PROTACs
PROTAC (PROteolysis-TArgeting Chimera) is a heterobifunctional nanomolecule containing two different ligands, ligand for ubiquitin E3 and ligand for target protein. The two parts are connected by linker to form a "three-unit" polymer, target protein ligand-linker-E3 ligase ligand. Building blocks of PROTAC molecules include PROTAC Linker, Ligand for Target Protein for PROTAC, Ligand for E3 Ligase, E3 Ligase Ligand-Linker Conjugate, Target Protein Ligand-Linker Conjugate, etc.
Alle PROTACs Isoform-spezifische Produkte anzeigen
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PROTACs Verwandte Produkte (1334)
Verwandte Produkte (1334)
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Antibodies (1)
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PROTACs Isoform Comparison
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cis-VZ185
0 ImagesArt. -Nr.: HY-114322ACAS. Nr.: 2306193-98-4cis-VZ185 serves as a non-degradative control and inactive analog of VZ185 (HY-114322), a dual-target BRD7/BRD9 degrader PROTAC. cis-VZ185 exerts antiproliferative activity against epithelioid sarcoma cells only at high concentrations. cis-VZ185 induces morphological changes in osteosarcoma cells. cis-VZ185 can be used in studies related to epithelioid sarcoma.
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MPD2
0 ImagesArt. -Nr.: HY-162464MPD2 is a Cereblon (CRBN) ligand and SARS-CoV-2 MPro degrader with an IC50 <1000 nM against SARS-CoV-2 MPro[1]. MPD2 engages CRBN to mediate ubiquitination and proteasomal degradation of SARS-CoV-2 MPro, reducing SARS-CoV-2 MPro protein levels in infected cells. MPD2 inhibits viral replication of various SARS-CoV-2 strains and acts against nirmatrelvir-resistant SARS-CoV-2 viruses. MPD2 can be used for the research of covid-19 and for fighting against drug-resistant viral variants..
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XF056-132
0 ImagesArt. -Nr.: HY-150400ACAS. Nr.: 2694057-55-9Synonyms: MS132N TFAXF056-132 (MS132N TFA) is an inactive WDR5 PROTAC degrader with a Kd value of 106 nM against human targets, and exhibits no significant binding to the VHL complex, serves as a negative control for MS132. XF056-132 binds to WDR5, does not induce WDR5 degradation in pancreatic cancer cells, and exerts no inhibitory effect on adenocarcinoma cells. XF056-132 can be used in the research of pancreatic ductal adenocarcinoma.
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PROTAC VEGFR-2 degrader-1
0 ImagesArt. -Nr.: HY-146368CAS. Nr.: 2601594-19-6
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PROTAC SMARCA2/4 degrader-8
0 ImagesArt. -Nr.: HY-159460CAS. Nr.: 2568507-14-0
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PROTAC HPK1 Degrader-7
0 ImagesArt. -Nr.: HY-179727PROTAC HPK1 Degrader-7 (compound D02) is a potent and selective PROTAC HPK1 degrader with an DC50 of 3.07 nM. PROTAC HPK1 Degrader-7 exhibits selectivity over GLK. PROTAC HPK1 Degrader-7 induces HPK1 degradation in a CRBN- and proteasome-dependent manner. PROTAC HPK1 Degrader-7 inhibits SLP-76 phosphorylation, induces IL-2 and IFN-γ secretion in human primary T cells. PROTAC HPK1 Degrader-7 can be used for immunology research.
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PROTAC WDR5 degrader 1
0 ImagesArt. -Nr.: HY-168487CAS. Nr.: 2737222-94-3PROTAC WDR5 degrader 1 is a heterobifunctional WDR5 PROTAC degrader with a DC50 value of 53 nM and a Kd value of 18 nM, exhibiting selective WDR5 degradation activity and cell permeability. PROTAC WDR5 degrader 1 induces proliferation defects in leukemia cells, with enhanced efficacy in cells overexpressing VHL. PROTAC WDR5 degrader 1 is applicable to research related to acute myeloid leukemia.
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PROTAC TSSK1 Degrader-2
0 ImagesArt. -Nr.: HY-184464PROTAC TSSK1 Degrader-2 is a cereblon-recruiting PROTAC degrader targeting TSSK1, with a DC50 of 10.8 nM and an IC50 of 56.8 nM against TSSK1. PROTAC TSSK1 Degrader-2 recruits the cereblon E3 ubiquitin ligase to induce proteasomal degradation of TSSK1. PROTAC TSSK1 Degrader-2 reduces the motility and in vitro fertilization capacity of mouse sperm. PROTAC TSSK1 Degrader-2 undergoes metabolic N-dealkylation and exhibits high efflux. PROTAC TSSK1 Degrader-2 can be used in studies related to male fertility.
