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Results for "

VHL E3 ubiquitin ligase

" in MedChemExpress (MCE) Product Catalog:

By Targets:	E1/E2/E3 Enzyme (2) E3 Ligase Ligand-Linker Conjugates (16) Ligands for E3 Ligase (11) Androgen Receptor (1) Apoptosis (7) Bcl-2 Family (2) Bcr-Abl (1) Btk (1) c-Myc (1) Casein Kinase (1) Caspase (1) CDK (1) CXCR (1) Cyclophilin (2) Deubiquitinase (1) DNA/RNA Synthesis (1) Drug Isomer (1) Epigenetic Reader Domain (2) Fat Mass and Obesity-associated Protein (FTO) (1) HCV (2) Histone Methyltransferase (7) HIV (2) IFNAR (1) IKK (1) Ligands for Target Protein for PROTAC (3) Mixed Lineage Kinase (2) Molecular Glues (4) p38 MAPK (1) PARP (1) Pim (1) PROTAC Linkers (1) PROTACs (29) Ras (2) RIP kinase (1) ROS Kinase (1) SOS1 (2) STAT (3) STING (1) SWI/SNF Complex (1) YTHDF (1)
By Research Areas:	Cancer (56) Cardiovascular Disease (1) Infection (3) Inflammation/Immunology (3)
Click Chemistry:	PROTAC Synthesis (1) Azide (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Click Chemistry

Targets Recommended: E1/E2/E3 Enzyme Ligands for E3 Ligase E3 Ligase Ligand-Linker Conjugates 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-156730

KT-333	Molecular Glues STAT	Cancer
KT-333 is a molecular glues that degrades STAT3 protein. KT-333 mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .

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-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-162250

MS8847	PROTACs Histone Methyltransferase	Cancer
MS8847 is a PROTAC degrader and antiproliferative agent targeting EZH2 (DC₅₀=34.4 nM in EOL-1 MLL-rAML cells). MS8847 recruits the E3 ligase von Hippel-Lindau (VHL) to mediate the degradation of EZH2 via the ubiquitin-proteasome system. MS8847 induces antiproliferative effects in MLL-rearranged acute myeloid leukemia cells and inhibits the growth of triple-negative breast cancer cell lines or 3D triple-negative breast cancer models. MS8847 is applicable to research related to MLL-rearranged acute myeloid leukemia and triple-negative breast cancer .

HY-139218

(S,R,S)-AHPC-Me-C6-NH2	E3 Ligase Ligand-Linker Conjugates	Others
(S,R,S)-AHPC-Me-C6-NH2 is a VHL E3 ubiquitin ligase ligand-linker conjugate structurally modified based on VHL ligand 2 (HY-112078). (S,R,S)-AHPC-Me-C6-NH2 can be used for the synthesis of PROTACs .

HY-114402

ARD-69	PROTACs Androgen Receptor	Cancer
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-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-130815A

MAK683-C2-acid hydrochloride	Ligands for Target Protein for PROTAC Histone Methyltransferase	Cancer
MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 (HY-130614) and PROTAC EED degrader-2 (HY-130615) .

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-123961

SJF-8240	PROTACs p38 MAPK	Cancer
SJF-8240 is a selective p38α PROTAC degrader. SJF-8240 promotes ubiquitination and selective degradation of p38α. SJF-8240 can be used in breast cancer-related research .

HY-148671

(S,R,S)-AHPC-amido-C7-acid	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-amido-C7-acid incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design PROTACs .

HY-128845

PROTAC CRBN Degrader-1	PROTACs E1/E2/E3 Enzyme	Cancer
PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other . (Blue: VHL ligand (S,R,S)-AHPC (HY-125845); Pink: CRBN ligand Pomalidomide-C2-NH2 (HY-128846); Black: Linker (HY-128847))

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-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-173011A

RJS308 TFA	PROTACs Cyclophilin HIV HCV	Infection
RJS308 TFA is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 TFA 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 TFA exhibits anti-HIV-1 and anti-HCV activities. RJS308 TFA can be used in studies related to viral infections .

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-177119

ZBP1 Covalent PROTAC-1	PROTACs RIP kinase Mixed Lineage Kinase	Infection Inflammation/Immunology
ZBP1 Covalent PROTAC-1 is a covalent Z-DNA binding protein 1 ZBP1 PROTAC degrader, with its DC₅₀ being 25.69 nM. ZBP1 Covalent PROTAC-1 integrates the ligand that recruits the VHL E3 ubiquitin ligase and the DNA aptamer (Aptamer Z3) with the specific Zα domain that can bind to ZBP1, which has a high affinity (K_D = 2.71 nM) with ZBP1. After degrading ZBP1, the phosphorylation levels of downstream signaling molecules RIPK3 and MLKL significantly decrease. ZBP1 Covalent PROTAC-1, encapsulated by nano-liposomes, significantly improves the survival rate of mice infected with influenza A virus (IAV) after administration via the trachea .

