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Pathways Recommended:	PROTAC

Results for "

small-molecule PROTACs

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PROTAC Linkers (1) PROTACs (6) ADC Linker (1) Adrenergic Receptor (1) Androgen Receptor (2) Apoptosis (4) c-Myc (1) CaMK (1) Caspase (1) CDK (1) E1/E2/E3 Enzyme (1) Epigenetic Reader Domain (1) Ligands for E3 Ligase (2) MDM-2/p53 (1) SARS-CoV (1) Tau Protein (1) α-synuclein (1)
By Research Areas:	Cancer (11) Infection (1) Neurological Disease (2)
Click Chemistry:	PROTAC Synthesis (1) Azide (1)

Inhibitors & Agonists

Screening Libraries

Click Chemistry

Targets Recommended: Small Interfering RNA (siRNA) PROTACs ALCAM/CD166 PROTAC Linkers Ligands for Target Protein for PROTAC PROTAC-Linker Conjugates for PAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-111556

BSJ-03-123 2 Publications Verification	PROTACs CDK	Cancer
BSJ-03-123 is a PROTAC connected by ligands for Cereblon and CDK as a potent and novel CDK6-selective small-molecule degrader.

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-138669

C004019	PROTACs Tau Protein	Neurological Disease
C004019 is a small-molecule *PROTAC. C004019 simultaneously recruites tau* and E3-ligase (Vhl) and thus selectively enhances ubiquitination and proteolysis of tau proteins. C004019 can be used for Alzheimer disease (AD) research .

HY-155021

PROTAC α-synuclein degrader 5	PROTACs α-synuclein	Neurological Disease
PROTAC α-synuclein degrader 5 is a highly selective small-molecule degraders (PROTAC) of α-synuclein aggregates, with an DC₅₀ of 7.51 μM and the highest degradation rate D_max of 89%. PROTAC α-synuclein degrader 5 contains probe molecule sery308 and E3 ligase ligands. PROTAC α-synuclein degrader 5 can be used for neurological disease research .

HY-131203

PROTAC BRD4 Degrader-6	Epigenetic Reader Domain Apoptosis c-Myc Caspase	Cancer
PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4 degrader with IC₅₀ value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research .

HY-151719

Azidoacetic Acid 2-Azidoacetic acid	ADC Linker	Others
Azidoacetic Acid (2-Azidoacetic acid) (compound 92-1) is a click chemistry reagent containing an azide group. Azidoacetic Acid can be used as a small molecule tool for the synthesis of PROTAC .

HY-146324

PROTAC eEF2K degrader-1	PROTACs CaMK Apoptosis	Cancer
PROTAC eEF2K degrader-1 (Compound 11l) is an eEF2K-Targeting *PROTAC* small molecule that induces apoptosis in MDA-MB-231 cells. PROTAC eEF2K degrader-1 mediates eEF2K degradation .

HY-114312

MD-224 4 Publications Verification	PROTACs MDM-2/p53 E1/E2/E3 Enzyme	Cancer
MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 consists of ligands for Cereblon and MDM2. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC₅₀ value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent . MD-224 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-400766

BWA-522 intermediate-2	Others	Cancer
BWA-522 intermediate-2 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .

HY-401056

BWA-522 intermediate-3	Others	Cancer
BWA-522 intermediate-3 is a BWA-522 intermediate. BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7 .

HY-W877989

BWA-522 intermediate-1	Ligands for E3 Ligase	Cancer
BWA-522 intermediate-1 is an intermediate in the synthesis of PROTAC BWA-522 (HY-149433) and serves as a ligand molecule for cereblon E3 ubiquitin ligase. BWA-522 is an orally active small molecule protein-targeting chimera (PROTAC) that has significant degradation effects on AR-FL and AR-V7 .

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) .

HY-149434

PROTAC AR-NTD degrader 1	Androgen Receptor Apoptosis	Cancer
PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule protein-targeting chimera (PROTACs) targeting the Androgen Receptor AR-V7. PROTAC AR-NTD antagonist 1 antagonizes the N-terminal domain of AR (AR-NTD), degrades AR-V7 protein, and induces apoptosis in prostate cancer (PC) cells. The efficiencies of PROTAC AR-NTD antagonist 1 in degrading AR-V7 in VCaP cells were 62.2% (1 μM) and 71.1% (5 μM), respectively .

HY-147100

α1A-AR Degrader 9c	PROTACs Adrenergic Receptor	Cancer
α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC₅₀ of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC₅₀ of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research .

HY-162464

MPD2	SARS-CoV	Infection
MPD2 is a PROTAC (Proteolysis Targeting Chimera) reducer that targets SARS-CoV-2's main protease (MPro). MPD2 reduces MPro protein levels through time-dependent, CRBN (Cereblon) mediated and proteasoma-driven mechanisms. MPD2 has the potential to be an antiviral small molecule compound against a variety of SARS-CoV-2 strains, including drug-resistant strains .

HY-149433

BWA-522	Androgen Receptor Apoptosis	Cancer
BWA-522 is an orally available small molecule protein-targeting chimera (PROTACs) with significant degradation effect on AR-FL and AR-V7. BWA-522 antagonizes the N-terminal domain (AR-NTD) of the androgen receptor (Androgen Receptor) and induces apoptosis in PC cells. BWA-522 inhibits tumor growth in LNCaP xenograft model studies (60 mg/kg, po; TGI=76%). The efficiencies of BWA-522 in degrading AR-V7 and AR-FL were 77.3% (1 μM) and 72.0% (5 μM) in VCaP and LNCaP cells, respectively .

Cat. No.	Product Name

HY-L128

E3 Ligase Ligand Library	58 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 58 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.

E3 Ligase Ligand Library

58 compounds

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 58 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.

HY-L129

Target Protein Ligand Library	39 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. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance. MCE carefully prepared a unique collection of 39 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

Target Protein Ligand Library

39 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. Therefore, PROTACs execute their functions by degrading the target proteins rather than inhibiting them, which has a great superiority in overcoming resistance caused by target mutation or overexpression. To date, PROTAC technology has been applied to a variety of targets, including AR, ER, BTK, BET, and BCR-ABL to overcome resistance.

MCE carefully prepared a unique collection of 39 ligands for target proteins, which have been reported to be used in PROTAC design. MCE Target Protein Ligand Library is a useful tool for PROTAC development.

Azidoacetic Acid 2-Azidoacetic acid		PROTAC Synthesis Azide
Azidoacetic Acid (2-Azidoacetic acid) (compound 92-1) is a click chemistry reagent containing an azide group. Azidoacetic Acid can be used as a small molecule tool for the synthesis of PROTAC .

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