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Results for "

E3 ligase VHL

" in MedChemExpress (MCE) Product Catalog:

By Targets:	E1/E2/E3 Enzyme (6) E3 Ligase Ligand-Linker Conjugates (140) Ligands for E3 Ligase (29) Akt (2) Anaplastic lymphoma kinase (ALK) (1) Androgen Receptor (3) Apoptosis (19) Autophagy (2) Bcl-2 Family (2) Bcr-Abl (1) BMI1 (1) Btk (1) c-Myc (2) Casein Kinase (1) Caspase (1) CCR (1) CDK (1) CXCR (1) Cyclophilin (2) Cytochrome P450 (1) Deubiquitinase (1) DNA/RNA Synthesis (2) Drug Isomer (2) EGFR (1) Epigenetic Reader Domain (6) ERK (2) FAK (1) Fat Mass and Obesity-associated Protein (FTO) (1) FKBP (1) FLT3 (2) GLP Receptor (1) Glycosidase (1) HBV (1) HCV (2) HDAC (7) HIF/HIF Prolyl-Hydroxylase (4) Histone Methyltransferase (14) HIV (2) HSP (1) IFNAR (1) IKK (1) IRAK (1) Ligands for Target Protein for PROTAC (7) MDM-2/p53 (1) MEK (2) Mixed Lineage Kinase (2) Molecular Glues (5) Nuclear Hormone Receptor 4A/NR4A (1) p38 MAPK (2) PARP (2) PERK (1) Phosphatase (1) PI3K (1) Pim (3) PINK1/Parkin (2) PROTAC Linkers (1) PROTAC-Linker Conjugates for PAC (1) PROTACs (81) Raf (1) Ras (5) Reactive Oxygen Species (ROS) (2) Reference Standards (12) RIP kinase (2) ROS Kinase (1) SGK (1) SOS1 (2) STAT (5) STING (1) SWI/SNF Complex (3) Target Protein Ligand-Linker Conjugates (10) Tyrosinase (1) WDR5 (2) YAP (1) YTHDF (1) α-synuclein (1)
By Research Areas:	Cancer (252) Cardiovascular Disease (2) Infection (5) Inflammation/Immunology (12) Neurological Disease (1)
Click Chemistry:	PROTAC Synthesis (1) Azide (10) Alkynes (1)

276

Inhibitors & Agonists

Screening Libraries

Peptides

Click Chemistry

Targets Recommended: Ligands for E3 Ligase E3 Ligase Ligand-Linker Conjugates E1/E2/E3 Enzyme ByeTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-130604

DT2216 2 Publications Verification	Bcl-2 Family PROTACs Apoptosis	Cancer
DT2216 is a potent and selective BCL-XL (Bcl-2 family member) degrader based on PROTAC technology. DT2216 causes effective degradation of BCL-XL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. DT2216 is composed of the Bcl-2 family protein inhibitor Navitoclax-piperazine (HY-44432), a linker, and a VHL E3 ubiquitin ligase (Pink: Navitoclax-piperazine; Blue: VHL ligand; Black: linker) .

HY-112078

(S,R,S)-AHPC-Me VHL ligand 2; E3 ligase Ligand 1A	Ligands for E3 Ligase	Cancer
(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 .

HY-103602

(S,R,S)-AHPC-PEG3-NH2 hydrochloride VH032-PEG3-NH2 hydrochloride; VHL Ligand-Linker Conjugates 1 hydrochloride; E3 ligase Ligand-Linker Conjugates 5	E3 Ligase Ligand-Linker Conjugates	Cancer
(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.

HY-42424

(S,R,S)-AHPC-Me hydrochloride VHL ligand 2 hydrochloride; E3 ligase Ligand 1	Ligands for E3 Ligase	Cancer
(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 .

HY-125905

VH032-cyclopropane-F 1 Publications Verification VHL ligand 3; E3 ligase Ligand 19	Ligands for E3 Ligase	Cancer
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 .

HY-103604

(S,R,S)-AHPC-PEG4-NH2 hydrochloride 2 Publications Verification VH032-PEG4-NH2 hydrochloride; VHL Ligand-Linker Conjugates 4 hydrochloride; E3 ligase Ligand-Linker Conjugates 7	E3 Ligase Ligand-Linker Conjugates	Cancer
(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.