HY-122702

PEG6-(CH2CO2H)2	PROTAC Linkers	Others
PEG6-(CH2CO2H)2 is a symmetric PEG PROTAC linker, for the synthesis of Homo-PROTACs which is bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation .

HY-159147

SIAIS039	PROTACs ROS Kinase Apoptosis	Cancer
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-151227

VL285 Phenol	Ligands for E3 Ligase	Cancer
VL285 Phenol is a phenol-based VL285 analog. VL285 is an E3 ubiquitin ligase VHL ligand and can be used in the synthesis of HaloPROTAC3, degrading HaloTag7 fusion protein (IC₅₀=0.34 μM).

HY-175025

CH091138	PROTACs Ras Apoptosis	Cancer
CH091138 is a potent and selective KRASG12D PROTAC degrader with DC₅₀s of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. CH091138 selectively degrades exogenous and endogenous KRASG12D but not KRAS ^WT or other KRAS mutants (G12C/G12S/G12V), depending on the VHL-mediated ubiquitin-proteasome system. CH091138 exhibits potent anti-tumor activity and induces cancer cell apoptosis. CH091138 can be used for the studies of pancreatic cancer and colon cancer. (Pink: KRASG12D ligand (HY-175144); Blue: VHL E3 ligase ligand (HY-138678); Black: Linker; VHL E3 ligase ligand + Linker (HY-136006B)) .

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-156730A

KT-333 ammonium	Molecular Glues STAT	Cancer
KT-333 ammonium (Compound A) is a molecular glues that degrades STAT3 protein. KT-333 ammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 ammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 ammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .

HY-175885

PROTAC FTO degrader 1	PROTACs Fat Mass and Obesity-associated Protein (FTO) Apoptosis Caspase PARP YTHDF	Cancer
PROTAC FTO degrader 1 is a Fat Mass and Obesity-associated Protein (FTO) PROTAC degrader. PROTAC FTO degrader 1 selectively degrades FTO depending on VHL E3 ligase and ubiquitin-proteasome system. PROTAC FTO degrader 1 can increase m₆A modifications on mRNAs associated with ribosome biogenesis and promote their YTHDF2-mediated decay. PROTAC FTO degrader 1 can inhibit cancer cells proliferation and induce apoptosis. PROTAC FTO degrader 1 can be used for the research of cancer, such as acute myeloid leukemia (AML) . (Structure Note: Pink: FTO ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042); VHL ligand-Linker: (HY-139218))

HY-169086

KL-465	PROTACs	Cancer
KL-465 is a MAGE-A3 PROTAC degrader that degrades MAGE-A3 in HeLa cells with a DC₅₀ of 2 μM. KL-465 inhibits the proliferation of MAGE-A3-positive cancer cells. KL-465 can be used for the research of MAGE-A3-related cancers .

HY-158036

PROTAC STING Degrader-2	PROTACs STING IKK IFNAR CXCR	Inflammation/Immunology
PROTAC STING Degrader-2 is a STING PROTAC degrader with a DC₅₀ of 0.53 μM. PROTAC STING Degrader-2 reduces the phosphorylation levels of TBK1 and IRF3. PROTAC STING Degrader-2 decreases the mRNA expression levels of IFN-β, CXCL10 and TNF-α, and blocks luciferase secretion. PROTAC STING Degrader-2 can be used in the research of autoimmune diseases .

HY-136163

(S,R,S)-AHPC-C2-NH2 dihydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C2-NH2 dihydrochloride incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-OH can be used in the synthesis of a series of PROTACs .

HY-130816

(S,R,S)-AHPC-O-Ph-PEG1-NH2 VH032-O-Ph-PEG1-NH2	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-O-Ph-PEG1-NH2 (VH032-O-Ph-PEG1-NH2) is E3 ligase ligand-linker conjugate and incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-O-Ph-PEG1-NH2 is used in PROTAC EED degrader-1 (HY-130614). PROTAC EED degrader-1 is a PROTAC targeting EED with a pK_D of 9.02 .

HY-130815

MAK683-CH2CH2COOH	Histone Methyltransferase Ligands for Target Protein for PROTAC	Cancer
MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design PROTAC EED degrader-1 (HY-130614) and PROTAC EED degrader-2 (HY-130615) .

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-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-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-153425

PROTAC SMARCA2/4 degrader-41	PROTACs	Cancer
PROTAC SMARCA2/4 degrader-41 is a SMARCA2/4 PROTAC degrader with a DC₅₀ and IC₅₀ both < 0.1 μM. PROTAC SMARCA2/4 degrader-41 is applicable to research on SMARCA2/4-related or SMARCA2/4-deficient cancers .

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-136008A

(S,R,S)-AHPC-PEG1-NH2 dihydrochloride VH032-PEG1-NH2 dihydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-PEG1-NH2 (VH032-PEG1-NH2) dihydrochloride incorporates a VHL ligand for the E3 ubiquitin ligase and a PROTAC linker. (S,R,S)-AHPC-PEG1-NH2 dihydrochloride can be used to design PROTACs .

