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 (1395)
Related Products (1395)
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Antibodies (1)
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PROTACs Isoform Comparison
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L18I
0 ImagesL18I is a Bruton's tyrosine kinase (BTK) PROTAC degrader that targets wild-type and BTKC481, and recruits the cereblon E3 ligase to mediate proteasomal degradation. L18I regulates the BCR, TLR, FcγR and NLRP3 inflammasome signaling pathways, inhibits the phosphorylation of PLCγ-2, ERK1/2 and p38, and reduces the levels of B cell activation markers CD25, CD69 and CD86. L18I downregulates the NF-κB, TNF and TLR signaling pathways, reduces the production of pro-inflammatory cytokines, and decreases immune cell infiltration and immune complex deposition. L18I inhibits the proliferation of BTK-expressing lymphoma cells, induces tumor regression in xenograft models, and exhibits synergistic activity when combined with inhibitors of SYK, PI3K or Lyn. L18I can be used in research related to lupus, diffuse alveolar hemorrhage and B-cell lymphoma.
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PROTAC USP39 Degrader-1
0 ImagesCat. No.: HY-180907Purity: 98.00%PROTAC USP39 Degrader-1 is a USP39 PROTAC degrader with Kd values of 136 nM and 232 nM, and a DC50 value of 1.06 nM (24 h). PROTAC USP39 Degrader-1 binds to the VHL E3 ubiquitin ligase, forms a ternary complex with USP39, mediates USP39 ubiquitination and proteasomal degradation dependent on VHL recruitment, modulates splicing activity and induces 5' splice site-specific splicing patterns. PROTAC USP39 Degrader-1 can be used in the research of cervical cancer.
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MS181
0 ImagesMS181 is a BMI1 and RING1B degrader with antiproliferative activity. MS181 induces degradation via an EED-, CRBN-, and ubiquitin-proteosome system-dependent pathway, with preferential targeting over PRC2 components. MS181 acts in VHL-defective cancer cells. MS181 serves as a chemical biology tool to study PRC1 roles in cancer. MS181 can be used for the research of myelogenous leukemia, renal cell carcinoma, metastatic prostate cancer, triple negative breast cancer.
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SR-1114
0 ImagesSR-1114 is a ENL PROTAC degrader, with DC50 values of 150 nM, 311 nM and 1.65 μM in MV4;11, MOLM-13 and OCI/AML-2 cells, respectively. SR-1114 has an IC50 of 155 nM against the human CRL4CRBN complex. SR-1114 can be used in research related to acute leukemia and acute myeloid leukemia.
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TL13-12
0 ImagesTL13-12 is a CRBN-recruiting ALK PROTAC degrader, with a DC50 of 10 nM in H3122 cells. TL13-12 induces dimerization of CRBN and truncated ALK, which brings the DNA-binding domain and transactivation domain into close proximity, thereby activating the expression of downstream reporter genes, while exhibiting extremely low leaky expression under non-inducing conditions. TL13-12 serves as a tool molecule for the orthogonal PROTAC-CID system, and is applied in research on non-small cell lung cancer, anaplastic large cell lymphoma, and neuroblastoma.
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PROTAC Bcl-xL degrader-2
0 ImagesPROTAC Bcl-xL degrader-2 is a selective Bcl-xL PROTAC degrader with a DC50 of 4.8 nM against Bcl-xL. PROTAC Bcl-xL degrader-2 forms a ternary complex with VHL E3 ligase, thereby redirecting the ubiquitin-proteasome system to mediate the degradation of Bcl-xL. PROTAC Bcl-xL degrader-2 triggers Apoptosis. PROTAC Bcl-xL degrader-2 can be used in the research of solid tumors and hematologic malignancies.
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SZUH280
0 ImagesSZUH280 is a selective HDAC8 PROTAC degrader with a DC50 of 0.58 μM. SZUH280 recruits the CRBN E3 ubiquitin ligase to mediate polyubiquitination and proteasomal degradation of HDAC8, and exhibits higher selectivity for HDAC8 over other HDAC family members. SZUH280 induces apoptosis and G2/M cell cycle arrest in cancer cells. SZUH280 impairs DNA damage repair and promotes radiosensitization in cancer cells. SZUH280 inhibits the proliferation of cancer cells. SZUH280 is used in research related to lung cancer and breast cancer.
