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.
PROTACs Isoform Specific Products
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PROTACs Related Products (1355)
Related Products (1355)
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Antibodies (1)
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PROTACs Isoform Comparison
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HaloPROTAC 4
0 ImagesCat. No.: HY-187337HaloPROTAC 4 is a HaloPROTAC degrader with a pIC50 of 8.1 against human CRBN. HaloPROTAC 4 binds to CRBN to recruit the CUL4CRBN E3 ubiquitin ligase complex, and covalently binds to HaloTag fusion proteins, thereby inducing proteasome-dependent degradation of HaloTag fusion proteins. HaloPROTAC 4 serves as a protein knockdown tool for chemogenetic-related studies.
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His-TERRα
0 ImagesCat. No.: HY-180961CAS No.: 2408835-49-2His-TERRα is a ERRα PROTAC degrader. His-TERRα uses a single amino acid (His) as the E3 ligand and employs the N-end rule pathway to induce the degradation of the target protein, significantly reducing the molecular size, and thus is called a mini-PROTAC. His-TERRα significantly inhibits the proliferation and migration of MCF7 breast cancer cells. His-TERRα can be used for the study of breast cancer.
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Jak1 RIMTAC-1
0 ImagesCat. No.: HY-187502Jak1 RIMTAC-1 is a JAK1 RIMTAC degrader (a PROTAC-like agent) with a DC50 of 322.8 nM. Jak1 RIMTAC-1 forms a ternary complex with JAK1 and RIPK1, thereby recruiting the VHL E3 ligase complex to ubiquitinate JAK1 via the ubiquitin-proteasome system and mediate its subsequent proteasomal degradation. Jak1 RIMTAC-1 does not alter JAK1 mRNA levels (pink: Jak1 ligand-1 (HY-187503); blue: RIPK1-ligand-4 (HY-187391); black: Linker (HY-B0704)).
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Azo-PROTAC-4C-trans
0 ImagesCat. No.: HY-180983Azo-PROTAC-4C-trans is a BCR-ABL PROTAC degrader that can efficiently degrade the BCR-ABL fusion protein and ABL protein. Azo-PROTAC-4C-trans exhibits potent selective anti-proliferative activity against K562 cells. Azo-PROTAC-4C-trans allows real-time, reversible regulation of its activity via UV (to inactivate it) /visible light (to activate it) irradiation. Azo-PROTAC-4C-trans can be used for the study of myeloid leukemia.
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dASK1
0 ImagesCat. No.: HY-174862CAS No.: 3064086-31-0dASK1 is a selective and cereblon (CRBN)-based PROTAC degrader of apoptosis signal-regulating kinase 1 (ASK1). dASK1 forms a stable ternary complex with ASK1, facilitating ASK1 rapid and sustained degradation via the ubiquitin-proteasome pathway. dASK1 demonstrates potent ASK1 degradation. dASK1 can be used for the research of steatohepatitis.
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PROTAC AURKB Degrader-1
0 ImagesCat. No.: HY-184329CAS No.: 3114874-73-3PROTAC AURKB Degrader-1 is a selective AURKB PROTAC degrader with a DC50 value of 0.6 nM. PROTAC AURKB Degrader-1 promotes ubiquitination and degradation of AURKB. PROTAC AURKB Degrader-1 downregulates the expression levels of chromosomal passenger complex components Borealin, INCENP, Survivin as well as the transcription factor YY1. PROTAC AURKB Degrader-1 induces G2/M phase arrest and triggers Apoptosis in cells. PROTAC AURKB Degrader-1 serves as a chemical probe for biological studies of the chromosomal passenger complex. PROTAC AURKB Degrader-1 can be used in research related to acute myeloid leukemia, colorectal cancer, and non-small cell lung cancer.
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PROTAC ERα Degrader-11
0 ImagesCat. No.: HY-174870PROTAC ERα Degrader-11 is a selective and intrinsically fluorescent (Ex: 366 nm, Em: 440 nm) ERα PROTAC degrader. PROTAC ERα Degrader-11 shows good antiproliferative activity, selective ERα degradation and imaging capabilities in MCF-7 breast cancer cell lines. PROTAC ERα Degrader-11 induces G2/M phase arrest and induces apoptosis in MCF-7 cells. PROTAC ERα Degrader-11 is well-tolerated up to a dose of 500 mg/ kg with no acute toxicity in athymic nude mice. PROTAC ERα Degrader-11 can be used for the study of breast cancer.(Pink: ERα ligand (HY-167701), Blue: CRBN Ligand (HY-150831), Black: Linker, E3 ligase ligand-linker conjugate (HY-174880)).