HY-168290

(S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-Me-12-((4-Bromobutyl)amino)dodecanamide can be used in the synthesis of PROTACs, such as MS934 (HY-153863). MS934 is a novel improved VHL-recruiting MEK 1/2 PROTAC degrader .

HY-153321A

(R,R)-Bexobrutideg (R,R)-NX-5948; (R,R)-BTK-IN-24	Drug Isomer PROTACs Btk	Inflammation/Immunology Cancer
(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .

HY-156730B

KT-333 diammonium	Molecular Glues STAT	Cancer
KT-333 diammonium is a molecular glues that degrades STAT3 protein. KT-333 diammonium mediates the selective degradation of STAT3 through the ubiquitin-proteasome system by binding to STAT3 protein and E3 ubiquitin ligase von Hippel-Lindau protein (VHL). KT-333 diammonium has strong selectivity for STAT3 protein degradation and good antitumor activity. KT-333 diammonium can be used in the study of hematologic malignancies such as large granular lymphocytic leukemia (LGL-L), peripheral T-cell lymphoma (PTCL), and cutaneous T-cell lymphoma (CTCL) .

HY-163219

VHL Ligand 8-PEG2-O-piperidine-Boc	E3 Ligase Ligand-Linker Conjugates	Cancer
VHL Ligand 8-PEG2-O-piperidine-Boc is a conjugate of E3 ubiquitin ligase ligand-Linker, which can be used to synthesize complete PROTACs molecules.

HY-168454

trans-VH032-Cyclopropane-F-C-cyclohexane-p-C-OTs	E3 Ligase Ligand-Linker Conjugates	Cancer
trans-VH032-Cyclopropane-F-C-cyclohexane-p-C-OTs incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 15 can be used to design PROTACs, such as dBAZ2B (HY-168453) .

HY-141651

(S,R,S)-AHPC-C3-COOH	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C3-COOH (compound 28i) is a carboxylic acid derivative of the VHL E3 ubiquitin ligase ligand-Linker conjugate. (S,R,S)-AHPC-C3-COOH can be used to synthesize PROTACs .

HY-168026

CEP1347-VHL-02	PROTACs Mixed Lineage Kinase	Cancer
CEP1347-VHL-02 is a PROTAC targeting MLK3. CEP1347-VHL-02 consists of PROTAC target protein ligand CEP-1347 (HY-10412) (red part), E3 ubiquitin ligase ligand (S,R,S)-AHPC-Me (HY-112078) (blue part) and PROTAC Linker Amino-PEG3-CH2COOH (HY-140189) (black part), of which the target protein ligand activity control is CEP-1347-acid (HY-168027), and the conjugate of E3 ubiquitin ligase ligand + Linker is (S,R,S)-AHPC-Me-CO-CH2-PEG3-NH2 (HY-131387) ^{[1] ^.}

HY-130798

(S,R,S)-AHPC-amido-C5-acid	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-amido-C5-acid incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design XY028-133 (HY-129180) .

HY-172645

(S,R,S)-AHPC-Me-amide-C-O-C5-Br	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-Me-amide-C-O-C5-Br incorporates an VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-Me-amide-C-O-C5-Br can be used to design PROTACs, such as ERD-308 (HY-128600) .

HY-181949

PROTAC BRD9 Degrader-10	PROTACs Epigenetic Reader Domain	Cancer
PROTAC BRD9 Degrader-10 is a PROTAC degrader targeting BRD9, with an IC₅₀ of 2.97 μM against BRD9. PROTAC BRD9 Degrader-10 induces BRD9 degradation via the ubiquitin-proteasome system by recruiting the VHL E3 ubiquitin ligase. PROTAC BRD9 Degrader-10 reduces the viability and inhibits the proliferation of myeloid leukemia cells. PROTAC BRD9 Degrader-10 is applicable for the research of acute myeloid leukemia .

HY-181728

MS243	PROTACs Ras	Cancer
MS243 is a potent KRAS ^G12D PROTAC degrader with a DC₅₀ of 4.2 nM. MS243 promotes the proximity between KRAS ^G12D and the VHL E3 ubiquitin ligase, drives the ubiquitination and proteasomal degradation of KRAS ^G12D, and inhibits the proliferation of cancer cells harboring KRAS ^G12D. MS243 can be used in the research of KRAS ^G12D-carrying cancers, such as colon cancer and pancreatic cancer .

HY-181787

DOT1L705	PROTACs Histone Methyltransferase	Cardiovascular Disease
DOT1L705 is a PROTAC degrader that targets DOT1L. DOT1L705 recruits the VHL E3 ubiquitin ligase to induce proteasomal degradation of DOT1L. DOT1L705 reduces the viability of leukemia cells. DOT1L705 inhibits H3K79 methylation. DOT1L705 can be used in studies related to MLL-rearranged leukemia .

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-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-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) .

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