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 (1398)
Related Products (1398)
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Antibodies (1)
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PROTACs Isoform Comparison
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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 VHL-recruiting PI3K/110β PROTAC degrader, with DC50 values of 1.258 μM and 2.185 μM in MCF-7/ADM and A549/DDP cells, respectively. PROTAC PI3K/110β degrader-2 induces proteasomal degradation of PI3K/110β, inhibits phosphorylation of AKT and expression of Bcl-2, while suppressing the activity and expression of P-gp. It also induces endoplasmic reticulum stress and mitochondrial apoptosis via the PERK/CHOP pathway. PROTAC PI3K/110β degrader-2 exerts anti-tumor activity against multidrug-resistant cancer cells both in vitro and in vivo, and produces a synergistic effect when combined with Doxorubicin (HY-15142A) or Cisplatin (HY-17394), making it applicable for the research of multidrug-resistant cancers.
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ISM-PR44
0 ImagesCat. No.: HY-189442ISM-PR44 is an orally active PROTAC degrader targeting BTK, with a DC50 of 0.05 nM in BTK-HiBiT Ramos cells. ISM-PR44 recruits CRBN E3 ligase to induce ubiquitination and proteasomal degradation of BTK. ISM-PR44 exhibits antiproliferative and cytotoxic activities in B-cell lymphoma cells. ISM-PR44 can be used for research on B-cell lymphoma.
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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 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 (FAK) 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.
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PROTAC PAPD5 degrader 1
0 ImagesCat. No.: HY-162327PROTAC PAPD5 degrader 1 is a selective PAPD5 PROTAC degrader. PROTAC PAPD5 degrader 1 induces ubiquitination and degradation of PAPD5 without causing degradation of PAPD7. PROTAC PAPD5 degrader 1 reduces Hepatitis B virus mRNA and Hepatitis B surface antigen levels in vitro. PROTAC PAPD5 degrader 1 inhibits both Hepatitis A virus and Hepatitis B virus. PROTAC PAPD5 degrader 1 can be used for research on Hepatitis A virus infection and Hepatitis B virus infection.
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Psa-AR
0 ImagesCat. No.: HY-179056Psa-AR is a PROTAC degrader targeting PSMA, with a Kd of 7.2 nM. Psa-AR exhibits strong degradation capabilities for AR, AR-V7, and HSP90, and induces cell apoptosis. Psa-AR demonstrates potent tumor suppressive activity in the 22Rv1 xenograft tumor model. Psa-AR can be used in the research of castration-resistant prostate cancer.
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RIP2 Kinase Inhibitor 4
0 ImagesCat. No.: HY-136010CAS No.: 2126803-41-4
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ML 2-23
0 ImagesCat. No.: HY-153582ML 2-23 is a PROTAC degrader that recruits RNF114 to target BCR-ABL/c-ABL for degradation. ML 2-23 promotes proteasome-dependent degradation of the target protein and inhibits phosphorylation of downstream CRKL. At concentrations used for BCR-ABL degradation, ML 2-23 only causes slight impairment to the viability of cancer cells. ML 2-23 can be used in the research of chronic myeloid leukemia.
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PROTAC EML4-ALK Degrader-1
0 ImagesCat. No.: HY-174368Synonyms: Pro-BAPROTAC EML4-ALK Degrader-1 (Pro-BA) is an orally active EML4-ALK PROTAC degrader that recruits GID4, with a Kd value of 144 nM against human EML4-ALK and a DC50 of 74 nM in H3122 cells. PROTAC EML4-ALK Degrader-1 promotes EML4-ALK ubiquitination and proteasomal degradation, reduces cancer cell viability, inhibits cancer cell and tumor growth, induces apoptosis, and alters cell cycle distribution. PROTAC EML4-ALK Degrader-1 can be used in studies related to EML4-ALK-positive cancers and non-small cell lung cancer.
