Search Result

Pathways Recommended:	PROTAC

Results for "

VHL PROTAC

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Ligands for Target Protein for PROTAC (17) PROTAC Linkers (3) AAK1 (1) Akt (4) Anaplastic lymphoma kinase (ALK) (1) Androgen Receptor (4) Apoptosis (27) ASK1 (2) ATP Synthase (1) Autophagy (3) Bcl-2 Family (4) Bcr-Abl (2) Btk (1) CDK (2) Cyclophilin (1) Cytochrome P450 (1) Deubiquitinase (1) DNA/RNA Synthesis (1) Drug-Linker Conjugates for ADC (1) E1/E2/E3 Enzyme (3) E3 Ligase Ligand-Linker Conjugates (118) EGFR (1) Ephrin Receptor (1) Epigenetic Reader Domain (29) ERK (2) Estrogen Receptor/ERR (2) FAK (2) Ferroptosis (1) FGFR (2) FKBP (2) FLT3 (6) GLP Receptor (1) Glutaminase (1) HBV (1) HCV (1) HDAC (8) HIF/HIF Prolyl-Hydroxylase (3) Histone Methyltransferase (10) HIV (1) IRAK (3) Isotope-Labeled Compounds (1) Itk (1) JAK (2) Ligands for E3 Ligase (33) LRRK2 (1) MAP4K (1) MDM-2/p53 (4) MEK (3) MELK (1) METTL3 (4) Mixed Lineage Kinase (1) Na+/K+ ATPase (1) NAMPT (2) NF-κB (2) P-glycoprotein (1) p38 MAPK (4) PARP (1) PERK (1) Phosphatase (1) PI3K (3) PROTACs (124) Raf (1) Ras (7) Reactive Oxygen Species (ROS) (1) Reference Standards (1) RIP kinase (2) ROR (2) ROS Kinase (1) Ser/Thr Kinase (1) SGK (1) SOS1 (2) STAT (3) STING (4) SWI/SNF Complex (1) Target Protein Ligand-Linker Conjugates (9) TNF Receptor (1) Toll-like Receptor (TLR) (1) Tyrosinase (1) ULK (1) WDR5 (1) Wee1 (1) α-synuclein (1)
By Research Areas:	Cancer (279) Infection (6) Inflammation/Immunology (11) Metabolic Disease (1) Neurological Disease (4)
Click Chemistry:	PROTAC Synthesis (2) Azide (12) Alkynes (2)

309

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Click Chemistry

Targets Recommended: PROTAC Linkers PROTAC-Linker Conjugates for PAC Ligands for Target Protein for PROTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-158345

PROTAC VHL-type degrader-1	PROTACs	Cancer
PROTAC VHL-type degrader-1 (compound 9b) is a VHL-type PROTAC degrader. PROTAC VHL-type degrader-1 induces ATM degradation synergistically enhancing the efficacy of ATR inhibitor AZD6738 .

HY-120217

VH032 5 Publications Verification	Ligands for E3 Ligase	Cancer
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 K_dPROTACs .

HY-148896

(S,R,S)-AHPC-C2-PEG3-BCN	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C2-PEG3-BCN (Compound 16b) is a VHL ligand, and can be used for synthesis of PROTACs .

HY-47070

VH 101, acid	Ligands for E3 Ligase	Others
VH 101, acid is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. VH 101, acid contains an E3 ligase ligand plus an alkyl linker with terminal amine ready for conjugation to a target protein ligand .

HY-163167

VH 032 amide-alkylC5-azide	E3 Ligase Ligand-Linker Conjugates	Others
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-172767

STAT3-D11-PROTAC-VHL	PROTACs STAT Apoptosis	Cancer
STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a *PROTAC* degrader targeting Signal Transducer and Activator of Transcription 3 (STAT3). STAT3-D11-PROTAC-VHL exhibits anti-tumor activity with IC₅₀ values of 1335 nM and 1973 nM against HeLa and MCF-7 cells, respectively. STAT3-D11-PROTAC-VHL binds to the DNA-binding domain of STAT3 and recruits the E3 ligase VHL to form a ternary complex, leading to the ubiquitination of STAT3 and subsequent degradation by the proteasome. STAT3-D11-PROTAC-VHL also inhibits tumor cell growth, induces cell cycle arrest and apoptosis, and suppresses tumor immune evasion .

