligand for protein (e.g., SMARCA BD ligand) by a linker to form PROTACs (e.g., PROTAC 1). PROTAC 1 is a partial degrader of SMARCA2 and SMARCA4 .
1
1 Cited Publications
Target:
Research Areas:
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 .
1
1 Cited Publications
Synonyms: VH032-PEG2-N3; VHL Ligand-Linker Conjugates 6; E3 ligase Ligand-Linker Conjugates 13
Research Areas:
(S,R,S)-AHPC-PEG2-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker. (S,R,S)-AHPC-PEG2-N3 can be used for the synthesis of PROTACs .
1
1 Cited Publications
Synonyms: VH032-PEG2-C4-Cl; VHL Ligand-Linker Conjugates 7; E3 ligase Ligand-Linker Conjugates 10
Research Areas:
(S,R,S)-AHPC-PEG2-C4-Cl (VH032-PEG2-C4-Cl) is a conjugate of ligands for E3 and 13-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-PEG2-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-PEG2-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
1
1 Cited Publications
Cat. No.: HY-145816A
Research Areas:
JPS016 TFA is a class I histone deacetylase (HDAC) PROTAC inhibitor. JPS016 TFA recruits the VHL E3 ligase (Ligands for E3 Ligase) to mediate the ubiquitination and proteasomal degradation of HDAC1, HDAC2 and HDAC3. JPS016 TFA reduces the viability of colon cancer cells and induces Apoptosis. JPS016 TFA activates the PINK1/Parkin mitochondrial Autophagy pathway, enhances cardiomyocyte viability, alleviates mitochondrial damage, and reduces mitochondrial ROS production in cells. JPS016 TFA is applicable to research related to colon cancer and sepsis cardiomyopathy .
1
1 Cited Publications
PROTAC FKBP Degrader-3 is a selective FKBP PROTAC degrader with an IC50 of 1.8 nM. PROTAC FKBP Degrader-3 targets and degrades the FKBP protein by recruiting the VHL E3 ligase, and this degradation process is primarily mediated by K11 and K48 ubiquitin chain linkages. PROTAC FKBP Degrader-3 can be applied in cancer research .
1
1 Cited Publications
Synonyms: VH032-C6-PEG3-C4-Cl; VHL Ligand-Linker Conjugates 12; E3 ligase Ligand-Linker Conjugates 8
Research Areas:
(S,R,S)-AHPC-C6-PEG3-C4-Cl (VH032-C6-PEG3-C4-Cl) is a conjugate of ligands for E3 and 20-atom-length linker. The connector of linker is Halogen group. (S,R,S)-AHPC-C6-PEG3-C4-Cl incorporates the (S,R,S)-AHPC based VHL ligand and an alkyl/ether-based linker. (S,R,S)-AHPC-C6-PEG3-C4-Cl is capable of inducing the degradation of GFP-HaloTag7 in cell-based assays .
Synonyms: VHL ligand 2; E3 ligase Ligand 1A
Target:
Research Areas:
(S,R,S)-AHPC-Me (VHL ligand 2) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein . (S,R,S)-AHPC-Me can be used to synthesize ARV-771, a von Hippel-Landau (VHL) E3 ligase-based BET PROTAC degrader. ARV-771 potently degrades BET protein in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM .
Synonyms: VH032-PEG3-NH2 hydrochloride; VHL Ligand-Linker Conjugates 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 5
Research Areas:
(S,R,S)-AHPC-PEG3-NH2 (VH032-PEG3-NH2) hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
-
-
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