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PROTAC FKBP Degrader-3
0 ImagesPROTAC FKBP Degrader-3 is a selective FKBP PROTAC degrader with an IC50 of 1.8 nM. PROTAC FKBP Degrader-3 targets and degrades the FKBP protein by recruiting the VHL E3 ligase, and this degradation process is primarily mediated by K11 and K48 ubiquitin chain linkages. PROTAC FKBP Degrader-3 can be applied in cancer research.
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PROTAC PARP1 degrader
0 ImagesPROTAC PARP1 degrader is a PROTAC PARP1 degrader. PROTAC PARP1 degrader mediates the interaction between PARP1 and MDM2 E3 ubiquitin ligase, thereby inducing ubiquitination of PARP1 and subsequent proteasome-mediated degradation. PROTAC PARP1 degrader selectively inhibits the growth of breast cancer cells. PROTAC PARP1 degrader induces cell apoptosis by activating caspase-3 and phosphatidylserine externalization. PROTAC PARP1 degrader can be used in the research of triple-negative breast cancer.
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INY-03-041 trihydrochloride
0 ImagesCat. No.: HY-133120AINY-03-041 trihydrochloride is a potent, highly selective and PROTAC-based pan-AKT degrader consisting of the ATP-competitive AKT inhibitor Ipatasertib (HY-15186) conjugated to Lenalidomide (HY-A0003). INY-03-041 trihydrochloride inhibits AKT1, AKT2 and AKT3 with IC50s of 2.0, 6.8 and 3.5 nM, respectively.
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CCT367766 formic
0 ImagesCat. No.: HY-122653APurity: 98.10%CCT367766 formic is a pirin PROTAC degrader. CCT367766 formic forms a ternary complex with cereblon and induces pirin depletion via the ubiquitin-proteasome pathway in a concentration- and time-dependent manner. CCT367766 formic can be used for ovarian cancer research.
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DD-03-171
0 ImagesDD-03-171 is a PROTAC BTK degrader. DD-03-171 inhibits mantle cell lymphoma (MCL) cell proliferation (IC50 = 5.1 nM) and prolongs the survival of mice bearing a lymphoma PDX model by degrading BTK, IKFZ1, and IKFZ3. DD-03-171 also inhibits platelet function and thrombosis. (Pink: BTK ligand 9 (HY-168292); Black: linker (HY-28875); Blue: Thalidomide-NH-CH2-COOH (HY-131717)).
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RJS308 TFA
0 ImagesCat. No.: HY-173011APurity: 98.36%RJS308 TFA is a selective Cyclophilin A (CypA) PROTAC degrader. RJS308 TFA induces ubiquitin-dependent CypA degradation by recruiting the VHL E3 ligase complex, and forms a ternary complex with CypA and VHL/elongin C/elongin B. RJS308 TFA exhibits anti-HIV-1 and anti-HCV activities. RJS308 TFA can be used in studies related to viral infections.
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22-SLF
0 ImagesCat. No.: HY-163807CAS No.: 3079209-82-522-SLF is a PROTAC degrader, that degrades FK506-binding protein 12 (FKBP12) with a DC50 of 0.5 µM. 22-SLF interacts with C227 and C228 in FBXO22 to induce a ternary complex between FKBP12 and FBXO22, and degrades FKBP12 in a FBXO22-dependent manner. 22-SLF can be used for fundamental cancer research as a probe to study the FBXO22 degradation pathway.
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ARD-2051
0 ImagesARD-2051 is a selective and orally active androgen receptor (AR) PROTAC 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.
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PROTAC BTK Degrader-16
0 ImagesPROTAC BTK Degrader-16 is a BTK PROTAC degrader with a DC50 of 0.0006 nM in TMD8 cells. PROTAC BTK Degrader-16 recruits E3 ligase CRBN to tag BTK for degradation, leading to loss of BTK signaling. PROTAC BTK Degrader-16 induces degradation of BTK, leading to inhibition of cell growth in ABC-DLBCL cells. PROTAC BTK Degrader-16 can be used for the research of activated b-cell-like diffuse large b-cell lymphoma (ABC-DLBCL).
