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PROTACLigand 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.
PROTAC BRD4 ligand-1
T125512313230-51-0In house
PROTAC BRD4 ligand-1, a component of Protac GNE-987, is a ligand for BRD4 and acts as an inhibitor of BET.
- $125
Size
QTY
Ibrutinib
T1835936563-96-1
Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
- $36
Size
QTY
(+)-JQ-1
T21101268524-70-4
(+)-JQ-1 (JQ1) is a specific, reversible BET bromine domain inhibitor that targets BRD4 (1 2) with IC50 values of 77 33 nM. (+)-JQ-1 induces cell autophagy and inhibits cell proliferation.
- $30
Size
QTY
Quizartinib
T2066950769-58-1
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.
- $53
Size
QTY
Navitoclax-piperazine
T121862143096-93-7
Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor.
- $112
Size
QTY
SLF-amido-C2-COOH
T139141092369-24-8
SLF-amido-C2-COOH (ZZY01-083) is an FKBP ligand with potential antimicrobial activity for the synthesis of PROTAC.
- $48
Size
QTY
SMARCA-BD ligand 1 for Protac
T138481997319-92-2In house
SMARCA-BD ligand 1 for Protac is a compound that binds to SMARCA2, the BAF ATPase subunit, utilizing Protac technology to degrade SMARCA2.
- $61
Size
QTY
DUPA
T19301302941-52-2
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.
- $37
Size
QTY
PD0325901-O-C2-dioxolane
T402172581116-22-3
The main body of PD0325901-O-C2-dioxolane is PD0325901, which is a typical non-ATP-competitive MEK1 2 (mitogen-activated protein kinase) inhibitor occupying a variant-binding pocket near the ATP-binding site, with anticancer effects of decreasing ERK phosphorylation and inhibiting cell proliferation.
- $112
Size
QTY
BI-4464
T54801227948-02-8
BI-4464, a highly selective ATP-competitive inhibitor of PTK2 FAK, exhibits an IC50 of 17 nM and serves as a PTK2 ligand for PROTAC (Proteolysis Targeting Chimera).
- $52
Size
QTY
Dasatinib carbaldehyde
T185952112837-79-1
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].
- $30
Size
QTY
AP1867-3-(aminoethoxy)
T135492127390-15-0In house
AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.
Inquiry
Androgen receptor antagonist 1
T103201338812-36-4In house
Androgen receptor antagonist 1, an orally available full androgen receptor antagonist (IC50: 59 nM), is utilized in the synthesis of PROTAC AR degraders, achieving 24% and 47% AR protein degradation in LNCaP cells at concentrations of 1 μM and 10 μM, respectively.
- $1,520
Size
QTY
Imatinib carbaldehyde
T185921436868-85-7
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].
- Inquiry Price
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PROTAC BRD9-binding moiety 1 hydrochloride
T13915L
PROTAC BRD9-binding moiety 1 hydrochloride inhibits BRD9 activity by binding to BRD9, utilizing the PROTAC (Proteolysis Targeting Chimera) mechanism.
- $373
Size
QTY
GNF5-amido-Me
T18593778277-37-5
GNF5-amido-Me, the moiety based on GNF5 (ABL inhibitor),binds through a linker to the IAP ligand forming SNIPER[1].
- Inquiry Price
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CCW16-PEG2-butyl-BocNH
T203751
CCW16-C9-BocNH is composed of an RING finger protein 4 (RNF4)-recruiting ligand, includes a linker with both hydrophobic and hydrophilic elements, and features a pendant amine that reacts with a carboxylic acid on the target ligand. It is crucial for synthesizing protein degraders used in targeted protein degradation and PROTAC research.
- Inquiry Price
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CCW16-C9-BocNH
T203750
CCW16-C9-BocNH is an essential key component in the synthesis of targeted protein degraders and PROTACs.
- Inquiry Price
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PAG 4'-piperazine-4-methylpiperidine
T203766
'PAG 4'-piperazine-4-methylpiperidine is a specialized cereblon ligand employed in PROTAC research and development. It includes an E3 ligase ligand and a terminal piperidine, allowing for further chemical modifications to produce Protein Degraders with rigid linkers. This compound is part of a suite of functionalized tool molecules used in PROTAC R&D.
- Inquiry Price
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Apcin-A
T103451683617-62-0
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.
- $169
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QTY
BET-IN-6
T105222570470-39-0
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.
- $1,520
Size
QTY
CDK9-IN-11
T107432748368-15-0
CDK9-IN-11 is a potent CDK9 inhibitor and serves as the ligand for the PROTAC CDK9 Degrader-1 [1].
- $1,520
Size
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FN-1501-propionic acid
T136962408642-48-6
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.
- $1,520
Size
QTY
H117
T203027
H117 is a PROTAC target protein ligand that can be used in the synthesis of PROTAC HP211206. It competitively binds to and inhibits the main protease (Mpro) of SARS-CoV-2, with an IC50 of 151.3 nM.
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