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Results for "

Proteolysis targeting chimera

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Ligands for Target Protein for PROTAC (2) Target Protein Ligand-Linker Conjugates (1) Androgen Receptor (1) Apoptosis (5) Bcl-2 Family (1) Btk (1) c-Met/HGFR (1) E1/E2/E3 Enzyme (1) EGFR (3) Epigenetic Reader Domain (5) FAK (1) Ferroptosis (1) FLT3 (1) Glutathione Peroxidase (1) HDAC (7) Hedgehog (1) Histone Methyltransferase (1) NAMPT (1) PARP (2) PROTACs (23) Raf (1) Ras (1)
By Research Areas:	Cancer (28) Infection (1) Metabolic Disease (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Targets Recommended: Target Protein Ligand-Linker Conjugates Ligands for Target Protein for PROTAC

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-163410

AU-24118	PROTACs Epigenetic Reader Domain	Cancer
AU-24118 is orally bioavailable proteolysis targeting chimera (PROTAC) degrader of mSWI/SNF ATPases (SMARCA2 and SMARCA4) and PBRM1 .

HY-111758

PROTAC B-Raf degrader 1 1 Publications Verification	PROTACs Raf	Cancer
PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity .

HY-156395

MN551	E1/E2/E3 Enzyme	Cancer
MN551 is a potent inhibitor of cysteine-directed electrophilic covalent that plays important roles in the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation .

HY-123961

SJF-8240	PROTACs c-Met/HGFR	Cancer
SJF-8240 (PROTAC 7) is a proteolysis targeting chimera (PROTAC) degrader. SJF-8240 induces polyubiquitination of c-Met and inhibits the proliferation of GTL16 cells (IC₅₀=66.7 nM) .

HY-139156

SK-575	PROTACs PARP	Cancer
SK-575 is a highly potent and specific proteolysis-targeting chimera (PROTAC) degrader of PARP1, with an IC₅₀ of 2.30 nM. SK-575 potently inhibits the growth of cancer cells bearing BRCA1/2 mutations .

HY-124625

BI-4464	FAK Ligands for Target Protein for PROTAC	Infection Cancer
BI-4464 is a highly selective, ATP competitive PTK2/FAK protein kinase inhibitor with an IC₅₀ value of 17 nM. BI-4464 can be used as a PTK2 ligand for constructing proteolysis targeting chimeras (PROTAC).

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-162241

SJH1-62B	PROTACs	Others
SJH1-62B is a proteolysis targeting chimera (PROTAC) that can target the androgen receptor (AR) .

HY-163019

EN884	Target Protein Ligand-Linker Conjugates Epigenetic Reader Domain	Metabolic Disease
EN884 is a BRD4 degrader via a SKP1- and proteasome-dependent manner. EN884 can be used in synthetic proteolysis targeting chimeras (PROTACs) .

HY-149328

phoBET1	PROTACs	Cancer
phoBET1 is a photocaged-PROTAC. phoBET1 can achieve BRD4 degradation and effectively suppress tumor growth .

HY-156814

HPP-9	Hedgehog	Cancer
HPP-9 is a Proteolysis-Targeting Chimeras （PROTACs） based on Hedgehog Pathway Inhibitor-1 (HPI-1), with the pIC₅₀ of 6.71, that can degrade BET bromodomains. HPP-9 has antitumor activity ^[1[.

HY-146423

PROTAC EGFR degrader 6	PROTACs EGFR Apoptosis	Cancer
PROTAC EGFR degrader 6, a PROTAC EGFR degrader, potently degrades EGFR ^Del19 in HCC827 cells with the DC₅₀ of 45.2 nM. PROTAC EGFR degrader 6 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase .

HY-146422

PROTAC EGFR degrader 5	PROTACs EGFR Apoptosis	Cancer
PROTAC EGFR degrader 5 (Compound 10), a PROTAC EGFR degrader, potently degrades EGFR ^Del19 in HCC827 cells with the DC₅₀ of 34.8 nM. PROTAC EGFR degrader 5 significantly induces the apoptosis of HCC827 cells and arrest the cells in G1 phase .