HY-103603

(S,R,S)-AHPC-PEG2-NH2 hydrochloride VH032-PEG2-NH2 hydrochloride; VHL Ligand-Linker Conjugates 3 hydrochloride; E3 ligase Ligand-Linker Conjugates 6	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG2-NH2 hydrochloride (VH032-PEG2-NH2 hydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs .

HY-44432

Navitoclax-piperazine ABT-263-piperazine	Ligands for Target Protein for PROTAC Bcl-2 Family	Cancer
Navitoclax-piperazine (ABT-263-piperazine) is a Navitoclax (HY-10087) analog and BCL-XL inhibitor. Navitoclax-piperazine is the ligand for target protein of PROTAC DT2216 (HY-130604). Navitodax-pperaie and E3 ubiquitin ligase VHL ligand can be used to synthesize PROTAC DT2216 (HY-130604) .

HY-136262

CRBN-6-5-5-VHL 1 Publications Verification	PROTACs E1/E2/E3 Enzyme	Cancer
CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based cereblon (CRBN) degrader with a DC₅₀ value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3. (Pink: VHL ligand (HY-125845); Blue: E3 Ligase ligand (HY-10984); Black: linker (HY-403544)) .

HY-103601

(S,R,S)-AHPC-PEG4-N3 1 Publications Verification VH032-PEG4-N3; VHL Ligand-Linker Conjugates 5; E3 ligase Ligand-Linker Conjugates 4	E3 Ligase Ligand-Linker Conjugates	Others
(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.

HY-160525

NVS-VHL720	Molecular Glues	Cancer
NVS-VHL720 is a selective VHL-based cysteine dioxygenase (CDO1) molecular glue degrader. NVS-VHL720 recruits CDO1 to the VHL E3 ligase complex, driving ubiquitin-dependent proteasomal degradation of CDO1. NVS-VHL720 can be used for the research of cancer .

HY-173011

RJS308	PROTACs Cyclophilin HIV HCV	Infection
RJS308 is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 induces ubiquitin-dependent CypA degradation by recruiting the VHL E3 ligase complex, and forms a ternary complex with CypA and VHL/elongin C/elongin B. RJS308 exhibits anti-HIV-1 and anti-HCV activities. RJS308 can be used in studies related to viral infections .

HY-130845A

AR antagonist 1 hydrochloride	Ligands for E3 Ligase Ligands for Target Protein for PROTAC Androgen Receptor	Cancer
AR antagonist 1 (compound 29) hydrochloride is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020) .

HY-103598

(S,R,S)-AHPC-PEG3-N3 VH032-PEG3-N3; VHL Ligand-Linker Conjugates 8; E3 ligase Ligand-Linker Conjugates 12	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG3-N3 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. (S,R,S)-AHPC-PEG3-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.

HY-103600

(S,R,S)-AHPC-PEG1-N3 VH032-PEG1-N3; VHL Ligand-Linker Conjugates 9; E3 ligase Ligand-Linker Conjugates 3	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG1-N3 (VH032-PEG1-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG1-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.

HY-158684

YX-02-030	PROTACs MDM-2/p53 Apoptosis	Cancer
YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a K_d 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 .

HY-168016

PROTAC YAP degrader-1	PROTACs YAP	Cancer
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 .

HY-160924

MS147	PROTACs BMI1 E1/E2/E3 Enzyme Histone Methyltransferase	Cancer
MS147 is a VHL-based PROTAC degrader of BMI1 and RING1B (polycomb repressive complex 1 core components). MS147 directly binds EED and VHL E3 ligase, recruiting the ligase to the EED-BMI1/RING1B complex to induce time-dependent, ubiquitination-mediated degradation of BMI1 and RING1B. MS147 reduces histone H₂A Lys119 mono-ubiquitination without altering histone H₃ Lys27 tri-methylation and inhibits cancer cells proliferation. MS147 can be used for the research of cancer, such as chronic myelogenous leukemia and b-cell lymphoma . (Pink: BMI1/RING1B ligand (HY-183634); Blue: VHL ligand (HY-125845); Black: linker)

HY-103604A

(S,R,S)-AHPC-PEG4-NH2 2 Publications Verification VH032-PEG4-NH2; VHL Ligand-Linker Conjugates 4 ; E3 ligase Ligand-Linker Conjugates 7 Free Base	E3 Ligase Ligand-Linker Conjugates	Cancer
(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.

