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 アイソフォーム特異的製品
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PROTACs 関連製品 (1398)
関連製品 (1398)
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抗体 (1)
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PROTACs Isoform Comparison
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MZP-54
0 ImagesMZP-54 is a PROTAC degrader that selectively targets BRD3/BRD4, with a DC50 of < 0.05 μM in AML cells. MZP-54 recruits VHL to form a ternary complex, induces BRD3/BRD4 degradation via the ubiquitin-proteasome pathway, inhibits c-Myc expression, and exerts antiproliferative activity. MZP-54 can be used for the research of acute myeloid leukemia.
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PROTAC BRD4 Degrader-8
0 ImagesPROTAC BRD4 Degrader-8 is a PROTAC connected by ligands for von Hippel-Lindau and BRD4, with IC50s of 1.1 nM and 1.4 nM for BRD4 BD1 and BD2, respectively. PROTAC BRD4 Degrader-8 is capable of potently degrading the BRD4 protein in PC3 prostate cancer cells.
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PROTAC EED degrader-1
0 ImagesPROTAC EED degrader-1 is a von Hippel-Lindau-based PROTAC targeting EED with a pKD of 9.02. PROTAC EED degrader-1 is a polycomb repressive complex 2 (PRC2) inhibitor (pIC50=8.17) targeting the EED subunit.
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SIAIS164018 hydrochloride
0 Images製品番号: HY-147219A純度: 98.06%SIAIS164018 hydrochloride is a multi-kinase (ALK, EGFR, FAK, PYK2, PTK6) PROTAC degrader, with IC50 values of 2.5 nM and 6.6 nM against ALK and ALK (G1202R), respectively. SIAIS164018 hydrochloride promotes the ubiquitination and degradation of ALK, EGFR, FAK, PYK2 and PTK6. SIAIS164018 hydrochloride induces cell cycle arrest at the G1 phase and triggers cell Apoptosis. SIAIS164018 hydrochloride exhibits preferential inhibitory activity against FER kinase. SIAIS164018 hydrochloride can be used in research related to non-small cell lung cancer, ovarian cancer and triple-negative breast cancer.
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BSJ-05-037
0 ImagesBSJ-05-037 is an ITK PROTAC degrader that effectively targets and degrades ITK in T-cell lymphoma cell lines. BSJ-05-037 blocks the activation of the NF-κB/GATA-3 signaling pathway, inhibits PLCγ1 phosphorylation, and reduces the proliferative capacity of T-cell lymphoma cells. BSJ-05-037 enhances the sensitivity of T-cell lymphoma cells to chemotherapy. In mouse models of T-cell lymphoma, BSJ-05-037 induces ITK degradation, reduces GATA-3 expression, decreases tumor volume, and reverses chemotherapy resistance. BSJ-05-037 is applicable to research related to T-cell lymphoma.
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JP-163-16
0 ImagesJP-163-16 is a NF-κB RelA/p65 PROTAC degrader that recruits CRBN. JP-163-16 selectively induces RelA/p65 degradation via the ubiquitin-proteasome pathway, exerts cytotoxicity and induces apoptosis in cancer cells, while showing low toxicity to non-malignant lymphocytes. JP-163-16 can be used for the research of chronic lymphocytic leukemia, triple-negative breast cancer and multiple myeloma.
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PROTAC AURKA degrader 3
0 Images製品番号: HY-168543純度: 99.78%PROTAC AURKA degrader 3 is a selective AURKA PROTAC degrader, with DC50 values of 2.05, 157.85 and 43.05 nM against AURKA, AURKB and TTK, respectively. PROTAC AURKA degrader 3 exhibits cytotoxicity against acute myeloid leukemia cells. PROTAC AURKA degrader 3 can be used for research related to acute myeloid leukemia.
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YD54
0 ImagesYD54 is an orally active and selective SMARCA2 PROTAC degrader. YD54 induces SMARCA4 degradation but with low potency and selectivity. YD54 selectively inhibits the growth of various cancer cells and suppresses tumor growth in mouse xenograft models. YD54 can be used for the research of SMARCA4-mutant lung cancer.