HY-155371

BT-PROTAC	PROTACs	Others
BT-PROTAC is a bioorthogonally activatable prodrug. BT-PROTAC can accurately control the activity of PROTAC .

HY-160142

UBX-382	Btk	Cancer
UBX-382 is an orally available proteolysis-targeting chimeras (PROTACs) that target BTK to inactivate B-cell receptor signaling. UBX-382 shows superior degradation activity for wild-type and mutant BTK proteins and shows anti-cancer activity in murine xenograft models of TMD-8 cells .

HY-148381

A947	Epigenetic Reader Domain PROTACs Apoptosis	Cancer
A947 is a potent and selective *SMARCA2 proteolysis-targeting* chimera molecule (PROTAC). A947 also is a potent and moderately selective SMARCA2 degrader. A947 has binding affinity to the SMARCA2 bromodomain with a K_d** value of 93 nM. A947 can be used for the research of cancer .

HY-141486A

PROTAC PARP/EGFR ligand 1	PARP EGFR Ligands for Target Protein for PROTAC	Others
PROTAC PARP/EGFR ligand 1 is an active compound that can be used for the synthesis of dual PARP EGFR degraders by proteolytic targeting chimera (PROTAC) technology .

HY-149862

ARD-2051	PROTACs Androgen Receptor	Cancer
ARD-2051 is a potent and orally active androgen receptor (AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC₅₀ values of 0.6 nM for AR protein degradation in both the LNCaP and VCaP prostate cancer cell lines. ARD-2051 can be used for the research of prostate cancer .

HY-157213

LWY713	Apoptosis PROTACs FLT3	Cancer
LWY713 is a PROTAC-class FLT3 degrader (DC₅₀=0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways. LWY713 inhibits cell proliferation and induces G0/G1 phase arrest and apoptosis in MV4-11 cells. LWY713 shows effective in vivo antitumor activity in MV4-11 xenograft models . LWY713 consists of a target protein ligand (red part) Gilteritinib (HY-12432), an E3 ubiquitin ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC linker (black part) Glycolic acid (HY-W015967). E3 ubiquitin ligase and linker can form Lenalidomide-Glycolic acid (HY-169373); the active control for the target protein ligand is Naproxen Gilteritinib (HY-169374).

HY-145815

JPS014	HDAC PROTACs	Cancer
JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-145816

JPS016	HDAC PROTACs	Cancer
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-145818

JPS035	HDAC PROTACs	Cancer
JPS035 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS035 degrades class I histone deacetylase (HDAC). JPS035 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-145819

JPS036	HDAC PROTACs	Cancer
JPS036 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS036 degrades class I histone deacetylase (HDAC). JPS036 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-145816A

JPS016 TFA	HDAC PROTACs	Cancer
JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-126147

J22352	HDAC	Cancer
J22352 is a PROTAC (proteolysis-targeting chimeras)-like and highly selective HDAC6 inhibitor with an IC₅₀ value of 4.7 nM. J22352 promotes HDAC6 degradation and induces anticancer effects by inhibiting autophagy and eliciting the antitumor immune response in glioblastoma cancers, and leading to the restoration of host antitumor activity by reducing the immunosuppressive activity of PD-L1 .

HY-125877

PROTAC Mcl1 degrader-1 1 Publications Verification	PROTACs Bcl-2 Family	Cancer
PROTAC Mcl1 degrader-1 (compound C3), a proteolysis targeting chimera (PROTAC) based on Cereblon ligand, is a potently and selectively Mcl-1 (Bcl-2 family member) inhibitor with an IC₅₀ of 0.78 μM. PROTAC Mcl1 degrader-1 inhibits Bcl-2 with an IC₅₀ of 0.54 μM .