HY-128756

SIAIS178	PROTACs Bcr-Abl	Cancer
SIAIS178 is a potent and selective BCR-ABL degrader based on PROTAC technology with an IC₅₀ of 24 nM. SIAIS178 causes effective degradation of BCR-ABL protein by recruiting Von Hippel-Lindau (VHL) E3 ubiquitin ligase. SIAIS178 has anticancer activity .

HY-42419

(S,R,S)-AHPC-Me-NHBoc	Ligands for E3 Ligase	Cancer
(S,R,S)-AHPC-Me-NHBoc is an E3 ubiquitin ligase *VHL* ligand used to recruit the VHL protein. (S,R,S)-AHPC-Me-NHBoc can be linked to a target protein ligand via a linker to form a PROTAC.

HY-159779

NR-V04	PROTACs Nuclear Hormone Receptor 4A/NR4A	Inflammation/Immunology Cancer
NR-V04 is a selective NR4A1 PROTAC degrader. NR-V04 forms a ternary complex with NR4A1 and the VHL E3 ligase, mediates proteasome-dependent degradation of NR4A1. NR-V04 induces tumor-infiltrating B cells and effector memory CD8 ⁺ T cells and reduces monocytic myeloid-derived suppressor cells in tumor microenvironments. NR-V04 can be used for the research of melanoma and colon cancer .

HY-130271

(S,R,S)-AHPC-PEG5-COOH VH032-PEG5-COOH; VHL Ligand-Linker Conjugates 16; E3 ligase Ligand-Linker Conjugates 58	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG5-COOH (VH032-PEG5-COOH) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 5-unit PEG linker used in PROTAC technology .

HY-103603A

(S,R,S)-AHPC-PEG2-NH2 VH032-PEG2-NH2 ; VHL Ligand-Linker Conjugates 3 ; E3 ligase Ligand-Linker Conjugates 6 Free Base	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG2-NH2 (VH032-PEG2-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 2-unit PEG linker used in the synthesis of PROTACs .

HY-103599

(S,R,S)-AHPC-PEG2-N3 1 Publications Verification VH032-PEG2-N3; VHL Ligand-Linker Conjugates 6; E3 ligase Ligand-Linker Conjugates 13	E3 Ligase Ligand-Linker Conjugates	Cancer
(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** .

HY-42424A

(S,R,S)-AHPC-Me dihydrochloride VHL ligand 2 dihydrochloride; E3 ligase Ligand 1 dihydrochloride	Ligands for E3 Ligase	Cancer
(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 .

HY-170859

AH078	PROTACs Casein Kinase	Cancer
AH078 is a PROTAC-based CK1δ/ε degrader (DC₅₀=0.55 μM, D_max=70%) that lacks subtype selectivity between CK1δ and CK1ε. AH078 induces target protein degradation either by recruiting the CUL4-CRBN E3 *ligase* complex and proteasome, or via the *VHL- and ubiquitin-dependent pathway. AH078 also exhibits selectivity for CK1α*, and is widely applicable to research related to colon cancer, pancreatic cancer, breast cancer, ovarian cancer, chronic lymphocytic leukemia, acute myeloid leukemia, glioma, and metastatic breast adenocarcinoma .

HY-175358

PROTAC USP7 Degrader-1	PROTACs Deubiquitinase	Cancer
PROTAC USP7 Degrader-1 is a *VHL*-recruiting PROTAC and USP7 degrader with binding activity to both USP7 and the *VHL* E3 ubiquitin ligase. PROTAC USP7 Degrader-1 recruits the *VHL* E3 ligase to mediate the ubiquitination and subsequent proteolytic degradation of USP7 .

HY-130991

K-Ras ligand-Linker Conjugate 6	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 6 incorporates a ligand for K-Ras recruiting moiety, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 6 can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523), which is potent PROTAC K-Ras degrader that exhibits ≥70% degradation efficacy in SW1573 cells .

HY-176366

AHPC-PEG6-CH2COOH	E3 Ligase Ligand-Linker Conjugates	Cancer
AHPC-PEG6-CH2COOH is an *E3 ligase* ligand-linker conjugate** that incorporates a VHL ligand and 6-unit PEG linker (HY-122702). AHPC-PEG6-CH2COOH can be used for synthesis of PROTAC CMP98 (HY-136257) .

