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Chimeras.

" in MedChemExpress (MCE) Product Catalog:

By Targets:	AUTACs (5) AUTOTACs (7) LYTACs (6) Akt (2) Androgen Receptor (4) Apoptosis (8) Autophagy (12) Bcl-2 Family (1) Btk (1) c-Met/HGFR (1) c-Myc (1) CaMK (1) CFTR (1) COX (1) Cyclic GMP-AMP Synthase (1) Cytochrome P450 (1) Drug Intermediate (2) E1/E2/E3 Enzyme (2) EGFR (2) Epigenetic Reader Domain (7) Estrogen Receptor/ERR (4) FAK (1) Ferroptosis (1) Glutathione Peroxidase (1) HDAC (7) Hedgehog (1) HIF/HIF Prolyl-Hydroxylase (1) Histone Acetyltransferase (1) Ligands for E3 Ligase (3) Ligands for Target Protein for PROTAC (3) MAP3K (1) MDM-2/p53 (3) Mitophagy (3) NAMPT (1) Orthopoxvirus (1) P2Y Receptor (1) p62 (2) PARP (2) Phosphatase (1) PKG (2) PPAR (1) PROTACs (27) Radionuclide-Drug Conjugates (RDCs) (1) Raf (1) Ras (1) SARS-CoV (1) Target Protein Ligand-Linker Conjugates (2) Tau Protein (1) ULK (1) Wee1 (4)
By Research Areas:	Cancer (72) Cardiovascular Disease (1) Infection (5) Inflammation/Immunology (1) Metabolic Disease (3) Neurological Disease (5)
Click Chemistry:	Azide (1) Alkynes (1)

Inhibitors & Agonists

Screening Libraries

Peptides

Click Chemistry

Targets Recommended: AUTOTACs AUTACs LYTACs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-139482

tri-GalNAc-COOH	LYTACs	Cancer
tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research .

HY-129652

HaloAUTAC tt15	AUTACs	Cancer
HaloAUTAC tt15 is an autophagy-targeting chimera (AUTAC), that targets the Halo Tag carrying proteins, and degrades via the autophagy mechanism .

HY-134640

AUTAC4 2 Publications Verification	AUTACs Mitophagy	Neurological Disease Cancer
AUTAC4 is a mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC4 downregulates cytosolic proteins and promotes targeted mitochondrial turnover via mitophagy .

HY-148509

PhosTAC5	Others	Cancer
PhosTAC5 is a phosphorylation targeting chimera (PhosTAC) molecule composed of a linker with fivePEG groups. PhosTAC5 induces dephosphorylation of PDCD4 and FOXO3a .

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-168865

E3 ligase Ligand 53	Ligands for E3 Ligase	Cancer
E3 ligase Ligand 53 是一种 FEM1B 配体，用于募集 Fem-1 homologue B (FEM1B) 蛋白。E3 ligase Ligand 53 可通过连接子与靶蛋白配体 (例如 HDAC1) 连接，形成 PROTAC 分子 (例如 FF2049) 。

HY-162241

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

HY-161408

GePhos1	EGFR Apoptosis	Cancer
GePhos1, a EGFR-targeting PhosTAC (phosphorylation targeting chimera), induces EGFR dephosphorylation. GePhos1 induces apoptosis .

HY-168139

MRS4865	P2Y Receptor	Cancer
MRS4865 (compund 7a) is a chimera of a P2Y14 receptor antagonist and a UDP-glucose agonist that protects against neuropathic pain .

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-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-148508

PhosTAC3	Others	Cancer
PhosTAC3 is a phosphorylation targeting chimera (PhosTAC) molecule composed of a linker with three PEG groups. PhosTAC3 induces dephosphorylation of PDCD4 and FOXO3a .

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-162966

MS7829	Cyclic GMP-AMP Synthase	Cancer
MS7829 is a cGAS inhibitor-based deubiquitinase-targeted chimera (DUBTAC), a targeted protein stabilization (TPS) technology. cGAS is a key component in the cGAS-STING pathway. .

HY-143343

LEB-03-153	Wee1	Cancer
LEB-03-153 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through no linker .

HY-161743

PBA-1105	AUTOTACs Autophagy	Cancer
PBA-1105 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 increases the autophagic flux of Ub-conjugated aggregates .

HY-161744

PBA-1106	AUTOTACs Autophagy	Cancer
PBA-1106 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1106 increases the autophagic flux of Ub-conjugated aggregates .