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DB-3-291
0 ImagesDB-3-291 is a CSK-targeting agent with a human CSK Kd of 1 nM and high selectivity for CSK over other kinases bound by dasatinib. DB-3-291 induces targeted degradation of CSK via a ubiquitin-dependent pathway and incorporates dasatinib as the kinase binding ligand. DB-3-291 can be used for the research of innate immune responses to viral DNA.
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ZXH-4-130 TFA
0 ImagesZXH-4-130 TFA is a potent and selective Cereblon (CRBN) degrader. ZXH-4-130 TFA recruits the VHL E3 ligase to specifically target CRBN as a substrate for selective degradation as a hetero-PROTAC molecule. ZXH-4-130 TFA can be applied in studies on the biological functions of CRBN and related research of frontotemporal dementia.
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SMD-3040 formate
0 Images製品番号: HY-156568B純度: 99.78%
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PROTAC HDAC6 degrader 2
0 Images製品番号: HY-171139純度: 99.45%PROTAC HDAC6 degrader 2 is a non‑hydroxamate selective HDAC6 PROTAC degrader with an IC50 of 0.643 μM and shows high selectivity for HDAC6 over HDAC1-4. PROTAC HDAC6 degrader 2 recruits VHL E3 ubiquitin ligase to trigger HDAC6 ubiquitination and subsequent proteasomal degradation. PROTAC HDAC6 degrader 2 selectively elevates acetylated α-tubulin levels in cancer cells, and does not induce histone H3 hyperacetylation or obvious loss of cell viability. PROTAC HDAC6 degrader 2 is applicable for research on multiple myeloma.
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L1BC8
0 ImagesL1BC8 (compound 13a) is a BRD4 PROTAC degrader with anticancer effects. L1BC8 is also a drug-linker conjugate for ADC that can be used for the synthesis of ADCs. The resulting BRD4-degrader antibody conjugates exhibit potent and antigen-dependent BRD4 degradation and antiproliferation activities in cell-based experiments.
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PZ671
0 Images製品番号: HY-174876純度: 98.70%PZ671 is a Bcl-xL PROTAC degrader that recruits cereblon, with a DC50 of 0.9 nM in MOLT-4 T-ALL cells. PZ671 induces apoptosis via activation of caspase-3 and cleavage of PARP, and exhibits antitumor activity in T-cell acute lymphoblastic leukemia and small cell lung cancer models. PZ671 can be used for the research of T-cell acute lymphoblastic leukemia and small cell lung cancer.
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BD-9136
0 ImagesBD-9136 is a selective BRD4 PROTAC degrader with a DC50 of 1.2 nM, and exhibits a selectivity of ≥1000-fold over BRD2 and BRD3. BD-9136 preferentially forms a ternary complex with the BD1 domain of BRD4, and downregulates the expression of B7-H4 by disrupting the PR-P300-BRD4 axis. BD-9136 depletes BRD4 protein in tumor tissues, inhibits tumor growth, reduces B7-H4 protein expression, increases CD8+ T cell infiltration, and enhances tumor sensitivity to anti-PD-L1. Degradation of BRD4 by BD-9136 rescues the erythroid differentiation block induced by LSD1 inhibition, and transient administration restores erythroid output while retaining HbF induction. BD-9136 causes no adverse effects in mice at effective doses. BD-9136 can be used in studies related to acute myeloid leukemia, acute lymphoblastic leukemia and breast cancer.
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BTX-6654 formate
0 Images製品番号: HY-161233A純度: 98.85%BTX-6654 formate is a SOS1 PROTAC degrader. BTX-6654 formate induces ubiquitination and degradation of SOS1 via the proteasomal pathway by bridging SOS1 with the E3 ligase CRBN to form a ternary complex, thereby blocking KRAS activation and downregulating the MAPK signaling pathway (pERK/pS6), and ultimately inhibiting tumor growth. BTX-6654 formate can be used in research on various cancers driven by KRAS mutations.
