Search Result
Results for "
Chimeras.
" in MedChemExpress (MCE) Product Catalog:
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-139482
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LYTACs
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Cancer
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tri-GalNAc-COOH is an asialoglycoprotein receptor (ASGPR) ligand that can be used for LYsosome TArgeting Chimera (LYTAC) research .
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- HY-161408
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GePhos1
1 Publications Verification
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EGFR
Apoptosis
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Cancer
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GePhos1, a EGFR-targeting PhosTAC (phosphorylation targeting chimera), induces EGFR dephosphorylation. GePhos1 induces apoptosis .
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- HY-129652
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AUTACs
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Cancer
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HaloAUTAC tt15 is an autophagy-targeting chimera (AUTAC), that targets the Halo Tag carrying proteins, and degrades via the autophagy mechanism .
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- HY-134640
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AUTAC4
2 Publications Verification
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AUTACs
Mitophagy
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Neurological Disease
Cancer
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AUTAC4 is a mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC4 downregulates cytosolic proteins and promotes targeted mitochondrial turnover via mitophagy .
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- HY-148509
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Others
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Cancer
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PhosTAC5 is a phosphorylation targeting chimera (PhosTAC) molecule composed of a linker with fivePEG groups. PhosTAC5 induces dephosphorylation of PDCD4 and FOXO3a .
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- HY-111758
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PROTACs
Raf
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Cancer
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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 .
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- HY-168865
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Ligands for E3 Ligase
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Cancer
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E3 ligase Ligand 53 is a FEM1B ligand used to recruit Fem-1 homologue B (FEM1B) proteins. E3 ligase Ligand 53 can be attached to target protein ligands (e.g. HDAC1) via a linker to form PROTAC molecules (e.g. FF2049) .
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- HY-162241
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PROTACs
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Others
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SJH1-62B is a proteolysis targeting chimera (PROTAC) that can target the androgen receptor (AR) .
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- HY-168139
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P2Y Receptor
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Cancer
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MRS4865 (compund 7a) is a chimera of a P2Y14 receptor antagonist and a UDP-glucose agonist that protects against neuropathic pain .
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- HY-141486A
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- HY-163019
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- HY-148508
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Others
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Cancer
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PhosTAC3 is a phosphorylation targeting chimera (PhosTAC) molecule composed of a linker with three PEG groups. PhosTAC3 induces dephosphorylation of PDCD4 and FOXO3a .
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- HY-162966
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Cyclic GMP-AMP Synthase
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Cancer
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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. .
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- HY-161744
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AUTOTACs
Autophagy
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Cancer
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PBA-1106 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1106 increases the autophagic flux of Ub-conjugated aggregates .
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- HY-143343
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Wee1
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Cancer
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LEB-03-153 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through no linker .
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- HY-103455
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Estrogen Receptor/ERR
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Others
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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.
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- HY-143340
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Wee1
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Cancer
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LEB-03-145 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C5 alkyl linker .
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- HY-143344
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PROTACs
CFTR
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Inflammation/Immunology
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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 .
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- HY-123961
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PROTACs
c-Met/HGFR
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Cancer
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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) .
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- HY-161746
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AUTOTACs
Autophagy
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Cancer
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Anle138b-F105 is an autophagy targeting chimera (AUTOTAC) with DC50 values of 3 nM. Anle138b-F105 targetes tauP301L for lysosomal degradation .
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- HY-400766
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Drug Intermediate
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Cancer
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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 .
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- HY-156395
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MN551
1 Publications Verification
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E1/E2/E3 Enzyme
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Cancer
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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 .
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- HY-139156
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SK-575
1 Publications Verification
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PROTACs
PARP
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Cancer
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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 .
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- HY-156814
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Hedgehog
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Cancer
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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[.
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- HY-124625
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- HY-401056
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Drug Intermediate
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Cancer
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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 .
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- HY-147102
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LYTACs
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Metabolic Disease
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tri-GalNAc biotin is a biotinylated ASGPR (Asialoglycoprotein receptor) ligand. tri-GalNAc biotin promotes cellular uptake of neutravidin (NA) via ASGPR. tri-GalNAc biotin delivers neutravidin to lysosomes for degradation. tri-GalNAc biotin can be used for research of LYsosome TArgeting Chimera (LYTAC) .
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- HY-148381
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Epigenetic Reader Domain
PROTACs
Apoptosis
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Cancer
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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 Kd value of 93 nM. A947 can be used for the research of cancer .