HY-125906

VHL Ligand-Linker Conjugates 15 E3 ligase Ligand-Linker Conjugates 56	E3 Ligase Ligand-Linker Conjugates	Cancer
VHL Ligand-Linker Conjugates 15 incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 15 can be used to design PROTACs .

HY-141797

MS33	Histone Methyltransferase PROTACs WDR5	Cancer
MS33 is a potent WDR5 degrader, with K_ds of 870 nM and 120 nM for VCB and WDR5, respectively. MS33 induces WDR5 degradation in an E3 ligase VHL, and proteasome-dependent manner. MS33 can be used for the research of acute myeloid leukemia .

HY-133046

VHL Ligand-Linker Conjugates 17	E3 Ligase Ligand-Linker Conjugates	Cancer
VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader . VHL Ligand-Linker Conjugates 17 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-114176

(S,R,S)-AHPC-C4-NH2 hydrochloride VH032-C4-NH2 hydrochloride; VHL Ligand-Linker Conjugates 13; E3 ligase Ligand-Linker Conjugates 28	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C4-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and a linker used for EED-Targeted PROTAC .

HY-120217A

(S,S,S)-VH032	Ligands for E3 Ligase	Cancer
(S,S,S)-VH032 is the ligand for E3 Ligase (VHL) that can be used for synthesis of PROTAC SGK3 degrader-2 (HY-176823) .

HY-103602A

(S,R,S)-AHPC-PEG3-NH2 VH032-PEG3-NH2; VHL Ligand-Linker Conjugates 1; E3 ligase Ligand-Linker Conjugates 5 Free Base	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG3-NH2 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.

HY-130845

AR antagonist 1	Ligands for E3 Ligase Ligands for Target Protein for PROTAC	Cancer
AR antagonist 1 (compound 29) is a potent androgen receptor (AR) antagonist and binds to E3 ligase ligands with weak binding affinities to VHL protein in the synthesis of PROTAC ARD-266 (HY-133020).

HY-164977

JCS-1	PROTACs Phosphatase	Cancer
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 (Pink: DcpS ligand (HY-102020); Blue: E3 ligase VHL ligand (HY-151227); Black: linker (HY-141230)) .

HY-173422

MS2133	PROTACs Histone Methyltransferase	Cancer
MS2133 is a DOT1L PROTAC degrader. MS2133 promotes ubiquitination and degradation of DOT1L in THP-1 and MV4-11 cells (DC₅₀: 56 nM and 25 nM, respectively), and reduces H3K79 methylation. MS2133 inhibits the growth of MLL-r leukemia cells and has anticancer activity. (Pink: DOT1L ligand (HY-173423); Blue: E3 ligase VHL ligand (HY-47070); Black: Linker (HY-79577); E3 ligase VHL ligand-linker conjugate (HY-173424)) .

HY-103602B

(S,R,S)-AHPC-PEG3-NH2 dihydrochloride VH032-PEG3-NH2 dihydrochloride; VHL Ligand-Linker Conjugates 1 dihydrochloride; E3 ligase Ligand-Linker Conjugates 5 dihydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG3-NH2 dihydrochloride (VH032-PEG3-NH2 dihydrochloride) 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

HY-111824

VH032-thiol-C6-NH2 VHL Ligand-Linker Conjugates 14; E3 ligase Ligand-Linker Conjugates 29	E3 Ligase Ligand-Linker Conjugates	Cancer
VH032-thiol-C6-NH2 (VHL Ligand-Linker Conjugates 14) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology.

HY-P11493

ALAPYIP	Ligands for E3 Ligase	Cancer
ALAPYIP is a ligand for E3 ligase. ALAPYIP recruits the VHL-E3 ubiquitin ligase. ALAPYIP can be used for the synthesis of FPP29 (HY-P11228) .

HY-176917

*E3 ligase* Ligand 76**	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 76 is a E3 ligase ligand that can be used in the recruitment of VHL protein. E3 ligase Ligand 76 can be connected to the KRAS ligand (HY-162960) by a linker to synthesis of PROTAC KRAS(on) degrader ACBI-4 (HY-176792) .

HY-125846

(S,R,S)-AHPC-PEG1-OTs VH032-PEG1-OTs; VHL Ligand-Linker Conjugates 2; E3 ligase Ligand-Linker Conjugates 51	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG1-OTs is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology.