HY-49514

SOS1 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

SOS1 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-44630

VH 032 amide-alkylC6-acid (S,R,S)-AHPC-CO-C6-COOH	E3 Ligase Ligand-Linker Conjugates	Cancer
VH 032 amide-alkylC6-acid ((S,R,S)-AHPC-CO-C6-COOH) is a VH032 analog that acts as a ligand for *VHL, recruiting von Hippel-Lindau (VHL) protein. VH 032 amide-alkylC6-acid can be used in the synthesis of PROTACs* .

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-162835

PROTAC SMARCA2/4-degrader-28	PROTACs Epigenetic Reader Domain	Cancer
PROTAC SMARCA2/4-degrader-28 (PROTAC 1) is a *PROTAC*-based partial degrader of SMARCA2 and SMARCA4(Bliue: CRL2 ^VHL ligand (S,R,S)-AHPC (HY-125845); Black: linker (HY-159680); Pink: a SMARCA-BD ligand (+)-JQ-1 (HY-13030)) .

HY-162553

GNE7599	Ligands for E3 Ligase	Cancer
GNE7599 is a high-affinity and orally active von Hippel-Lindau (VHL) ligand with a K_d of 540 pM. GNE7599 can be connected to the ligand for protein by a linker to form PROTACs .

HY-126456

(S,R,S)-AHPC-propargyl 2 Publications Verification VH032-propargyl; VHL ligand 7	Ligands for E3 Ligase	Cancer
(S,R,S)-AHPC-propargyl (VH032-propargyl) is a VHL ligand which is used in “click reaction” for PROTACs . (S,R,S)-AHPC-propargyl 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-136005

VH032-C7-COOH	E3 Ligase Ligand-Linker Conjugates	Others
VH032-C7-COOH is a functionalized von-Hippel-Lindau (VHL) protein ligand for PROTAC research and development. VH032-C7-COOH contains an E3 ligase ligand and an alkyl linker with a terminal amine for conjugation of target protein ligands .

HY-139334

VH 101 phenol-alkylC6-amine dihydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
VH 101 phenol-alkylC6-amine dihydrochloride is a functionalized von-Hippel-Lindau (VHL) protein-ligand that can be used for PROTAC synthesis .

HY-148406

(S,R,S)-AHPC-C10-NHBoc	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C10-NHBoc is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC (HY-125845) based VHL ligand and a linker used for BET-Targeted PROTAC .

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-129941

(S,R,S)-AHPC-C10-NH2 VH032-C10-NH2	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C10-NH2 (VH032-C10-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based *VHL* ligand and a linker used for BET-Targeted PROTAC .

HY-129941A

(S,R,S)-AHPC-C10-NH2 dihydrochloride VH032-C10-NH2 dihydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C10-NH2 dihydrochloride (VH032-C10-NH2 dihydrochloride) is a synthesized E3 ligase ligand-linker conjugate that incorporates the (S,R,S)-AHPC based *VHL* ligand and a linker used for BET-Targeted PROTAC .

HY-162362

MS8709	PROTACs GLP Receptor	Cancer
MS8709 (compound 10), a potential anticancer therapeutic, is a first-in-class G9a/GLP *PROTAC* degrader. MS8709 is based on G9a/GLP inhibitor UNC0642 and recruits the von Hippel Lindau (VHL) E3 ligase (Red: G9a/GLP inhibitor UNC0642; Blue: VHL ligand; Black: linker) .

HY-131866

(S,R,S)-CO-C2-acid VH 032 amide-alkylC2-acid	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-CO-C2-acid (VH 032 amide-alkylC2-acid) is a functionalized von-Hippel-Lindau (VHL) protein ligand that can be used in PROTAC research and development. (S,R,S)-CO-C2-acid contains an E3 ligand alkyl ligand for conjugation of target protein ligands .

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-172625

VH 101-amide-piperidine-Pip-alkyne	E3 Ligase Ligand-Linker Conjugates	Cancer
VH 101-amide-piperidine-Pip-alkyne is an E3 Ligase Ligand-Linker Conjugates that can be used to synthesize PROTAC degrader. The linker part of VH 101-amide-piperidine-Pip-alkyne is tert-Butyl 4-ethynyl-[1,4'-bipiperidine]-1'-carboxylate (HY-W442074), and the VHL-type E3 ubiquitinase ligand is VH 101, acid (HY-47070) .