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- HY-161743
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AUTOTACs
Autophagy
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Neurological Disease
Cancer
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PBA-1105 is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 selectively binds to exposed hydrophobic regions of misfolded proteins, facilitating their degradation via the autophagic pathway. PBA-1105 increases the autophagic flux of Ub-conjugated aggregates .
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- HY-144999
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Wee1
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Cancer
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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 .
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- HY-133869
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cGMP-HaloTag-ligand
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Autophagy
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Cancer
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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 .
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- HY-170453
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Epigenetic Reader Domain
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Cancer
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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 .
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- HY-158408
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ULK
Mitophagy
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Neurological Disease
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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 .
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- HY-143342
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Wee1
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Cancer
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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 .
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- HY-135312
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Estrogen Receptor/ERR
PROTACs
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Cancer
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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 .
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- HY-162504
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SARS-CoV
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Infection
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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 .
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- HY-158985
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AUTACs
Autophagy
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Cancer
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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) .
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- HY-161745
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AUTOTACs
p62
Autophagy
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Cancer
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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 .
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- HY-161743A
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AUTOTACs
Autophagy
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Neurological Disease
Cancer
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PBA-1105 TFA is an autophagy-targeting chimera (AUTOTAC) that induces p62 self-oligomerization. PBA-1105 TFA selectively binds to exposed hydrophobic regions of misfolded proteins, facilitating their degradation via the autophagic pathway. PBA-1105 TFA increases the autophagic flux of Ub-conjugated aggregates .
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- HY-156820
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Epigenetic Reader Domain
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Cancer
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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 .
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- HY-160902
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Autophagy
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Others
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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 .
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- HY-152261
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PROTACs
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Cancer
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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.
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- HY-145818
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HDAC
PROTACs
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Cancer
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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 .
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- HY-145816
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HDAC
PROTACs
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Cancer
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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 .
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- HY-145819
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HDAC
PROTACs
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Cancer
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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 .
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- HY-145816A
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HDAC
PROTACs
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Cancer
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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 .
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- HY-W877989
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Ligands for E3 Ligase
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Cancer
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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 .
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- HY-156106
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Ligands for E3 Ligase
HIF/HIF Prolyl-Hydroxylase
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Cancer
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VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs) .
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- HY-168456
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Ligands for Target Protein for PROTAC
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Infection
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RNA recruiter 1 is the RNA ligand of RNAse L RIBOTAC (HY-168456), 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 1 can be utilized in the synthesis of RIBOTAC .
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- HY-145815
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HDAC
PROTACs
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Cancer
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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 .
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- HY-174877
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PROTACs
HDAC
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Cancer
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PROTAC HDAC6 degrader 6 (Compound 12) is a selective HDAC6-targeting photochemically targeting chimeras (PHOTACs) (subset of PROTAC) degrader with a ∼50% Dmax only upon activation to its cis-state with 390 nm light irradiation . Pink: HDAC6 ligand; Blue: CRBN ligase ligand (HY-A0003); Black: linker
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- HY-125877
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PROTACs
Bcl-2 Family
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Cancer
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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 .
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- HY-145388
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AU-15330
Maximum Cited Publications
10 Publications Verification
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PROTACs
Epigenetic Reader Domain
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Cancer
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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 .
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- HY-126147
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HDAC
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Cancer
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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 .
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- HY-168458
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Target Protein Ligand-Linker Conjugates
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Infection
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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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- HY-168457
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SARS-CoV
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Others
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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 .
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- HY-145815A
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PROTACs
HDAC
Apoptosis
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Cancer
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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 .
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- HY-P1556
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PKG
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Cardiovascular Disease
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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 .
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- HY-168455
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PROTACs
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Infection
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RNAse L RIBOTAC (compound C64) is 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. (Blue: RNA ligand (HY-168456); Black: linker (HY-130591); Pink: Rnase L ligand (HY-168457))
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- HY-149428
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AD4
1 Publications Verification
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PROTACs
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Cancer
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AD4 is an artemisinin derivative that is a proteolytic targeting chimera (PROTAC) targeting PCLAF. AD4 can effectively degrade PCLAF in RS4;11 cells (IC50: 0.6 nM), thereby activating the p21/Rb axis and exerting anti-tumor activity. AD4 also prolonged survival of RS4;11-transplanted NOD/SCID mice, with in vivo efficacy .
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- HY-162106
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Ferroptosis
PROTACs
Glutathione Peroxidase
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Cancer
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PROTAC GPX4 degrader-2 (compound 18a) is a proteolysis targeting chimeras (PROTACs) that can degrade glutathione peroxidase 4 (GPX4), with the DC50, 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 .
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- HY-P1556A
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PKG
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Metabolic Disease
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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 .
