PROTACs
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PROTACs Related Products (458)
Related Products (458)
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G6374
0 ImagesCat. No.: HY-180787G6374 is a IRE1 PRORAC degrader with DC50 values of 0.04 μM (AMO1) and 0.13 μM (KMS27), an EC50 value of 0.11 μM, and KD values of 0.56 nM and 90.2 nM for IRE1 and VHL, respectively. G6374 binds to the ATP pocket of the IRE1 kinase domain and VHL to form a ternary complex that recruits CRL2VHL, inducing K48-linked polyubiquitination of IRE1 at lysine residues K704 and K717, which in turn drives proteasomal degradation of monomeric and dimeric IRE1. G6374 can be used for the research of multiple myeloma.
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HC278
0 ImagesCat. No.: HY-185230CAS No.: 3096503-40-8HC278 is a selective TEAD1/TEAD3 PROTAC degrader. HC278 induces proteasome-dependent degradation by forming a stable ternary complex with CRBN/DDB1. HC278 is applicable to the research of mesothelioma.
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PROTAC NTRK1 degrader-1
0 ImagesCat. No.: HY-181052CAS No.: 2922274-35-7PROTAC NTRK1 degrader-1 is a wild-type and mutant NTRK1 PROTAC degrader with IC50 values of 4 nM (wild-type), 2 nM (G595R), 5 nM (G667C), and <0.5 nM (F598L). PROTAC NTRK1 degrader-1 catalyzes ubiquitination and subsequent proteasome-mediated degradation of wild-type and mutant (G595R, G667C, F598L) NTRK1. PROTAC NTRK1 degrader-1 can be used for the research of solid tumors.
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QZ2135
0 ImagesCat. No.: HY-170852QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854).
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PROTAC SMARCA2/4 degrader-36
0 ImagesCat. No.: HY-170347CAS No.: 3033588-00-7
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PROTAC ATR degrader-4
0 ImagesCat. No.: HY-184293PROTAC ATR degrader-4 is a PROTAC-based ATR kinase degrader, with a DC50 of 6.18 μM and a Dmax of 71.42% in LoVo cells. PROTAC ATR degrader-4 downregulates ATR protein expression, inducing nuclear envelope rupture, genomic instability, DNA damage and apoptosis. PROTAC ATR degrader-4 exhibits anti-tumor activity in xenograft tumor mouse models and can be used for the research of atm-deficient cancers.
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PROTAC FLT3/CDK9 degrader-1
0 ImagesCat. No.: HY-148521CAS No.: 3033084-05-5
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PROTAC EZH2 Degrader-17
0 ImagesCat. No.: HY-181300CAS No.: 3093642-23-7
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PROTAC SMARCA2/4 degrader-17
0 ImagesCat. No.: HY-163870CAS No.: 2568276-88-8PROTAC SMARCA2/4-degrader-17 (Compound I-345) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-17 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM.
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PROTAC FGFR3 Degrader-1
0 ImagesCat. No.: HY-181153PROTAC FGFR3 Degrader-1 is a fibroblast growth factor receptor 3 (FGFR3) PROTAC degrader, promotes FGFR3 degradation via the ubiquitin-proteasome pathway, and inhibits the downstream FGFR3/PI3K/AKT signaling pathway. PROTAC FGFR3 Degrader-1 can be used for the research of hepatocellular carcinoma.