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PROTAC erf3a Degrader-2
0 ImagesArt. -Nr.: HY-163938ACAS. Nr.: 3033871-15-4PROTAC erf3a Degrader-2 (Compound C59) is an orally active PROTAC erf3a Degrader. PROTAC erf3a Degrader-2 inhibits protein expression of SRD5A3 and GSPT1(eRF3a). PROTAC erf3a Degrader-2 inhibits cancer cell proliferation (eg: 22Rv1). PROTAC erf3a Degrader-2 can be used for research of prostate cancer, ovarian cancer, liver cancer, cervical cancer, leukemia, breast cancer.
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PROTAC sEH degrader-1
0 ImagesArt. -Nr.: HY-159494PROTAC sEH degrader-1 is a PROTAC degrader targeting soluble epoxide hydrolase (sEH) with a DC50 of 0.5 nM, and it also possesses sEH inhibitory activity. PROTAC sEH degrader-1 has an IC50 of 3.8 nM against human sEH and an IC50 of 210 nM against mouse sEH. PROTAC sEH degrader-1 relies on the ubiquitin-proteasome system to achieve target protein degradation, and it selectively degrades cytoplasmic sEH. PROTAC sEH degrader-1 rapidly reduces endoplasmic reticulum stress in cells, downregulates the phosphorylation levels of IRE1α, PERK and eIF2α, enhances cell viability, and alleviates Thapsigargin (HY-13433)-induced apoptosis. PROTAC sEH degrader-1 effectively degrades sEH in mouse liver and brown adipose tissue. PROTAC sEH degrader-1 can be used in studies related to metabolic disorders and inflammation.
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PROTAC IRAK4 degrader-14
0 ImagesArt. -Nr.: HY-181708CAS. Nr.: 3113890-51-7
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BI01826025
0 ImagesArt. -Nr.: HY-153574Synonyms: pArg-JQ1BI01826025 (pArg-JQ1) is a BacPROTAC-type bifunctional degrader that induces the degradation of BRDTBD1-containing substrates by recruiting the ClpC1P1P2 protease system. BI01826025 binds to the BRDTBD1 substrate via its JQ1 moiety and to ClpC1 via its pArg moiety; it delivers the substrate to ClpC1, where the substrate undergoes ClpC1-mediated unfolding followed by proteolysis by ClpP1P2. BI01826025 can be used to study ClpC1P1P2-mediated targeted protein degradation and ClpC2-regulated bacterial protein homeostasis.
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PROTAC SMARCA2/4 degrader-3
0 ImagesArt. -Nr.: HY-159454CAS. Nr.: 2568507-10-6
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EC21
0 ImagesArt. -Nr.: HY-184678EC21 is a PROTAC degrader that binds to CDK6, thereby targeting EYA2 for degradation. EC21 enhances the interaction between CDK6 and EYA2, thereby driving ubiquitin-proteasome-dependent degradation of EYA2. EC21 reduces EYA2 protein levels in tumor tissues without obvious toxicity. EC21 disrupts the DNA damage repair pathway and inhibits cancer cell proliferation. EC21 can be used in breast cancer-related research.
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PROTAC SMARCA2 degrader-5
0 ImagesArt. -Nr.: HY-159449CAS. Nr.: 2568277-68-7PROTAC SMARCA2 degrader-5 (Compound I-425) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2. PROTAC SMARCA2 degrader-5 degrades SMARCA2 in MV411 and in A549 with DC50 <100 nM, degrades SMARCA4 with DC50 of 100-500 nM. (Pink: Ligand for target protein (HY-159531); Black: Linker (HY-159538); Blue: Ligand for E3 ligase (S,R,S)-AHPC (HY-125845))
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JQ1-JX5
0 ImagesArt. -Nr.: HY-183575JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. JQ1-JX5 covalently modifies Cys58 of DCAF16, promotes ternary complex formation with BRD4, enables BRD4 ubiquitination and proteasomal degradation. JQ1-JX5 induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC50 of 43.97 and 16.77 nM. JQ1-JX5 can be used for the research of cancer, such as acute myeloid leukemia.