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- HY-145232
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Phosphatase
Tau Protein
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Neurological Disease
Cancer
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PhosTAC7 is a heterobifunctional molecule named as a Phosphorylation Targeting Chimera (PhosTAC). PhosTAC7 can dephosphorylate the PDCD4 protein, FOXO3a protein, and Tau protein by recruiting serine/threonine protein phosphatase 2A (PP2A). PhosTAC7 offers the advantage of selectively modulating the phosphorylation state of individual target proteins, making it a promising tool for research in cancer and tau protein-related neurodegenerative diseases .
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- HY-147225
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AUTACs
Mitophagy
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Neurological Disease
Metabolic Disease
Cancer
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TSPO Ligand-Linker Conjugates 1 contains a ligand for translocator protein (TSPO) and a linker, which is used for the synthesis of mitochondria-targeting autophagy-targeting chimera (AUTAC). AUTAC can bind the TSPO on the outer mitochondrial membrane (OMM) of mitochondria and degrades impaired mitochondria and proteins via mitophagy, and improves mitochondrial activity. TSPO Ligand-Linker Conjugates 1 can be used in mitochondrial dysfunction related research, including neurodegenerative diseases, cancer, and diabetes .
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- HY-171148
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PROTACs
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Cancer
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F1-RIBOTAC is a ribonuclease-targeting chimeras (RIBOTACs). F1-RIBOTAC decreases QSOX1-a mRNA expression level in an RNase L-dependent manner. F1-RIBOTAC can be used for the research of cancer . (Pink: RNA ligand (HY-168460); Black: linker (HY-W008005); Blue: RNase L ligand (HY-168452))
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- HY-124108
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ETYA
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COX
PPAR
Orthopoxvirus
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Others
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Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively) . Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 μM . Eicosatetraynoic acid specifically interferes with the replication of the cowpox virus both in vivo and in vitro . Eicosatetraynoic acid is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-163445
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NAMPT
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Cancer
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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 .
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- HY-13260
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Akt
Autophagy
Apoptosis
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Cancer
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CCT128930 is a ATP-competitive and selective inhibitor of AKT (IC50=6 nM for AKT2). CCT128930 has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). Antitumor activity.
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- HY-161742
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AUTOTACs
MetAP
Autophagy
p62
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Cancer
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Fumagilin-105 is an autophagy-targeting chimera (AUTOTAC) that degrades MetAP2 via p62-mediated macroautophagy in a ubiquitination-independent manner. Fumagilin-105 can inhibit the migration of tumor cells and induce programmed cell death. Fumagilin-105 has anti-tumor activity. (p62-ZZ ligand (HY-W489121); target-binding ligand (HY-B0751); linker (HY-W245803)) .
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- HY-P10446
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Epigenetic Reader Domain
PROTACs
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Cancer
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TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer .
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- HY-176071
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ByeTAC
Epigenetic Reader Domain
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Cancer
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TEC 4 is a ByeTAC (Bypassing E-Ligase-Targeting Chimera) BRD4 degrader, with 33% BRD4 remaining at 500 nM in Ramos B-cells. TEC 4 shows toxicity for Ramos B-cells, with an IC50 of 30.5 nM. ByeTACs directly recruits a protein to the proteasome via interactions with Rpn-13 for degradation. Pink: BRD4 lignad (HY-78695); Blue: Rpn-13 ligand (HY-159808); Black: linker (HY-W008352) .
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- HY-161740
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AUTOTACs
Estrogen Receptor/ERR
Autophagy
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Cancer
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PHTPP-1304 is a PHTPP-based autophagy targeting chimera (AUTOTAC). PHTPP-1304 induces the degradation of estrogen receptor ERβ through the autophagy pathway, rather than ubiquitination (DC50 ≈ 2 nM, in HEK293T cells; < 100 nM in ACHN renal carcinoma and MCF-7 breast cancer cells). PHTPP-1304 can induce the self-oligomerization of p62. PHTPP-1304 can be used to study various cancers mediated by ERβ .
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- HY-175179
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Epigenetic Reader Domain
E1/E2/E3 Enzyme
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Cancer
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LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells .
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- HY-155356A
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PROTACs
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Cancer
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YN14 mixture of diastereomers is the diastereomers of YN14 (HY-155356).
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 .
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- HY-149862
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PROTACs
Androgen Receptor
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Cancer
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ARD-2051 is a selective 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 exhibits effective anti-tumor activity in VCaP xenograft mice model. ARD-2051 can be used for the research of prostate cancer (Pink: AR ligand (HY-400666), Blue: CRBN Ligand (HY-14658), Black: Linker) .
