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PROTAC Selection

产品编号 产品名称
T16701 QCA570
T13929 TL13-112 TL13-112 is a selective degrader of ALK-PROTAC and inhibits ALK activity (IC50: 0.14 nM).
T11291 FKBP12 PROTAC dTAG-13
T12555 PROTAC FLT-3 degrader 1 PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD) with an IC50 of 0.6 nM and exhibits anti-proliferative activity.
T13850 PROTAC BET degrader-3 PROTAC BET Degrader-3 is a potent degrader of BET proteins based on the PROTAC (PROteolysis TArgeting Chimera) technology.
T18606 PROTAC ER Degrader-2 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].
T17728 PROTAC CDK9 degrader-2 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].
T12554 PROTAC EED degrader-2 PROTAC EED degrader-2 is a PROTAC targeting EED (pKD of 9.27) and an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.11.
T13561 AT6
T18609 PROTAC ERRα Degrader-2 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].
T13781 MS4077
T18681 SJFα SJFα is a 13-atom linker PROTAC that degrades p38α with a DC50 of 7.16 nM, 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].
T18634 PROTAC MDM2 Degrader-4 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].
T12553 PROTAC EED degrader-1 PROTAC EED degrader-1, a PROTAC targeting EED (pKD = 9.02), is an inhibitor of polycomb repressive complex 2 (PRC2) with a pIC50 of 8.17.
T18610 PROTAC FKBP Degrader-3 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].
T15484 HJB97 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)。
T18060 KB02-JQ1 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].
T12798 (S)-GNE-987
T13627 CP-10
T12559 PROTAC BET degrader-2 PROTAC BET degrader-2 is a highly potent degrader of Bromodomain and Extra-Terminal (BET) proteins, with an IC50 of 9.6 nM.
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