Ligand for Target Protein for PROTAC

产品编号	产品名称
T18515	Palbociclib-propargyl	Palbociclib-propargyl, a PROTAC ligand targeting the protein CDK6, connects to the CRBN ligand through a PEG linker to form PROTAC CP-10. CP-10 exhibits a potent DC50 value of 2.1 nM against CDK6[1].
T18641	SirReal1-O-propargyl	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].
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.
T14288	Androstanolone acetate	Androstanolone acetate is a compound that functions as an androgen ligand, specifically targeting the androgen receptor (AR). It binds to the cIAP1 ligand Bestatin through a linker, resulting in the formation of PROTACs[1].
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 binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
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。
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。
T2066	Quizartinib	Quizartinib (AC220) 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。
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。

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Ligand for Target Protein for PROTAC