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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
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Ibrutinib
Cited
T1835936563-96-1
Ibrutinib (PCI-32765) is an irreversible inhibitor of BTK (IC50: 0.5 nM) that selectively blocks B cell activation.
- $36
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Cited(+)-JQ-1 Cited
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
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
T121862143096-93-7
Navitoclax-piperazine (ABT-263-piperazine) is a B-cell lymphoma extra large (BCL-XL) inhibitor.
- $158
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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
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
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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.
- $65
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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).
- $52
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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
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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
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
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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].
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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
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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].
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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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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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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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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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ITK ligand 1
T203599
ITK ligand 1 is a PROTAC target protein ligand (Ligands for Target Protein for PROTACS) that is used in the synthesis of PROTACs.
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SMARCA2 ligand-11
T2036153033592-44-5
SMARCA2 ligand-11 is a ligand for SMARCA2 and can be utilized as a target protein ligand in the synthesis of the PROTAC SMARCA2 degrader-32.
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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.
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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.
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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.
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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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SMARCA2 ligand-12
T2033272755762-94-6
SMARCA2 ligand-12 is a ligand for the target protein in PROTAC (Ligand for Target Protein forPROTAC), used in the synthesis of the PROTAC SMARCA2 degrader-25.
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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.
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Estrone-N-O-C1-amido
T17940138219-84-8
Estrone-N-O-C1-amido (ERα ligand 1) is an estrogen ligand derivative of Estrone that specifically binds to estrogen receptor α (ERα). With a linker, it complexes with the cIAP1 ligand Bestatin, forming SNIPER[1].
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Ch55-O-C3-NH2
T18650144298-98-6
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].
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SirReal1-O-propargyl
T186411862237-99-7
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].
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Ipatasertib-NH2
T180531001382-14-4
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].
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CDK ligand for PROTAC hydrochloride
T10734L
CDK ligand for PROTAC hydrochloride is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.
- $311
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STAT3 ligand 5
T203108
STAT3ligand 5 is a STAT3 ligand, serving as a target protein ligand for the synthesis of the PROTAC degrader [SD-436].
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ILB-14
T203810
ILB-14 is primarily used in the design of PROTACs, functioning to specifically bind to cereblon.
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Pomalidomide-PEG5-Alkyne
T203769
Pomalidomide-PEG5-Alkyne serves as a key building block in the synthesis of targeted protein degraders and PROTACs. This compound includes a (CRBN)-recruiting ligand and a PEGylated crosslinker that features a pendant alkyne, which facilitates click chemistry reactions with an azide on the target ligand.
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c-Myc ligand 1
T2036201942834-87-8
c-Mycligand 1 is a c-Myc inhibitor and functions as a ligand for target proteins in PROTAC (Proteolysis Targeting Chimeras). It is utilized in the synthesis of PROTAC c-Myc inhibitor 7.
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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.
Inquiry
AP1867-2-(carboxymethoxy)
T186112230613-03-1
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].
- $284
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Palbociclib-propargyl
T185152366269-23-8
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].
- $83
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HG-7-85-01-Decyclopropane
T18594
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].
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A-1210477-piperazinyl
T191722351218-72-7
A-1210477-piperazinyl is a compound that specifically targets and binds to the protein myeloid cell leukemia 1 (MCL1) [myeloid cell leukemia 1]. This compound is utilized in PROTAC technology, harnessing the ability to selectively degrade target proteins.
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CDK ligand for PROTAC
T10734
CDK ligand for PROTAC is a CDK inhibitor with antitumor activity. It has been used to design PROTAC CDK4/6 degraders.
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I-BET762 carboxylic acid
T130861300019-38-8
I-BET762 carboxylic acid is an inhibitor of BRD4(pIC50 of 5.1).
- $48
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SI-109
T129052429877-30-3
SI-109 is a potent inhibitor of STAT3 SH2 domain (Ki=9 nM),and with antitumor activity.
- $1,645
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CCR7 Ligand 1
T10716681514-83-0
CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. This thiadiazole-dioxide ligand suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM.
- $1,928
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Pomalidomide-pyridine-PEG1-piperazine hydrochloride
T203767
Pomalidomide-pyridine-PEG1-piperazine hydrochloride is a key building block in the synthesis of targeted protein degraders and PROTACs. It features a Cereblon (CRBN)-recruiting ligand, a more rigid linker, and a pendant amine designed to react with a carboxylic acid on the target ligand.
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Thalidomide-Photoswitch3-NH2 hydrochloride
T203799
Thalidomide-Photoswitch3-NH2 hydrochloride is essential in creating PHOTACs, which are PROTACs activated by specific light wavelengths. These compounds become inactive in darkness and switch to an active cis isomer state under 390 nm irradiation, while wavelengths above 450 nm reverse this activation. This compound comprises a CRBN-recruiting ligand, an azobenzene photoswitchable crosslinker, and a pendant amine that interacts with an acid on the target warhead, and is used to synthesize PHOTAC-I-10 and PHOTAC-II-6.
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IRAK4 ligand-12
T2030242573304-97-7
IRAK4 ligand-12 is a target protein ligand for PROTAC (Ligand for Target Protein for PROTAC) and is utilized in the synthesis of KTX-951.
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