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- HY-13260A
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Akt
Autophagy
Apoptosis
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Cancer
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CCT128930 hydrochloride is a potent and selective inhibitor of AKT (IC50=6 nM). CCT128930 hydrochloride has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). CCT128930 hydrochloride induces cell cycle arrest, DNA damage, and autophagy. Antitumor activity .
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- HY-158985A
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Autophagy
AUTACs
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Cancer
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Amino-PEG3-2G degrader-1 hydrochloride is the hydrochloride salt form of Amino-PEG3-2G degrader-1 (HY-158985). Amino-PEG3-2G degrader-1 hydrochloride is a conjugate of a PEG Linker and a pyrazole-linked FBnG tag for ubiquitin-proteasome system (UPS) induction. Amino-PEG3-2G degrader-1 hydrochloride can be used to synthesize autophagy-targeting chimeras (AUTACs) .
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- HY-149434
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Androgen Receptor
PROTACs
Apoptosis
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Cancer
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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 .
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- HY-155356
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PROTACs
Ras
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Cancer
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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.
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- HY-156104
-
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PROTACs
CaMK
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Neurological Disease
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CaMKIIα-PHOTAC is a photochemically targeted chimera (PHOTAC) targeting Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα). Molecules such as PHOTAC can catalyze the ubiquitination and degradation of target proteins through the endogenous proteasome under specific wavelengths of light. CaMKIIα-PHOTAC reduces synaptic function under light conditions, and it attenuates the intensity of evoked field excitatory postsynaptic potentials in the mouse hippocampus in response to physiological stimuli. CaMKIIα-PHOTAC plays a critical role in maintaining long-term potentiation and memory capacity in subcellular dendritic domains .
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- HY-149433
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Androgen Receptor
Apoptosis
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Cancer
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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 .
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- HY-146393
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PROTACs
Cytochrome P450
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Cancer
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PROTAC CYP1B1 degrader-1 (Compound 6C), a α-naphthoflavone chimera derivative, is able to eliminate cytochrome P450 (CYP)1B1-mediated agent resistance via targeted CYP1B1 degradation, with IC50s of 95.1 and 9838.6 nM for CYP1B1 and CYP1A2, respectively. PROTAC CYP1B1 degrader-1 can be used for the research of CYP1B1-overexpressing prostate cancer .
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- HY-152247
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MAP3K
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Cancer
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DDO3711, a PP5-recruiting phosphatase recruitment chimeras (PHORCs), is formed by connecting a small molecular apoptosis signal-regulated kinase 1 (ASK1) inhibitor to a PP5 activator through a chemical linker. DDO3711 specifically inhibits ASK1 (IC50 =164.1 nM) not ASK2 (IC50>20 μM). DDO3711 significantly dephosphorylates p-ASK1 T838 by recruiting PP5 and shows the ASK1-dependent antiproliferative activity. DDO3711 has anti-cancer activity and has the potential for abnormally phosphorylated oncoproteins research .
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- HY-153713
-
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PROTACs
c-Myc
Apoptosis
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Cancer
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MYC-RIBOTAC is a nucleic acid-targeting degrader (ribonuclease-targeting chimera, RIBOTAC) that targets the MYC internal ribosome entry site (IRES). MYC-RIBOTAC contains a MYC mRNA binding component and a small molecule that recruits and locally activates RNAse L1. MYC-RIBOTAC reduces MYC mRNA and protein expression levels, induces cell apoptosis, and can be used for antitumor research . MYC-RIBOTAC consists of pre-miR-155 binder Anticancer agent 167 (HY-156839), RNA binder NCI-B16 (HY-156215), and Linker Amino-PEG4-alcohol (HY-W008005).
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- HY-148118A
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LYTACs
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Cancer
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Tri-GalNAc(OAc)3 TFA is a trivalent N-acetylgalactosamine (GalNAc) derivative that can be used to synthesize GalNAc-LYTAC. Tri-GalNAc is a specific ligand targeting the asialoglycoprotein receptor (ASGPR), mediating the endocytosis and transport of cell surface proteins (such as EGFR, HER2) to lysosomes for degradation by lysosomal targeting chimeras (LYTACs). Tri-GalNAc significantly reduces the level of target proteins and inhibits downstream signaling pathways (such as EGFR-mediated Akt and MAPK signals). Tri-GalNAc(OAc)3 TFA can be used for hepatocyte targeting studies, and can degrade carcinogenic membrane proteins and inhibit tumor cell proliferation in liver cancer cell models .