HY-136055

(S,R,S)-AHPC-C5-COOH VH032-C5-COOH	E3 Ligase Ligand-Linker Conjugates HIF/HIF Prolyl-Hydroxylase	Cancer
(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 K_d of 185 nM, has the potential for the study of anemia and ischemic diseases .

HY-163209

VH 032 amide-PEG6-amine hydrochloride (S,R,S)-AHPC-PEG6-NH2 hydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
VH 032 amide-PEG6-amine hydrochloride (Step 4) is a functionalized von-Hippel-Lindau protein-ligand (VHL) for PROTAC development, consisting of an E3 ligand and a PEG6 ligand. Terminal amines can be coupled to target protein ligands .

HY-130711A

(S,R,S)-AHPC-C3-NH2 TFA VH032-C3-NH2 TFA	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C3-NH2 TFA (VH032-C3-NH2 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .

HY-130711

(S,R,S)-AHPC-C3-NH2 VH032-C3-NH2	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .

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-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-136186A

(S,R,S)-AHPC-C7-amine dihydrochloride VH032-C7-amine dihydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C7-amine dihydrochloride is the dihydrochloride form of (S,R,S)-AHPC-C7-amine (HY-136186). (S,R,S)-AHPC-C7-amine is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker. (S,R,S)-AHPC-C7-amine can be used for estrogen-related receptor α (ERRα) *PROTAC* degrader .

HY-130711C

(S,R,S)-AHPC-C3-NH2 dihydrochloride VH032-C3-NH2 dihydrochloride	E3 Ligase Ligand-Linker Conjugates	Cancer
(S,R,S)-AHPC-C3-NH2 (dihydrochloride) is the dihydrochloride form of (S,R,S)-AHPC-C3-NH2 (HY-130711). (S,R,S)-AHPC-C3-NH2 (VH032-C3-NH2) is a synthesized E3 ligase ligand-linker conjugate that incorporates the VH032 based VHL ligand and a linker used in PROTAC technology. (S,R,S)-AHPC-C3-NH2 can be used in the synthesis of a series of PROTACs, such as UNC6852 (HY-130708). UNC6852 is an EED-targeted bivalent chemical degrader .

HY-130604

DT2216 1 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-152154

Nampt degrader-2	PROTACs NAMPT	Cancer
Nampt degrader-2 is a fluorescent *PROTAC, which efficiently degrades NAMPT* with an IC₅₀ of 41.9 nM. Nampt degrader-2 binds to NAMPT and VHL to form a ternary complex and subsequently induced NAMPT degradation via ubiquitin-proteasome system (UPS). Nampt degrader-2 leads to significant reduction of NAD ⁺ and exerts potent antitumor activities .

HY-129776

K-Ras ligand-Linker Conjugate 2	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 2 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 2 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-129775

K-Ras ligand-Linker Conjugate 1	Target Protein Ligand-Linker Conjugates	Cancer
K-Ras ligand-Linker Conjugate 1 incorporates a ligand for K-Ras, and a PROTAC linker, which recruit E3 ligases (such as VHL, CRBN, MDM2, and IAP). K-Ras ligand-Linker Conjugate 1 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-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-145479

PROTAC AR-V7 degrader-1	PROTACs Androgen Receptor	Cancer
PROTAC AR-V7 degrader-1 is an orally active and selective AR-V7 PROTAC degrader with a DC₅₀ of 0.32 μM (in 22Rv1 cells). PROTAC AR-V7 degrader-1 can inhibit the proliferation of tumor cells and exhibit anti-tumor activity. PROTAC AR-V7 degrader-1 can be used for the research of cancers such as prostate cancer .(Pink: VPC-14228 (HY-117669); Black: linker (HY-W041652); Blue: VHL Ligand (HY-112078))

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 study 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-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-161367

VHL-SF2	Ligands for E3 Ligase	Cancer
VHL-SF2 is a VHL ligand, and can be used for synthesis of PROTACs

HY-155356

YN14	PROTACs Ras	Cancer
YN14 is a KRASG12C proteolysis targeting chimera (PROTAC). YN14 is highly potent and selective KRASG12C degrader and induces a stable KRASG12C: YN14: VHL ternary complex with low binding free energy (ΔG). YN14 has antiproliferative effects and significantly inhibits KRASG12C-mutant cancer cell growth. YN14 leads to tumor regression with tumor growth inhibition (TGI%) rates more than 100 % in the MIA PaCa-2 xenograft model.