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Pro-PEG3-BA
0 ImagesCat. No.: HY-180965CAS No.: 3057939-64-4Pro-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research.
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HP211206
0 ImagesCat. No.: HY-170598CAS No.: 3119106-17-8HP211206 is a bifunctional CRBN-recruiting SARS-CoV-2 Mpro PROTAC degrader with a CRBN IC50 of 3.2 μM and a SARS-CoV-2 Mpro DC50 of 621 nM. HP211206 recruits E3 ubiquitin ligase CRBN to drive ubiquitination and proteasomal degradation of wild-type SARS-CoV-2 Mpro and E166 mutant while inhibiting Mpro enzymatic activity, exhibits no cytotoxicity against normal mammalian cells at tested concentrations, and can be used for the study of COVID-19 and SARS-CoV-2 infection
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PROTAC EML4-ALK Degrader-2
0 ImagesCat. No.: HY-180972CAS No.: 2417174-28-6PROTAC EML4-ALK Degrader-2 is an EML4-ALK PROTAC degrader. PROTAC EML4-ALK Degrader-2 shows potent selective inhibitory activity to ALK with an IC50 of 1.6 nM. PROTAC EML4-ALK exhibits selectivity over IGF1R, INSR, FLT3, and FGFR2. PROTAC EML4-ALK Degrader-2 shows anti-cancer activities both in vitro and vivo. PROTAC EML4-ALK Degrader-2 can be used for non-small cell lung cancer (NSLC), liver lung and cervical cancer research.
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PROTAC SMARCA2/4 degrader-29
0 ImagesCat. No.: HY-162743CAS No.: 2568273-82-3PROTAC SMARCA2/4-degrader-29 (Compound I-279) is a PROTAC degrader for catalytic subunit of the SWI/SNF complex SMARCA2 and SMARCA4. PROTAC SMARCA2/4-degrader-29 degrades SMARCA2 in A549 with DC50 <100 nM, degrades SMARCA4 in MV411 with DC50 <100 nM.
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PROTAC BET Degrader-13
0 ImagesCat. No.: HY-175354PROTAC BET Degrader-13 is a BET PROTAC degrader that recruits TRIM21. PROTAC BET Degrader-13 utilizes wild-type TRIM21 to mediate the degradation of PML-eGFP-BRD4 (BD2) fusion protein aggregates, with an EC50 of 1.4 μM in A549 cells expressing TRIM21-FLAG. PROTAC BET Degrader-13 can be used for research on targeted protein degradation and protein aggregate clearance.
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BCL6-760
0 ImagesCat. No.: HY-178777CAS No.: 3084696-50-1BCL6-760 is an orally active BCL-6 PROTAC degrader with an EC50 of 0.8 nM. BCL6-760 only degrades BCL6 and has no effect on other CRBN substrates. BCL6-760 demonstrates significant efficacy in the orthotopic xenograft mouse model of OCI-LY-1 tumors. BCL6-760 can be used in the research of diffuse Large B-cell Lymphoma (DLBCL) (Pink: BCL-6 ligand (HY-179317); Blue: CRBN ligand (HY-179305); Black: Linker).
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PROTAC FLT-3 degrader 3
0 ImagesCat. No.: HY-161280PROTAC FLT-3 degrader 3 is a FLT-3 PROTAC degrader. PROTAC FLT-3 degrader 3 reduces the phosphorylation levels of FLT3-ITD, AKT, STAT5 and ERK. PROTAC FLT-3 degrader 3 induces apoptosis and cell cycle arrest in leukemia cells. PROTAC FLT-3 degrader 3 can be used for the research of acute myeloid leukemia.
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BSJ-04-146
0 ImagesCat. No.: HY-179512CAS No.: 2414478-45-6BSJ-04-146 is a highly efficient and selective PROTAC targeting focal adhesion kinase (FAK) inhibitor(IC50 = 26 nM). BSJ-04-146 achieves rapid and potent FAK degradation with high proteome-wide specificity in cancer cells and induces durable degradation in mice. BSJ-04-146 binds FAK and requires the ubiquitin-proteasome machinery to achieve FAK degradation. BSJ-04-146 can be used for the study of pancreatic cancer and triple-negative breast cancer.
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PROTAC OSBP Degrader-1
0 ImagesCat. No.: HY-178034PROTAC OSBP Degrader-1 (Compound 5) is a Oxysterol-binding protein (OSBP) PROTAC degrader with a DC50 of 322 nM (24 h). PROTAC OSBP Degrader-1 can rapidly penetrate into cells and induce massive recruitment of OSBP at the Trans-Golgi network. PROTAC OSBP Degrader-1 has potent anticancer activity with potent cytotoxicity against U-87 MG, A549, MCF7, HeLa and MDA-MB-231 cells. Pink: OSBP ligand (HY-178035); Blue: CRBN ligase ligand (HY-10984); Black: linker
