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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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(+)-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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CitedIbrutinib 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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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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Quizartinib 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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CitedSMARCA-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.
- $197
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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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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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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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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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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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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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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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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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SI-109
T12905
SI-109 is a potent inhibitor of STAT3 SH2 domain (Ki=9 nM),and with antitumor activity.
- Inquiry Price
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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.
- Inquiry Price
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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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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.
- Inquiry Price
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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.
- $1,870
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Androstanolone acetate
T142881164-91-6
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].
Inquiry
PROTAC BET-binding moiety 2
T12558916493-82-8
PROTAC BET-binding moiety 2 is an inhibitor of the BET bromodomain.
Inquiry
EED226-COOH
T17931
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].
- $183
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MAK683-CH2CH2COOH
T137652639882-68-9
MAK683-CH2CH2COOH binds to EED (embryonic ectoderm development protein) and, together with a VHL ligand for the E3 ubiquitin ligase, has been used to design EED-Targeted PROTACs, specifically EED degrader-1 and PROTAC EED degrader-2 [1].
- $1,517
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ATRA-hydroxyimino
T17733135325-47-2
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].
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Desmethyl-QCA276
T186012126819-55-2
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].
- Inquiry Price
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PROTAC Her3-binding moiety 1
T138411603845-36-8
PROTAC Her3-binding moiety 1 is a Her3 Ligand for PROTAC.
- Inquiry Price
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PROTAC IRAK4 ligand-1
T138432357108-39-3
PROTAC IRAK4 ligand-1 is a synthetic ligand targeting interleukin-1 receptor-associated kinase 4 (IRAK4).
Inquiry
PROTAC BET-binding moiety 1
T125572093387-77-8
PROTAC BET-binding moiety 1 is a crucial intermediate used in synthesizing high-affinity BET inhibitors.
Inquiry
PROTAC BRD9-binding moiety 1
T139152097512-23-5
PROTAC BRD9-binding moiety 1 that binds to BRD9, and used for inhibiting BRD9 activity, based on PROTAC.
- Inquiry Price
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PROTAC BRD4-binding moiety 1
T185992101200-10-4
PROTAC BRD4-binding moiety 1 is a BRD4 ligand that binds to the cereblon ligand via a linker, facilitating the formation of a PROTAC complex which efficiently degrades BRD4[1].
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