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
T18601	Desmethyl-QCA276	Desmethyl-QCA276, the QCA276-based moiety, binds to cereblon ligand via a linker to form PROTAC to degrade BET. QCA276 is a BET inhibitor with an IC50 of 10 nM, and with a Ki of 2.3 nM[1].
T18650	Ch55-O-C3-NH2	Ch55-O-C3-NH2, also known as RAR ligand 1, is a ligand derived from the Ch55 compound that specifically targets RAR. Through a linker, Ch55-O-C3-NH2 interacts with cIAP1 ligand Bestatin to form SNIPER[1].
T13843	PROTAC IRAK4 ligand-1	PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4.
T10320	Androgen receptor antagonist 1	Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
T10345	Apcin-A	Apcin-A is an anaphase-promoting complex (APC) inhibitor. It interacts strongly with Cdc20 and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V.
T12558	PROTAC BET-binding moiety 2	PROTAC BET-binding moiety 2 is an BET bromodomain inhibitor.
T12905	SI-109	SI-109 is a potent inhibitor of STAT3 SH2 domain (Ki=9 nM),and with antitumor activity.
T17940	Estrone-N-O-C1-amido	Estrone-N-O-C1-amido (ERα ligand 1) is an estrogen ligand derived from Estrone that specifically binds to estrogen receptor α (ERα). Through a linker, Estrone-N-O-C1-amido (ERα ligand 1) forms a complex with the cIAP1 ligand Bestatin, leading to the creation of SNIPER[1].
T10734L	CDK ligand for PROTAC hydrochloride	CDK ligand for PROTAC hydrochloride is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.
T13841	PROTAC Her3-binding moiety 1	PROTAC Her3-binding moiety 1 is a Her3 Ligand for PROTAC.
T13086	I-BET762 carboxylic acid	I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1).
T12557	PROTAC BET-binding moiety 1	PROTAC BET-binding moiety 1 is a key intermediate in the synthesis of high affinity BET inhibitors
T18053	Ipatasertib-NH2	Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for the target protein AKT used in PROTAC, binding to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 for AKT degradation[1].
T18611	AP1867-2-(carboxymethoxy)	AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG molecules[1].
T13915	PROTAC BRD9-binding moiety 1	PROTAC BRD9-binding moiety 1 that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
T18592	Imatinib carbaldehyde	Imatinib carbaldehyde (also known as CGP-57148B carbaldehyde) is a compound derived from Imatinib, an inhibitor of the ABL protein. Imatinib carbaldehyde binds to the IAP ligand with the assistance of a linker, resulting in the formation of SNIPER[1].
T10743	CDK9-IN-11	CDK9-IN-11 是一种有效的CDK9抑制剂，可作为 PROTAC CDK9 Degrader-1 的配体。
T10522	BET-IN-6	BET-IN-6 是一种有效且高亲和力的BRD2/BRD4抑制剂。BET-IN-6 是靶蛋白 BRD2/4 的配体，可用于合成 PROTAC BRD2/BRD4 degrader-1 。
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].

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Ligand for Target Protein for PROTAC