Ligand for Target Protein for PROTAC

BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC.

AP1867-2-(carboxymethoxy), the AP1867 (a synthetic FKBP12F36V-directed ligand) based moiety, binds to CRBN ligand via a linker to form dTAG molecules.

DUPA, belongs to a class of glutamate ureas, is used as the targeting moiety in drug conjugate to selectively deliver cytotoxic drugs to prostate cancer cells.

Dasatinib carbaldehyde (BMS-354825 carbaldehyde), the Dasatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER .

GNF5-amido-Me, the GNF5 (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.

Imatinib carbaldehyde (CGP-57148B carbaldehyde), the Imatinib (ABL inhibitor) based moiety, binds to IAP ligand via a linker to form SNIPER.

Androstanolone acetate is an androgen ligand, which targets androgen receptor (AR). Androstanolone acetate binds to cIAP1 ligand Bestatin via a linker to form PROTACs.

Estrone-N-O-C1-amido (ERα ligand 1) is an Estrone-based estrogen ligand, which targets estrogen receptor α (ERα). Estrone-N-O-C1-amido (ERα ligand 1) binds to cIAP1 ligand Bestatin via a linker to form SNIPER.

ATRA-hydroxyimino (CRABP-II ligand 1), the Retinoic acid (ATRA)-based moiety, binds to cIAP1 ligand (Bestatin) via a linker to form SNIPER to degrade CRABP-II in IMR-32 cells.

SirReal1-O-propargyl is a selective and highly potent Sirtuin 2 (Sirt2) inhibitor, with an IC50 of 2.4 μM.

SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) is a synthetic ligand for FKBP (SLF). SLF-amido-C2-COOH (PROTAC FKBP12-binding moiety 1) can be used in the synthesis of PROTACs.

PROTAC BET-binding moiety 1 is a key intermediate for the synthesis of high-affinity BET inhibitors.

N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825), the Dasatinib-based moiety, binds to IAP ligand via a linker to form SNIPER to degrade ABL.

PROTAC BRD9-binding moiety 1 is a compound that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.

I-BET762 carboxylic acid (Molibresib carboxylic acid) is an I-BET762-based warhead ligand for conjugation reactions of PROTAC targeting on BET. I-BET762 carboxylic acid (Molibresib carboxylic acid) is a BRD4 inhibitor with a pIC50 of 5.1.

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.

SMARCA-BD ligand 1 for Protac is a compound that binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.

PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain.

Apcin-A, an Apcin derivative, is an anaphase-promoting complex (APC) inhibitor.