T19301
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DUPA
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DUPA 是谷氨酸脲,在药物偶联中作为靶向部分,可选择靶向性地将细胞毒性药物递送到前列腺癌细胞。
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T2110
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(+)-JQ-1
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(+)-JQ-1 是一种有效特异性的可逆 BET 溴结构域抑制剂,可激活自噬,抑制BRD4(1/2)的IC50分别为 77 nM 和 33 nM。
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T12186
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Navitoclax-piperazine
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Navitoclax-piperazine 是一种特大型 B 细胞淋巴瘤(BCL-XL)抑制剂。它和 E3 泛素连接酶的 VHL 配体可用来合成 PROTAC DT2216。
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T1835
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Ibrutinib
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Ibrutinib 是一种不可逆的、选择性的Btk抑制剂,IC50=0.5 nM,它是一种 Btk 配体,用于合成一系列 PROTAC 分子,如 P13I。P13I 作用于人 Burkitt’s 淋巴瘤 RAMOS 细胞,浓度为 10 和 100 nM 时,分别降解 73% 和 89% Btk。
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T2066
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Quizartinib
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Quizartinib 是一种具有口服活性的高选择性Ⅱ 型 FLT3酪氨酸激酶抑制剂,可诱导细胞凋亡。它抑制 Wt FLT3 和 突变型 FLT3-ITD 自磷酸化,IC50分别为 4.1 nM 和 1.1 nM。它可通过优化的 linker 与 VHL 配体连接,从而形成 PROTAC Flt3 降解剂。
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T5480
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BI-4464
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BI-4464 是一种高选择性的 ATP 竞争性 PTK2/FAK 抑制剂,IC50=17 nM。它可用于PROTAC 降解剂的 PTK2 配体。
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T13086
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I-BET762 carboxylic acid
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I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1).
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T10879
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CPI-0610 carboxylic acid
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CPI-0610 carboxylic acid is a ligand for target protein for PROTAC. It is a potent bromodomain and extra-terminal (BET) protein inhibitor with the potential in the therapy of multiple myeloma.
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T13915
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PROTAC BRD9-binding moiety 1
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PROTAC BRD9-binding moiety 1 that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
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T18594
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HG-7-85-01-Decyclopropane
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HG-7-85-01-Decyclopropane, the HG-7-85-01 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER [1].
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T13549
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AP1867-3-(aminoethoxy)
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AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.
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T18650
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Ch55-O-C3-NH2
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Ch55-O-C3-NH2 (RAR ligand 1) is a Ch 55-based ligand, which targets RAR. Ch55-O-C3-NH2 (RAR ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER[1].
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T18595
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Dasatinib carbaldehyde
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Dasatinib carbaldehyde 基于 ABL 抑制剂达沙替尼,通过接头与 IAP 配体结合,形成 SNIPER [1]。
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T13848
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SMARCA-BD ligand 1 for Protac
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SMARCA-BD ligand 1 for Protac 能够与 BAF ATPase 亚基 SMARCA2 结合,可用于 PROTAC 技术,用于降解 SMARCA2。
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T18641
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SirReal1-O-propargyl
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SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM. SirReal1-O-propargyl, the SirReal1-based moiety, binds to the cereblon ligand via a linker to form PROTAC to degrade Sirt2[1].
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T18611
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AP1867-2-(carboxymethoxy)
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AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules[1].
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T12551
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PROTAC BRD4 ligand-1
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PROTAC BRD4 ligand-1 是 PROTAC GNE-987 靶向 BRD4 蛋白的配体,也是一种 BET 的抑制剂。
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T13915L
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PROTAC BRD9-binding moiety 1 hydrochloride
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PROTAC BRD9-binding moiety 1 hydrochloride binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
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T14288
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Androstanolone acetate
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Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs[1].
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T12558
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PROTAC BET-binding moiety 2
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PROTAC BET-binding moiety 2 is an BET bromodomain inhibitor.
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