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PROTACLigand for Target Protein for PROTAC
Ligands for Target Protein for PROTAC connect to the E3 ligase ligand via a linker, forming heterodimeric PROTAC molecules. Ligands for Target Protein for PROTAC recognize and bind to the target protein with high affinity and selectivity, determining the specificity and efficiency of degradation at the target site. Small molecules, peptides, and antibody fragments can all serve as Ligands for Target Protein for PROTAC.
Ibrutinib
Cited
PCI-32765
T1835936563-96-1
Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
- $34
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CitedPROTAC 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
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(+)-JQ-1 Cited
JQ1
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
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CitedQuizartinib Cited
AC220
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
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CitedNavitoclax-piperazine
ABT-263-piperazine
T121862143096-93-7
Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor.
- $67
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SLF-amido-C2-COOH
PROTAC FKBP12-binding moiety 1
T139141092369-24-8
SLF-amido-C2-COOH (ZZY01-083) is an FKBP ligand with potential antimicrobial activity for the synthesis of PROTAC.
- $48
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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
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DUPA
N,N''-Carbonylbis[L-glutamic acid], (2S,2'S)-2,2'-Carbonylbis(Azanediyl)Dipentanedioic Acid
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.
- $35
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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.
- $99
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Dasatinib carbaldehyde
PROTAC ABL binding moiety 4, BMS-354825 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
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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).
- $31
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Mc-MMAD
T183111401963-15-2
Mc-MMAD is monomethyl auristatin D (MMAD) modified with the protective group maleimidocaproyl (Mc). MMAD is a potent tubulin microtubule inhibitor that suppresses cancer cell proliferation and is commonly employed as a toxic payload in ADC synthesis.
ADC CytotoxinDrug-Linker Conjugates for ADCLigands for Target Protein for PROTACMicrotubule Associated
- $98
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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
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
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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BRD9 ligand-7
T203041
BRD9 ligand-7 acts as the target protein ligand for PROTAC (Ligand for Target Protein for PROTAC) and is utilized in the synthesis of BRD9 Degrader-1.
- Inquiry Price
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KDM4 ligand-1
T206819
KDM4ligand-1 is a ligand targeting the protein (histone lysine demethylase KDM4) in PROTACs. It can be utilized for the synthesis of PROTACs.
- Inquiry Price
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BCL6 ligand-3
T206439
BCL6ligand-3 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACs). It serves as an active control for the target protein ligand BMS-986458.
- 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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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
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PROTAC BRD9-binding moiety 1 hydrochloride
PROTAC BRD9-binding moiety 1 hydrochloride (2097512-23-5 free base)
T13915L
PROTAC BRD9-binding moiety 1 hydrochloride inhibits BRD9 activity by binding to BRD9, utilizing the PROTAC (Proteolysis Targeting Chimera) mechanism.
- $373
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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
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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
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