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T13929
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TL13-112
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TL13-112 is a selective degrader of ALK-PROTAC and inhibits ALK activity (IC50: 0.14 nM).
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T11291
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FKBP12 PROTAC dTAG-13
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FKBP12 PROTAC dTAG-13 (dTAG-13) is a degrader of FKBP12F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 (dTAG-13) also is a selective degrader of BET bromodomain transcriptional co-activator BRD4 by bridging BET bromodomains to an E3 ubiquitin ligase CRBN. FKBP12 PROTAC dTAG-13 (dTAG-13) is a PROTAC-based heterobifunctional degrader.
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T12555
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PROTAC FLT-3 degrader 1
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PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.
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T13850
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PROTAC BET degrader-3
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PROTAC BET Degrader-3 is a potent degrader OF BET based on PROTAC.
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T18606
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PROTAC ER Degrader-2
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PROTAC ER Degrader-2 serves as a synthesis intermediate for the production of PAC, a compound that incorporates the ADCs linker and PROTACs, which are subsequently conjugated to an antibody. PAC, exhibits a greater capability to degrade estrogen receptor-alpha (ERα) compared to PROTAC (without the presence of an antibody)[1].
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T17728
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PROTAC CDK9 degrader-2
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PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC[1].
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T12554
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PROTAC EED degrader-2
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PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27),is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.11.
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T17297
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ZXH-3-26
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ZXH-3-26 is a selective degrader of the PROTAC BRD4 (DC50/5h: ~ 5 nM).
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T13561
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AT6
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AT6 is a PROTAC AT1 analog which is a highly selective bromodomain (Brd4) degrader.
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T18609
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PROTAC ERRα Degrader-2
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PROTAC ERRα Degrader-2 is a compound consisting of an MDM2 ligand binding group, a linker, and an estrogen-related receptor alpha (ERRα) binding group. This compound is designed to specifically degrade estrogen-related receptor alpha (ERRα), acting as an ERRα degrader[1].
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T13781
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MS4077
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MS4077 is an degrader of anaplastic lymphoma kinase (ALK) PROTAC(Kd of 37 nM for binding affinity to ALK).
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T18681
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SJFα
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SJFα is a 13-atom linker PROTAC. SJFα degrades p38α with a DC50 of 7.16 nM, but is far less effective at degrading p38δ (DC50=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 μM[1].
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T18634
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PROTAC MDM2 Degrader-4
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PROTAC MDM2 Degrader-4 is a compound designed using PROTAC technology to degrade MDM2. It combines a powerful MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].
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T12553
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PROTAC EED degrader-1
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PROTAC EED degrader-1 is a PROTAC targeting EED (pKD = 9.02), is a inhibitor of polycomb repressive complex 2 (PRC2) with pIC50 of 8.17.
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T18610
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PROTAC FKBP Degrader-3
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PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an VHL binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader[1].
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T15484
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HJB97
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HJB97 可用于开发设计 PROTAC BET 的降解剂，具有抗肿瘤活性。HJB97 是高亲和力的 BET 抑制剂，Ki 值分别为 0.9 nM (BRD2 BD1)，0.27 nM (BRD2 BD2)，0.18 nM (BRD3 BD1)，0.21 nM (BRD3 BD2)，0.5 nM (BRD4 BD1)，1.0 nM (BRD4 BD2)。
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T18060
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KB02-JQ1
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KB02-JQ1 is a potent and specific proteolysis targeting chimera (PROTAC) that specifically degrades BRD4, acting as a molecular glue. It does not degrade BRD2 or BRD3. The mechanism of action involves covalent modification of the E3 ligase DCAF16, thereby promoting BRD4 degradation. Importantly, KB02-JQ1 demonstrates enhanced stability and durability in facilitating protein degradation within biological systems. The compound forms a complex with the ubiquitin E3 ligase ligand KB02 through a linker, resulting in the formation of KB02-JQ1[1].
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T12798
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(S)-GNE-987
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(S)-GNE-987 binds to the BRD4 BD1(IC50=4 nM) and BD2 (3.9 nM) bromodomains and can be used to design PROTAC-Antibody Conjugate (PAC).
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T13627
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CP-10
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CP-10 is a PROTAC with highly selective and remarkable CDK6 degradation (DC50: 2.1 nM). It inhibits the proliferation of several hematopoietic cancer cells including multiple myeloma and can degrade mutated and overexpressed CDK6.
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T12559
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PROTAC BET degrader-2
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PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins (IC50 of 9.6 nM ).
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