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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
23 Results for "
VHL-IN-1
" in MedChemExpress (MCE) Product Catalog:
Products (23)
23 Results for "VHL-IN-1" in MCE Product Catalog:
Research Areas:
VHL-IN-1 (Compound 30) is an E3 ligase VHL inhibitor with a Kd value of 37 nM. VHL-IN-1 blocks VHL-mediated ubiquitination and degradation of HIF-1α. VHL-IN-1 stabilizes the protein levels of HIF-1α and hydroxylated HIF-1α, and induces the transcriptional activity of HIF-1α. VHL-IN-1 can be used for PROTAC development. VHL-IN-1 is applicable for cancer research [1].
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10 Publications Verification
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VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kd[1] .
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3 Cited Publications
Synonyms: VH032-NH2 monohydrochloride; VHL ligand 1 monohydrochloride
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(S,R,S)-AHPC (VH032-NH2; VHL ligand 1) hydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein .
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2 Cited Publications
Synonyms: (S,S,S)-VH032-NH2 hydrochloride
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(S,S,S)-AHPC ((S,S,S)-VH032-NH2) hydrochloride is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC (Compound 27) is a ligand used as a negative control for (S,R,S)-AHPC (HY-125845). (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein .
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1 Cited Publications
Cat. No.: HY-171658
CAS No.: 3070346-91-4
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R1-ICR-5 is a highly selective RIPK1 PROTAC degrader. Mediated by VHL, R1-ICR-5 induces the degradation of RIPK1, which in turn dysregulates the TNFR1 and TLR3/4 signaling hubs, enhances the signaling outputs of NF-κB, MAPK and IFN, and simultaneously promotes RIPK3 activation and necroptosis (necroptosis). R1-ICR-5 can be used in the research of triple-negative breast cancer and skin inflammation [1].
Synonyms: VHL ligand 2; E3 ligase Ligand 1A
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(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 .
Cat. No.: HY-42424
CAS No.: 1948273-03-7
Synonyms: VHL ligand 2 hydrochloride; E3 ligase Ligand 1
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(S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) 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 hydrochloride 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 .
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 [1].
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SHP2-D26 isomer-1 (Compound 26) is an isomer of SHP2-D26 (HY-145162). SHP2-D26 is the first highly potent SHP2 PROTAC degrader. The induction of SHP2 degradation by SHP2-D26 requires binding to VHL-1 and SHP2 proteins, and is dependent on ubiquitin-like modification and the proteasome. SHP2-D26 can be used in the research of esophageal cancer and acute myeloid leukemia [1].
Cat. No.: HY-170824
CAS No.: 3033586-31-8
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SMD-3236 is a SMARCA2 PROTAC degrader with a DC50 of 0.5 nM, a Dmax of 98%, and an IC50 of 42.2 nM against human SMARCA2. SMD-3236 induces proteasome- and ubiquitin-like modification-dependent degradation of SMARCA2 protein by binding to SMARCA2 and VHL-1. SMD-3236 inhibits the growth of SMARCA4-deficient cancer cells. SMD-3236 induces significant and persistent depletion of SMARCA2 in tumor tissues. SMD-3236 suppresses tumor growth in SMARCA4-deficient human cancer xenograft models. SMD-3236 can be used in research related to SMARCA4-deficient cancers such as melanoma, non-small cell lung cancer, and acute myeloid leukemia [1].
Synonyms: VH032-C5-COOH
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(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases [1].
Cat. No.: HY-42424A
CAS No.: 2504950-56-3
Synonyms: VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride
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(S,R,S)-AHPC-Me dihydrochloride (VHL ligand 2 dihydrochloride) 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 dihydrochloride 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 .
Cat. No.: HY-157512
CAS No.: 2413035-43-3
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SJF-0661 is a variant of the von Hippel-Lindau (VHL) protein ligand with no targeted degradation ability and can be used as a control reagent for the VHL ubiquitin ligase ligand. SJF-0661 is a variant obtained by inverting the stereocenter of the key hydroxyproline group in the VHL ligand .
Cat. No.: HY-164977
CAS No.: 3093519-24-2
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JCS-1 is a potent DcpS PROTAC degrader. JCS-1 non-covalently binds DcpS with a RG3039-based warhead and recruits the E3
ligase VHL. JCS-1 promotes ubiquitination and degradation of DcpS at nanomolar concentrations (DC50 in MOLM-14 cells: 87 nM). JCS-1 can be used for the research of AML and other DcpS-dependent genetic disorders [1].
Cat. No.: HY-158685
CAS No.: 2360561-90-4
RG7112D is a potent MDM2 inhibitor with IC50s of 11 nM and >10000 nM and for MDM2-p53 and VHL-HIF1α by binding HTRF assay, respectively. RG7112D is coupled by an amide bond to VHL-Amine, resulting in a bi-functional molecule, YX-02-030. YX-02-03, a MDM2-PROTAC, potently inhibits MDM2-p53 binding (HTRF IC50=63nM). RG7112D can stabilize MDM2 protein and increase p53 protein levels [1].
Cat. No.: HY-170859A
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AH081 is a CK1δ/ε PROTAC degrader. AH081 serves as the negative control of AH078 (HY-170859). AH081 exhibits inhibitory activity but no degradative activity against CK1δ/ε by using an inactive stereoisomer of the VHL ligand .
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(R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669) [1].
Cat. No.: HY-P5908
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Cat. No.: HY-125845B
CAS No.: 1797406-78-0
Synonyms: (S,S,S)-VH032-NH2
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(S,S,S)-AHPC ((S,S,S)-VH032-NH2) is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC (Compound 27) is a ligand used as a negative control for (S,R,S)-AHPC (HY-125845). (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein .
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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