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- HY-148118
-
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LYTACs
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Cancer
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Tri-GalNAc(OAc)3is a trivalent N-acetylgalactosamine (GalNAc) derivative that can be used to synthesize GalNAc-LYTAC. Tri-GalNAc is a specific ligand targeting the asialoglycoprotein receptor (ASGPR), mediating the endocytosis and transport of cell surface proteins (such as EGFR, HER2) to lysosomes for degradation by lysosomal targeting chimeras (LYTACs). Tri-GalNAc significantly reduces the level of target proteins and inhibits downstream signaling pathways (such as EGFR-mediated Akt and MAPK signals). Tri-GalNAc(OAc)3can be used for hepatocyte targeting studies, and can degrade carcinogenic membrane proteins and inhibit tumor cell proliferation in liver cancer cell models .
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- HY-114312
-
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PROTACs
MDM-2/p53
E1/E2/E3 Enzyme
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Cancer
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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.
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- HY-173320
-
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Wee1
HSP
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Cancer
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HEMTAC WEE1 degrader-1 is a HSP90-mediated targeting chimera (HEMTAC) degrader of WEE1 (HSP90 enzyme inhibitory activity is IC50: 16.76 nM). HEMTAC WEE1 degrader-1 promotes the ubiquitination and degradation of WEE1. HEMTAC WEE1 degrader-1 blocks the G2/M cell cycle. HEMTAC WEE1 degrader-1 has anticancer activity in acute myeloid leukemia (AML) patient-derived xenograft (PDX) models. HEMTAC WEE1 degrader-1 can be used in AML research. (Pink: HSP90 binder; Blue: WEE1 ligand; Black: linker) .
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- HY-173135
-
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PROTACs
Histone Demethylase
Apoptosis
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Cancer
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PROTAC KDM4 degrader-1 (Compound 11) is a KDM4-targeted proteolysis targeting chimeras (PROTAC) degrader. PROTAC KDM4 degrader-1 can degrade KDM4A-C while sparing KDM4D. PROTAC KDM4 degrader-1 exhibits potent antiproliferative activity in esophageal cancer cells. PROTAC KDM4 degrader-1 induces apoptosis and cell cycle arrest, and inhibits histone H3 lysine demethylation. (Blue: E3 ligase ligand (HY-112078), Black: linker (HY-W013381); Pink: ligand for target protein (HY-173136) ) .
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- HY-169385
-
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AUTOTACs
Androgen Receptor
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Cancer
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ATC-324 is an bivalent AR (Androgen Receptor) degrader based on the protein degradation technology platform AUTOphagy-TArgeting Chimera (AUTOTAC). ATC-324 induces the formation of AR/p62 complex, leading to autophagy-lysosomal degradation of AR. ATC-324 can reduce nuclear AR levels and downregulate target gene expression of AR and AR-v7, and also has a degradation effect on common AR mutants in PCa . ATC-324 is composed of target-binding ligand (TBL) Enzalutamide (HY-70002) and p62/SQSTM1 autophagy-targeting ligand (ATL) YT 6-2 analog-1 (HY-169386), connected by Boc-NH-PEG4-CH2CH2NH2 (HY-W008352). Among them, the active control of the target protein ligand is Enzalutamide carboxylic acid (HY-70002B), and the conjugate composed of the autophagy-targeting ligand and the linker is YT 6-2-PEG3-C2-NH2 (HY-169387).
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HY-L151
-
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396 compounds
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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 396 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.
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HY-L129
-
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64 compounds
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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 64 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.
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HY-L128
-
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94 compounds
|
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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 94 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.
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1556A
-
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PKG
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Metabolic Disease
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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 .
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- HY-P1556
-
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PKG
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Cardiovascular Disease
|
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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 .
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- HY-P10446
-
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Epigenetic Reader Domain
PROTACs
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Cancer
|
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TAT-PiET-PROTAC is a proteolysis-targeting chimera (PROTAC)-modified TAT-PiET (HY-P10445), which is a cell-penetrating peptide targeting the extra-terminal (ET) domain of BRD4. TAT-PiET-PROTAC can reduce BRD4 and JMJD6 levels and inhibit cell proliferation. TAT-PiET-PROTAC also resists the endocrine resistance of ERα-positive breast cancer cells. TAT-PiET-PROTAC can be used for the research of cancer, such as breast cancer .
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| Cat. No. |
Product Name |
|
Classification |
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- HY-152261
-
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PROTAC Synthesis
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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.
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- HY-114312
-
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PROTAC Synthesis
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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.
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- HY-168458
-
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Alkynes
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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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- HY-168457
-
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Azide
|
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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 .
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