HY-103455

ZK164015	Estrogen Receptor/ERR	Others
ZK164015 is an estrogen-glucocorticoid receptor chimera that can be used as a compound screening tool to evaluate tissue-selective estrogen activity. ZK164015 was used to evaluate its effects on ER function in osteoblasts in studies based on green fluorescent protein (GFP)-receptor chimeras. In osteoblast-like (ROS and U2OS) and breast cancer (MCF7) cells, ZK164015 showed different effects in response to ER agonists, including modulation of ERE-luc activity and effects on nuclear mobility.

HY-161742

Fumagilin-105	AUTOTACs Estrogen Receptor/ERR Autophagy p62	Cancer
Fumagilin-105 is an autophagy targeting chimera (AUTOTAC) that induces p62 self-oligomerization with DC₅₀ values of 0.7 μM for MetAP2 in HEK293 cells .

HY-143340

LEB-03-145	Wee1	Cancer
LEB-03-145 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C5 alkyl linker .

HY-143344

NJH-2-056	PROTACs CFTR	Inflammation/Immunology
NJH-2-056 is a *deubiquitinase-targeting chimera* (DUBTAC) linking the OTUB1 recruiter EN523 to the CFTR** chaperone lumacaftor. NJH-2-056 can be used for cystic fibrosis research .

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-161746

Anle138b-F105	AUTOTACs Autophagy	Cancer
Anle138b-F105 is an autophagy targeting chimera (AUTOTAC) with DC₅₀ values of 3 nM. Anle138b-F105 targetes tauP301L for lysosomal degradation .

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-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-148118

Tri-GalNAc(OAc)3	LYTACs	Cancer
Tri-GalNAc(OAc)3 is a tri-GalNAc ligand that can be used for the synthesis of GalNAc-LYTAC. GalNAc-LYTAC engages the asialoglycoprotein receptor for targeted protein degradation. tri-GalNAc: triantenerrary N-acetylgalactosamine; LYTAC: lysosome-targeting chimera .

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-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-400766

BWA-522 intermediate-2	Drug Intermediate	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	Drug Intermediate	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-148118A

Tri-GalNAc(OAc)3 TFA	LYTACs	Cancer
Tri-GalNAc(OAc)3 TFA is a tri-GalNAc ligand that can be used for the synthesis of GalNAc-LYTAC. GalNAc-LYTAC engages the asialoglycoprotein receptor for targeted protein degradation. tri-GalNAc: triantenerrary N-acetylgalactosamine; LYTAC: lysosome-targeting chimera .

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-145368

Tri-GalNAc-NHS ester	LYTACs	Others
Tri-GalNAc-NHS ester is a LYsosome TArgeting Chimera (LYTAC) and a ligand of asialoglycoprotein receptor (ASGPR). ASGPR is a lysosomal targeting receptor specifically expressed on liver cells, for the degradation of extracellular proteins including membrane proteins. Tri-GalNAc-NHS ester can be used as a protein degrader and it can be used for the research of LYTAC .

HY-133869

cGMP-HTL cGMP-HaloTag-ligand	Autophagy	Cancer
cGMP-HTL contains a HT-ligand, a linker and the Cys-S-cGMP (autophagy tag). cGMP-HTL increases the K63-linked ubiquitination of mitochondria. AUTAC (autophagy-targeting chimera) is a novel targeted-clearance strategy that contains a degradation tag (guanine derivatives) and a warhead to provide target specificity .

HY-144999

LEB-03-146	Wee1	Cancer
LEB-03-146 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a PEG2 linker. LEB-03-146 shows significant WEE1 stabilization in HEP3B hepatoma cancer cells .

HY-158408

NZ-66	ULK Mitophagy	Neurological Disease
NZ-66 is a UNC-51-like kinase 1 (ULK1) targeting chimera, which is used to achieve proximity-induced and ULK1-dependent degradation of mitochondria. NZ-66 induces mitophagy. NZ-66 is potential for attenuating neurodegenerative disorders .

HY-170453

iHAC	Epigenetic Reader Domain	Cancer
iHAC is an inhibitor HSP90-anchoring chimera, that covalently binds BRD4 ligand (+)-JQ-1 to HSP90, and inhibits the proliferation of cancer cells. iHAC activates the anti-tumor immune response, inhibits the recurrence and metastasis of 4T1 breast cancer in mouse models .

HY-143342

LEB-03-144	Wee1	Cancer
LEB-03-144 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C3 alkyl linker. LEB-03-144 shows significant WEE1 stabilization in HEP3B hepatoma cancer cells .