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-168027

CEP-1347-acid	Ligands for Target Protein for PROTAC	Cancer
CEP-1347-acid is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). CEP-1347-acid can be used for synthesis CEP1347-VHL-02 (HY-168026) .

HY-150803

VHL Ligand 14	Ligands for E3 Ligase	Cancer
VHL Ligand 14 (Compound 11) is a VHL ligand for design of PROTAC estrogen receptor α (ERα) degraders, with a binding affinity IC₅₀ of 196 nM .

HY-111823

VH032 thiol VHL ligand 6	Ligands for E3 Ligase	Cancer
VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC .

HY-174860

ASK1 ligand 1	Ligands for Target Protein for PROTAC ASK1	Cancer
ASK1 ligand 1 is a binding ligand for ASK1 and can be used to synthesize PROTACs such as dASK1-VHL (HY-174858 ^)[1].

HY-47851

VH 101, thiol	Ligands for E3 Ligase	Cancer
VH 101, thiol (compound 20) is a VHL ligand for the synthesis of PROTACs .

HY-W584527

VH032 analogue-1	Ligands for E3 Ligase	Cancer
VH032 analogue-1 is a VH032 (HY-120217) analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH032 analogue-1 will remove the protective group under acidic conditions and be directly used for PROTAC molecular synthesis. VH032 analogue-1 is a key intermediate in the synthesis of PROTACs based on VHL ligands.

HY-W584528

VH032 analogue-2	Ligands for E3 Ligase	Cancer
VH032 analogue-2 is a VH032 (HY-120217) analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH032 analogue-2 will remove the protective group under acidic conditions, and can be directly used for the synthesis of PROTAC molecules. VH032 analogue-2 is a key intermediate for the synthesis of PROTACs based on VHL ligands.

HY-138678

(R,S,S)-VH032	Ligands for E3 Ligase	Cancer
(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) .

Cat. No.	Product Name

HY-L128

E3 Ligase Ligand Library

88 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 88 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	Chemical Structure

HY-13001S

Quizartinib-d8

Quizartinib-d₈ (AC220-d₈) is deuterium labeled Quizartinib. Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a K_d of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC₅₀s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis .

Cat. No.	Product Name		Classification

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-126456

(S,R,S)-AHPC-propargyl 2 Publications Verification VH032-propargyl; VHL ligand 7		Alkynes PROTAC Synthesis
(S,R,S)-AHPC-propargyl (VH032-propargyl) is a VHL ligand which is used in “click reaction” for PROTACs . (S,R,S)-AHPC-propargyl 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-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 the treatment 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-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-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-161132

Lenalidomide 4'-alkyl-C5-azide		Azide
Lenalidomide 4'-alkyl-C5-azide is a functionalized cerebellar ligand for PROTAC development that contains an E3 ligand and an alkyl LC5 ligand with terminal azides that can be coupled to a target protein ligand .

HY-145715

Azido-PEG2-VHL		Azide
Azido-PEG2-VHL is a multikinase degrader which can be used in the synthesis of PROTACs . Azido-PEG2-VHL 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-159457

PROTAC SMARCA2/4-degrader-6		Azide
PROTAC SMARCA2/4-degrader-6 (compound I-438) is a SMARCA2/4 degrader. PROTAC SMARCA2/4-degrader-6 has the potential for the research of cancer. (Pink: SMARCA2/4 ligand, (HY-159545); Black: linker (HY-W006635); Blue: VHL ligand (HY-112078)) .

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 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-103599

(S,R,S)-AHPC-PEG2-N3 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 used in *PROTAC* technology. (S,R,S)-AHPC-PEG2-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-103601

(S,R,S)-AHPC-PEG4-N3 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-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.

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