HY-176492

*E3 Ligase* Ligand-linker Conjugate 193**	E3 Ligase Ligand-Linker Conjugates	Cancer
E3 Ligase Ligand-linker Conjugate 193 is an *E3 ligase* ligand-linker conjugate** that incorporates the VHL Ligase Ligand (HY-170353) and linker (HY-176491). E3 Ligase Ligand-linker Conjugate 193 can be used for synthesis of PROTAC pan-KRAS degrader-1 (HY-176489) .

HY-W998339

(R,S,R)-AHPC-NHBoc	Ligands for E3 Ligase	Cancer
(R,S,R)-AHPC-NHBoc is an E3 ubiquitin ligase *VHL* ligand used to recruit the VHL protein. (R,S,R)-AHPC-NHBoc can be linked to a target protein ligand via a linker to form a PROTAC.

HY-49514

VHL Ligand intermediate-1	Ligands for E3 Ligase SOS1	Cancer
VHL Ligand intermediate-1 (intermediate 18a) is an intermediate in the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs .

HY-49515

VHL Ligand intermediate-2	Ligands for E3 Ligase SOS1	Cancer
VHL Ligand intermediate-2 (compound 18c) is an intermediate for the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs .

HY-170390

AB3067	PROTACs Epigenetic Reader Domain	Cancer
AB3067 is a PROTAC degrader for BET protein, that recruits two different E3 ligase Cereblon and VHL with good affinity (IC₅₀=559 nM for *VHL* in live HEK293; IC₅₀=190 nM for CRBN in live HEK293), and degrades BRD2, BRD3, BRD4 and CRBN with DC₅₀ of 2.1~2.3, 1.6, 15 and 75 nM, respectively. AB3067 inhibits the proliferation of RKO cell with an EC₅₀ of 111 nM . (Pink: ligand for target protein (HY-131633A); Black: linker (HY-170391); Blue: ligand for E3 ligase VHL (HY-112078) and CRBN(HY-W998346))

HY-174875

(S,R,S)-AHPC-CO-C2-phenylboronic acid	E3 Ligase Ligand-Linker Conjugates	Others
(S,R,S)-AHPC-CO-C2-phenylboronic acid is an *E3 ligase* ligand-linker conjugate** that incorporates the VH032-based VHL ligand (HY-125845) and linker. (S,R,S)-AHPC-CO-C2-phenylboronic acid can be used for synthesis of PROTAC AF151 (HY-174873) .

Cat. No.	Product Name

HY-L128

E3 Ligase Ligand Library

174 compounds

Proteolysis-targeting chimera (PROTAC) has been developed to be a useful technology for targeted protein degradation. PROTACs consist of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand (mostly small-molecule inhibitor) for protein of interest（target binder）. Upon binding to the target protein, the PROTACs can recruit E3 for target protein ubiquitination, which is subjected to proteasome-mediated degradation.

Although there are more than 600 E3 ubiquitin ligases, only several with small molecule ligands have been used for designing PROTACs, including Skp1-Cullin-F box complex containing Hrt1 (SCF), Von Hippel-Lindau tumor suppressor (VHL), Cereblon (CRBN), inhibitor of apoptosis proteins (IAPs), and mouse double minute 2 homolog (MDM2).

MCE carefully prepared a unique collection of 174 ligands for E3 ligase, which have been reported to be used in PROTAC design. MCE E3 ligase ligand library is a useful tool for PROTAC development.

Cat. No.	Product Name	Target	Research Area

HY-P11228

FPP29	PROTACs Apoptosis DNA/RNA Synthesis	Cancer
FPP29 is a potent peptide-based FOXM1 PROTAC degrader. FPP29 induces ubiquitination and degradation of FOXM1. FPP29 inhibits FOXM1 via the ubiquitin-proteasome degradation pathway. FPP29 induces Apoptosis. FPP29 suppresses tumor growth in hepatocellular carcinoma xenograft models. FPP29 can be used in the research of hepatocellular carcinoma (cell-penetrating peptide: (HY-P0133); VHL ligase ligand: (HY-P11493); linker: (HY-W013664); FOXM1 ligand: (HY-P11494)) .

HY-P11493

ALAPYIP	Ligands for E3 Ligase	Cancer
ALAPYIP is a ligand for E3 ligase. ALAPYIP recruits the VHL-E3 ubiquitin ligase. ALAPYIP can be used for the synthesis of FPP29 (HY-P11228) .

