Ligand for Target Protein for PROTAC

(+)-JQ-1 (JQ1) is a BET bromine domain inhibitor that inhibits BRD4 (1 2) (IC50=77 33 nM) with specificity and reversibility. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.

Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.

Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.

SMARCA-BD ligand 1 for Protac is a compound capable of binding to SMARCA2, the BAF ATPase subunit, based on the Protac technology for degrading SMARCA2

AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.

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.

PROTAC BRD4 ligand-1 is a ligand for PROTAC GNE-987 targeting the BRD4 protein and is an inhibitor of BET.

CDK ligand for PROTAC hydrochloride is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.

Ipatasertib-NH2 (GDC-0068-NH2;RG7440-NH2) is a ligand for target protein AKT for PROTAC, binds to lenalidomide, a ligand of ubiquitin E3 ligase cereblon (CRBN), via a ten-hydrocarbon linker to form INY-03-041 to degrade AKT[1].

SirReal1-O-propargyl, a moiety based on SirReal1, is a selective and highly potent inhibitor of Sirtuin 2 (Sirt2), demonstrating an IC50 of 2.4 μM. It operates by binding to the cereblon ligand through a linker, facilitating the formation of PROTAC for the degradation of Sirt2[1].

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].

SI-109 is a potent inhibitor of STAT3 SH2 domain (Ki=9 nM),and with antitumor activity.

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].

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].

PROTAC Her3-binding moiety 1 is a Her3 Ligand for PROTAC.

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].

CDK9-IN-11 is a potent CDK9 inhibitor that is the ligand for the PROTAC CDK9 Degrader-1 [1].

BET-IN-6, a ligand with potent and high affinity for inhibiting BRD2/BRD4, plays a crucial role in the synthesis of PROTAC BRD2/BRD4 degrader-1 [1], targeting the protein BRD2/4.

PROTAC BRD9-binding moiety 1 hydrochloride binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.

GNF5-amido-Me, the moiety based on GNF5 (ABL inhibitor),binds through a linker to the IAP ligand forming SNIPER[1].

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.

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.

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].

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].

I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1).

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.

CDK ligand for PROTAC is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.

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

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].

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

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

DUPA (N,N''-Carbonylbis[L-glutamic acid]) is used as the targeting moiety to actively deliver DTX for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.

SLF-amido-C2-COOH is a synthetic ligand for FKBP (SLF), and can be used in the synthesis of PROTACs.

Dasatinib carbaldehyde (PROTAC ABL binding moiety 4) is based on Dasatinib which is an ABL inhibitor, binds to the IAP ligand via a linker, and forms SNIPER [1].

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].

MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein). MAK683-CH2CH2COOH and a VHL ligand for the E3 ubiquitin ligase have been used to design EED-Targeted PROTAC which are EED degrader-1 and PROTAC EED degrader-2 [1].

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].

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].

Navitoclax-piperazine (ABT-263-piperazine) is an inhibitor of B-cell lymphoma extra large (BCL-XL).

PROTAC IRAK4 ligand-1 is a synthetic ligand for interleukin-1 receptor-associated kinase 4.

SLF is a synthetic ligand for FK506-binding protein (FKBP)( with an affinity of 3.1 μM for FKBP51 and an IC50 of 0.22 μM for FKBP12). SLF can be used in the synthesis of PROTAC.

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

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

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].

N-Deshydroxyethyl Dasatinib (N-Deshydroxyethyl BMS-354825) is a metabolite of Dasatinib, a dasatinib-based molecule that degrades ABL by binding to the IAP ligand via a linker to form SNIPER.N-Deshydroxyethyl Dasatinib is used in the study of cancer and immune diseases.