HY-145388

AU-15330 4 Publications Verification	PROTACs Epigenetic Reader Domain	Cancer
AU-15330 is a proteolysis-targeting chimera (PROTAC) degrader of the SWI/SNF ATPase subunits, SMARCA2 and SMARCA4. AU-15330 induces potent inhibition of tumour growth in xenograft models of prostate cancer and synergizes with the AR antagonist enzalutamide. AU-15330 induces disease remission in castration-resistant prostate cancer (CRPC) models without toxicity .

HY-145815A

JPS014 TFA	PROTACs HDAC Apoptosis	Cancer
JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 TFA degrades class I histone deacetylase (HDAC). JPS014 TFA is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells .

HY-162106

PROTAC GPX4 degrader-2	Ferroptosis PROTACs Glutathione Peroxidase	Cancer
PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC_{50, 48h} value of 1.68 μM. PROTAC GPX4 degrader-2 induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. PROTAC GPX4 degrader-2 has anti-proliferative effect .

HY-163445

NAMPT activator-6	NAMPT	Cancer
NAMPT activator-6 is a NAMPT activator, a regulatory molecule for the optical control system of NAMPT and NAD+. NAMPT activator-6 can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) to achieve up-down reversible regulation of NAMPT and NAD+ in a light-dependent manner and reduce the toxicity associated with inhibitor-based PS-PROTACs. PS-PROTAC can be used to achieve antitumor activity, NAMPT, and NAD+ modulation in vivo via optical manipulation .

HY-P10446

TAT-PiET-PROTAC	Epigenetic Reader Domain	Cancer
TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445). TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can disrupt the interaction between the breast cancer oncogene BRD4/JMJD6 and inhibit the growth of breast cancer cells. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells and is a potential inhibitor of breast cancer .

HY-148334

MS8815	PROTACs Histone Methyltransferase	Cancer
MS8815 is a selective enhancer of zeste homolog 2 (EZH2) PROTAC degrader. MS8815 has inhibition activity for EZH2 with an IC₅₀ value of 8.6 nM. MS8815 can be used for the research of triple-negative breast cancer (TNBC) .

Cat. No.	Product Name

HY-L151

PROTAC Library	296 compounds
PROTACs (Proteolysis-targeting chimeras) is a class of molecules that utilize ubiquitin-proteasome system (UPS) to ubiquitinate and degrade target proteins. The PROTACs molecule consists of two ligands joined by a linker. The one-to-one interaction between PROTACs and target proteins determines the high efficiency of PROTACs, making it a potential molecule for targeted protein degradation (TPD) therapy. MCE supplies a unique collection of 296 PROTACs that effectively degrade target proteins with more powerful screening capability. MCE PROTAC Library is a useful tool for signal pathway research, protein degradation therapy research, drug discovery and drug repurposing, etc.

PROTAC Library

296 compounds

PROTACs (Proteolysis-targeting chimeras) is a class of molecules that utilize ubiquitin-proteasome system (UPS) to ubiquitinate and degrade target proteins. The PROTACs molecule consists of two ligands joined by a linker. The one-to-one interaction between PROTACs and target proteins determines the high efficiency of PROTACs, making it a potential molecule for targeted protein degradation (TPD) therapy.

MCE supplies a unique collection of 296 PROTACs that effectively degrade target proteins with more powerful screening capability. MCE PROTAC Library is a useful tool for signal pathway research, protein degradation therapy research, drug discovery and drug repurposing, etc.

HY-L129

Target Protein Ligand Library	37 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 37 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

37 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 37 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.

HY-L128

E3 Ligase Ligand Library	54 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 54 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

54 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 54 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-P10446

TAT-PiET-PROTAC	Epigenetic Reader Domain	Cancer
TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445). TAT-PiET is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can disrupt the interaction between the breast cancer oncogene BRD4/JMJD6 and inhibit the growth of breast cancer cells. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells and is a potential inhibitor of breast cancer .

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