Cat. No.	Product Name		Classification

HY-103601

(S,R,S)-AHPC-PEG4-N3 1 Publications Verification VH032-PEG4-N3; VHL Ligand-Linker Conjugates 5; E3 ligase Ligand-Linker Conjugates 4		Azide
(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.

HY-103598

(S,R,S)-AHPC-PEG3-N3 VH032-PEG3-N3; VHL Ligand-Linker Conjugates 8; E3 ligase Ligand-Linker Conjugates 12		Azide
(S,R,S)-AHPC-PEG3-N3 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. (S,R,S)-AHPC-PEG3-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.

HY-103600

(S,R,S)-AHPC-PEG1-N3 VH032-PEG1-N3; VHL Ligand-Linker Conjugates 9; E3 ligase Ligand-Linker Conjugates 3		Azide
(S,R,S)-AHPC-PEG1-N3 (VH032-PEG1-N3) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based VHL ligand and 1-unit PEG linker used in PROTAC technology. (S,R,S)-AHPC-PEG1-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.

HY-114402

ARD-69		PROTAC Synthesis
ARD-69 is a PROTAC degrader based on the E3 ubiquitin ligase VHL and targeting the androgen receptor, which can induce androgen receptor (AR) protein degradation in AR-positive prostate cancer cells. ARD-69 inhibits AR-regulated gene expression, binds to the AR ligand binding domain at one end and binds to VHL at the other end, prompting AR to be recruited to the E3 ubiquitin ligase complex, triggering proteasome degradation, thereby inhibiting AR signaling pathways and downstream gene expression (such as PSA, TMPRSS2). ARD-69 can be used to study of castration-resistant prostate cancer (mCRPC) . ARD-69 is composed of a target protein ligand (pink part) AR antagonist 14 (HY-172624), a PROTAC linker (black part) tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and a VHL-type E3 ubiquitinase ligand (blue part) VH 101, acid (HY-47070); among them, the VHL ligand and the linker can form a conjugate VH 101-amide-piperidine-Pip-alkyne (HY-172625).

HY-103599

(S,R,S)-AHPC-PEG2-N3 1 Publications Verification VH032-PEG2-N3; VHL Ligand-Linker Conjugates 6; E3 ligase Ligand-Linker Conjugates 13		Azide
(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** .

HY-128767

VH032-PEG3-acetylene		Alkynes
VH032-PEG3-acetylene is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology . VH032-PEG3-acetylene is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

HY-163167

VH 032 amide-alkylC5-azide		Azide
VH 032 amide-alkylC5-amine is a functionalized von-Hippel-Lindau protein ligand (VHL) for PROTAC research and development; incorporates an E3 ligase ligand plus an alkyl linker with terminal amine ready for conjugation to a target protein ligand .

HY-159147

SIAIS039		Azide
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC₅₀s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .

HY-130654

(S,R,S)-AHPC-C2-PEG4-N3 VH032-C2-PEG4-N3		Azide
(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-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-C2-PEG4-N3 can be used in the synthesis of vRucaparib-TP4 (HY-130647). vRucaparib-TP4 a highly potent PARP1 degrader with a half-maximal degrading concentration (DC₅₀) of 82 nM . (S,R,S)-AHPC-C2-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.

HY-139341

Pomalidomide 4'-alkylC3-azide		Azide
Pomalidomide 4'-alkylC3-azide (compound 2a) is an E3 ligase ligand-linker conjugate containing a Pomalidomide (HY-10984) based cereblon (CRBN) ligand and a linker. Pomalidomide 4'-alkylC3-azide can be used in the synthesis of PROTAC .

HY-139343

Pomalidomide 4'-alkylC2-azide		Azide
Pomalidomide 4'-alkylC2-azide (compound 2a) is an E3 ligase ligand-linker conjugate containing a Pomalidomide (HY-10984) based cereblon (CRBN) ligand and a linker. Pomalidomide 4'-alkylC2-azide can be used in the synthesis of PROTAC .

HY-181356

(S,R,S,R)-AHPC-Me-CO-C7-N3		Azide
(S,R,S,R)-AHPC-Me-CO-C7-N3 is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S,R)-AHPC-Me based VHL ligand and a linker used in PROTAC technology. (S,R,S,R)-AHPC-Me-CO-C7-N3 can be connected to the ligand for protein by a linker to form PROTAC EZH2 Degrader-28 (HY-181355) .

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