HY-135312

AZ'6421	Estrogen Receptor/ERR PROTACs	Cancer
AZ'6421 acts as *Protcolysis Targeting Chimera* (PROTAC)** to selectively degrade estrogen receptor alpha. AZ'6421 has a potent anti-tumour effect to inhibit the uncontrolled cellular proliferation which arises from malignant disease. AZ'6421 can be used for the research of cancer such as breast cancer .

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-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-162504

2'-RIBOTAC-U	SARS-CoV	Infection
2'-RIBOTAC-U is a ribonuclease (RNase) targeting chimeras (RIBOTACs) and SARS-CoV-2 replication inhibitor. 2'-RIBOTAC-U is composed of a metabolic handle (Blue), a linker (Black) and a RNase L recruiter (Pink). RIBOTACs recruits cellular RNases to specific RNA targets, thereby leading to the degradation of these RNAs .

HY-158985

Amino-PEG3-2G degrader-1	AUTACs Autophagy	Cancer
Amino-PEG3-2G degrader-1 (compound ) is a conjugate of a PEG Linker and a pyrazole-linked FBnG tag for ubiquitin-proteasome system (UPS) induction. Amino-PEG3-2G degrader-1 can be used to synthesize autophagy-targeting chimeras (AUTACs) .

HY-161745

PBA-1105b	AUTOTACs p62 Autophagy	Cancer
PBA-1105b is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105b increases the autophagic flux of Ub-conjugated aggregates. PBA-1105b is a drastically longer PEG-based linker than PBA-1105 .

HY-152261

MS6105	PROTACs	Cancer
MS6105 is an LDH protein hydrolysis-targeted chimera (PROTAC) that effectively degrades LDHA and LDHB in a time- and ubiquitin-proteasome system-dependent manner and has anticancer activity . MS6105 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-145368B

Tri-GalNAc(OAc)3-Perfluorophenyl	LYTACs	Cancer
Tri-GalNAc(OAc)3-Perfluorophenyl is a pentafluorophenyl modified Tri-GalNAc(OAc)3 (HY-148118), a tri-GalNAc ligand that can be used for the synthesis of GalNAc-LYTAC. GalNAc-LYTAC engages the asialoglycoprotein receptor for targeted protein degradation. tri-GalNAc: triantenerrary N-acetylgalactosamine; LYTAC: lysosome-targeting chimera .

HY-156820

HLDA-221	Epigenetic Reader Domain	Cancer
HLDA-221 is a heterobifunctional small molecules called Regulated Induced Proximity Targeting Chimeras (RIPTACs). HLDA-221 elicits a stable ternary complex between a target protein selectively expressed in cancer tissue and a pan-expressed protein essential for cell survival, thus leading to cell death selectively in cells expressing the target protein .

HY-160902

2G-HaloAUTAC	Autophagy	Others
2G-HaloAUTAC (Compound tt44) is a second-generation autophagy-targeting chimera (2G-HaloAUTAC) that improves the activity of AUTACs by replacing the L-Cysteine (L-Cys) linker with other structures. 2G-HaloAUTAC exhibits degradation activity against EGFP-HaloTag protein through an autophagic mechanism .

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 .

Cat. No.	Product Name

HY-L151

PROTAC Library

330 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 330 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

56 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 56 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

65 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 65 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-P1556A

Vasonatrin Peptide (VNP) TFA	PKG	Metabolic Disease
Vasonatrin Peptide (VNP) TFA is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide TFA possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide TFA protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway .

HY-P1556

Vasonatrin Peptide (VNP)	PKG	Cardiovascular Disease
Vasonatrin Peptide (VNP) is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway .

HY-P10446

TAT-PiET-PROTAC	Radionuclide-Drug Conjugates (RDCs) 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 . TAT-PiET-PROTAC can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).

Cat. No.	Product Name		Classification

HY-168457

RNase L ligand 2		Azide
RNase L ligand 2 (compound 6) is the Rnase L ligand part of RNAse L RIBOTAC (HY-168455), an RNA-degrading chimera which binds to a four-way RNA helix called SL5 in the 5’ UTR of the SARS-CoV-2 RNA genome and inhibits the virus replication in lung epithelial carcinoma cells. RNase L ligand 2 can be used in the synthesis of RIBOTAC .

HY-168458

RNA recruiter-linker 1		Alkynes
RNA recruiter-linker 1 is the RNA ligand-linker part of RNAse L RIBOTAC (HY-168455), an RNA-degrading chimera which binds to a four-way RNA helix called SL5 in the 5’ UTR of the SARS-CoV-2 RNA genome and inhibits the virus replication in lung epithelial carcinoma cells. RNA recruiter-linker 1 can be utilized in the synthesis of RIBOTAC .

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