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LUF7996
0 ImagesCat. No.: HY-180571CAS No.: 3104736-80-0LUF7996 is a CCR2 PROTAC Degrader degrading CCR2 with DC50 = 2.6 μM. LUF7996 demonstrates engagement of both and the E3 ligase cereblon and displays sustain and concentration-dependent degradation of CCR2. LUF7996 reliance on the lysosomal pathway to induce CCR2 degradation. LUF7996 efficiently inhibits monocyte migration in virto.
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PROTAC PI3K/110β degrader-2
0 ImagesCat. No.: HY-174469CAS No.: 3070438-79-5PROTAC PI3K/110β degrader-2 is a selective PI3K/p110β PROTAC degrader. PROTAC PI3K/110β degrader-2 can significantly degrade 110β protein and inhibit the expression of P-glycoprotein. PROTAC PI3K/110β degrader-2 can increase the level of reactive oxygen species (ROS). PROTAC PI3K/110β degrader-2 exerts anti-tumor effects by activating the endoplasmic reticulum stress (ERS)-mediated mitochondrial apoptosis pathway and inhibiting the AKT/Bcl-2 signaling pathway. PROTAC PI3K/110β degrader-2 can be used for research on cancer.
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Tamoxifen-PEG-Clozapine
0 ImagesCat. No.: HY-168869CAS No.: 3104316-29-9Tamoxifen-PEG-Clozapine is a ERα PROTAC degrader. Tamoxifen-PEG-Clozapine induces ubiquitination and degradation of ERα protein. Tamoxifen-PEG-Clozapine mediates ERα degradation by utilizing UBR5 as a component of the ubiquitin-proteasome system. Tamoxifen-PEG-Clozapine exhibits anticancer activity against breast cancer. Tamoxifen-PEG-Clozapine can be used in the research of breast cancer.
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(S,R)-CFT8634
0 ImagesCat. No.: HY-145925CCAS No.: 2704617-95-6(S,R)-CFT8634 is a BRD9 PROTAC degrader that exerts activity via the ubiquitin-proteasome pathway. (S,R)-CFT8634 can be used in the research of acute myeloid leukemia, malignant rhabdoid tumor, synovial sarcoma, and multiple myeloma.
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PROTAC SMARCA2/4 degrader-33
0 ImagesCat. No.: HY-162741CAS No.: 2568276-36-6
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PROTAC TEAD/IAP degrader-1
0 ImagesCat. No.: HY-181594PROTAC TEAD/IAP degrader-1 is a TEAD/IAP PROTAC degrader. PROTAC TEAD/IAP degrader-1 is also a specific and Nongenetic inhibitor of apoptosis protein (IAP)-dependent protein eraser (SNIPERs). PROTAC TEAD/IAP degrader-1 recruits cIAP1 to form ternary complexes, induces ubiquitination, proteasomal TEAD1, TEAD4 degradation. PROTAC TEAD/IAP degrader-1 inhibits TEAD transcriptional activity, reduces CTGF expression, and reduces cell proliferation. PROTAC TEAD/IAP degrader-1 can be used for the research of mesothelioma.
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BI-0319
0 ImagesCat. No.: HY-176198CAS No.: 2341740-85-8BI-0319 is a potent and selective PTK2 PROTAC degrader with an IC50 of 19 nM and a DC50 of 243 nM (in A549 cells). By bridging PTK2 and VHL E3 ubiquitin ligase, BI-0319 induces polyubiquitination of PTK2, leading to its targeted degradation via the ubiquitin-proteasome system. BI-0319 can be used in research related to liver cancer and non-small cell lung cancer.
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BRD4 RIMTAC-1
0 ImagesCat. No.: HY-187390BRD4 RIMTAC-1 is a BRD4 PROTAC degrader based on the RIPK1-mediated targeted chimera (RIMTAC) technology. It hijacks the endogenous RIPK1-VHL complex via the RIPK1 inhibitor moiety to indirectly recruit the VHL E3 ligase, forming a BRD4-Compound 10-RIPK1-VHL quaternary complex, and degrades BRD4 through the ubiquitin-proteasome system (UPS). BRD4 RIMTAC-1 exhibits selectivity over other BET proteins, induces concentration- and time-dependent, reversible post-translational degradation of BRD4 without altering the target mRNA level. BRD4 RIMTAC-1 potently induces endogenous BRD4 degradation in RAW264.7 and HEK-293T cells, with DC50 values of 179.1 nM and 54.12 nM, respectively. BRD4 RIMTAC-1 can be used for the research of cancer and inflammation-related diseases.
