Ligand for Target Protein for PROTAC

Targeted protein degradation (TPD) is attracting substantial interest owing to its potential to therapeutically modulate proteins that have proved difficult to target with conventional small molecules. A major class of molecules that may enable such proteins to be modulated through TPD are known as proteolysis-targeting chimera (PROTAC) protein degraders. These are heterobifunctional small molecules consisting of two ligands joined by a linker: one ligand recruits and binds a protein of interest (POI) while the other recruits and binds an E3 ubiquitin ligase.

产品编号	产品名称
T18599	PROTAC BRD4-binding moiety 1	PROTAC BRD4-binding moiety 1 is a BRD4 ligand that binds to the cereblon ligand through a linker, enabling the formation of a PROTAC complex. This complex efficiently degrades BRD4[1].
T19172	A-1210477-piperazinyl	A-1210477-piperazinyl is a compound that specifically targets and binds to the protein myeloid cell leukemia 1 (MCL1). This compound is utilized in PROTAC technology, which harnesses the ability to selectively degrade target proteins.
T10734	CDK ligand for PROTAC	CDK ligand for PROTAC is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.
T13549	AP1867-3-(aminoethoxy)	AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.
T13915L	PROTAC BRD9-binding moiety 1 hydrochloride	PROTAC BRD9-binding moiety 1 hydrochloride inhibits BRD9 activity by binding to BRD9, utilizing the PROTAC (Proteolysis Targeting Chimera) mechanism.
T10716	CCR7 Ligand 1	CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM
T17733	ATRA-hydroxyimino	ATRA-hydroxyimino, also known as CRABP-II ligand 1, is a chemical compound derived from Retinoic acid (ATRA). This compound binds to the cIAP1 ligand, specifically Bestatin, through a linker, resulting in the formation of a complex called SNIPER. The purpose of this complex is to degrade CRABP-II within IMR-32 cells[1].
T18593	GNF5-amido-Me	GNF5-amido-Me, the moiety based on GNF5 (ABL inhibitor),binds through a linker to the IAP ligand forming SNIPER[1].
T13765	MAK683-CH2CH2COOH	MAK683-CH2CH2COOH 与 EED (胚胎外胚层发育蛋白) 结合。基于MAK683-CH2CH2COOH 和 E3 泛素连接酶的 VHL 配体，设计了靶向EED 的PROTACs， PROTAC EED degrader-1 和 PROTAC EED degrader-2 。
T17931	EED226-COOH	EED226-COOH, derived from EED226, serves as a ligand targeting the EED protein for PROTAC applications. It attaches to a VHL ligand through a linker, culminating in the formation of UNC6852, which specifically degrades PRC2[1].
T18594	HG-7-85-01-Decyclopropane	Decyclopropane, also known as HG-7-85-01, is a chemical compound with ABL inhibitor properties. It binds to the IAP ligand through a linker, resulting in the formation of SNIPER [1].
T13696	FN-1501-propionic acid	FN-1501-propionic acid, a CDK2/9 ligand, in conjunction with a CRBN ligand, has been utilized in the design of a PROTAC CDK2/9 degrader.
T1835	Ibrutinib	Ibrutinib (PCI-32765) 是一种布鲁顿酪氨酸激酶 (BTK) 抑制剂 (IC50=0.5 nM)，具有不可逆性和选择性。Ibrutinib 可以阻断 BTK 抑制 B 细胞的增殖和存活，具有抗肿瘤活性，可以用于治疗慢性淋巴细胞白血病等。
T19301	DUPA	DUPA (N,N''-Carbonylbis[L-glutamic acid]) 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。
T12551	PROTAC BRD4 ligand-1	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。
T12186	Navitoclax-piperazine	Navitoclax-piperazine (ABT-263-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。
T2110	(+)-JQ-1	(+)-JQ-1 (JQ1) 是一种 BET 溴结构域抑制剂，抑制 BRD4(1/2) (IC50=77/33 nM)，具有特异性和可逆性。(+)-JQ-1 可以诱导细胞自噬，抑制细胞增殖。
T2066	Quizartinib	Quizartinib (AC220) 是一种第二代 Ⅱ 型 FLT3 酪氨酸激酶抑制剂，具有口服活性和高选择性，抑制 FLT3-WT 和 FLT3-ITD 自磷酸化 (IC50=4.1/1.1 nM)。Quizartinib 可以诱导肿瘤细胞凋亡。
T18595	Dasatinib carbaldehyde	Dasatinib carbaldehyde (PROTAC ABL binding moiety 4) 基于 ABL 抑制剂达沙替尼，通过接头与 IAP 配体结合，形成 SNIPER [1]。
T5480	BI-4464	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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Ligand for Target Protein for PROTAC