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Target Protein Ligand-Linker Conjugates

Ligand-linker conjugates are chemical molecules that a linker molecule linked to the ligand against target proteins or against the E3 ubiquitin ligase. The binding affinities may be altered by additional chemical structures.

SLF
T13888195513-96-3
SLF is a synthetic ligand for FKBP12, which increases Ca2+ efflux and protein synthesis to improve skeletal muscle function, and is used in the study of central nervous system diseases and cancer.
  • $99
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K-Ras ligand-Linker Conjugate 6
T180592378261-89-1
K-Ras ligand-Linker Conjugate 6 is a compound that combines a K-Ras-recruiting fragment ligand and a PROTAC linker to recruit E3 ligase for the synthesis of PROTAC K-Ras Degrader-1.
  • $124
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BMS-1166-n-piperidine-co-n-piperazine dihydrochloride
T40111L2691796-83-3In house
BMS-1166-n-piperidine-co-n-piperazine dihydrochloride, a resorcinol di-Ph ether scaffold-based programmed cell death-1 (PD-1)/programmed cell death ligand 1 (PD-L1) inhibitor, inhibits the PD-1/PD-L1 interaction with an IC50 of 39.2 nM. It contains the target protein PD-1/PD-L1 ligand and PROTAC linker, which can be used to synthesize PROTAC PD-1/PD-L1 degrader-1 and has anticancer activity. Additionally, it serves as a diluent for the preparation of tablets for direct compression.
  • $113
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K-Ras ligand-Linker Conjugate 4
T180572378261-83-5
K-Ras ligand-Linker Conjugate 4 is a chemical compound combining a K-Ras recruiting ligand with a PROTAC linker, responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. It has the potential to be used in synthesizing PROTAC K-Ras Degrader-1, which shows a degradation efficacy of ≥70% in SW1573 cells[1].
  • $75
5 days
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EN884
T2083332189497-60-5
EN884 is a BRD4 degrader that functions through an SKP1 and proteasome-dependent degradation pathway. It is utilized in the synthesis of proteolysis-targeting chimeras (PROTAC).
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10-14 weeks
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ER ligand-9
T2049733026011-20-8
ER ligand-9 is a conjugate of an estrogen receptor (Estrogen Receptor/ERR) ligand and a linker, utilized in the synthesis of PROTACs ERD-1233.
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N-Deshydroxyethyl Dasatinib-C3-NH2
N-Deshydroxyethyl BMS-354825-C3-NH2
T2117191430089-58-9
N-Deshydroxyethyl Dasatinib-C3-NH2 is a target protein ligand-linker conjugate, comprising an LCK ligand and a PROTAC linker, designed to recruit E3 ligase. It is utilized in the synthesis of [PROTACSJ11646].
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10-14 weeks
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FKBP12 Ligand-Linker Conjugate 1
T2054362765059-01-4
FKBP12 Ligand-Linker Conjugate 1 is a complex comprising a target protein ligand for FKBP12 and a linker, which is utilized in the synthesis of the PROTAC degrader MC-25B.
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BRAF ligand-Linker Conjugate 1
T2120723094183-96-4
BRAF ligand-Linker Conjugate 1 is a target protein ligand-linker conjugate used for synthesizing PROTACCST905.
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10-14 weeks
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VUBI1-octanoic acid
T212169
VUBI1-octanoic acid is a conjugate of both the SOS1 ligand and linker, and it is applied in the synthesis of (4S)-PROTAC SOS1 degrader-1.
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Desmorpholinyl Quizartinib-PEG2-COOH
Desmorpholinyl Quizartinib-PEG2-COOH
T398182292116-14-2
Desmorpholinyl Quizartinib-PEG2-COOH is a compound featuring an FLT-3 ligand and a PEG-based PROTAC linker. It is employed in the synthesis of PROTAC FLT-3 degrader 1, which serves as a degrader for the FLT-3 internal tandem duplication (ITD) through PROTAC technology. The degrader exhibits an IC50 of 0.6 nM.
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DDR1 ligand 1-piperidine
T2072853081612-71-4
DDR1ligand 1-piperidine is a conjugate of a target protein ligand and linker, utilized in the synthesis of PROTAC DDR1 degrader-1.
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10-14 weeks
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KRAS G12D ligand-Linker Conjugate 2
T215161
KRAS G12D ligand-Linker Conjugate 2 is a conjugate of the KRAS (G12D) ligand with a linker. This compound is utilized in the synthesis of the PROTAC KRAS (G12D) degrader, ASP-3082.
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OSBP ligand-Linker Conjugate 1
T215153
OSBP ligand-Linker Conjugate 1 is a Target Protein Ligand-Linker Conjugate composed of an OSBP ligand and a PROTAC linker, which can recruit E3 ligase. It is utilized for the synthesis of PROTACOSBP Degrader-1.
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PROTAC BRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu
T2151812973054-19-0
PROTACBRD4 ligand-1-NH-PEG-phenol-PEG-COOtBu is a Target Protein Ligand-Linker Conjugate that comprises a BRD4 ligand and a PROTAC linker. This compound is utilized in the synthesis of PROTACBRD4 Degrader-14.
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ER ligand-14-PEG3-Boc
T217108
ER ligand-14-PEG3-Boc is a conjugate of a target protein ligand and a linker, composed of an estrogen receptor (estrogen receptor) ligand and a corresponding linker. It is used in the synthesis of PROTACs such as ERB-2. ERB-2 shows significant antiproliferative activity against non-small cell lung cancer resistant to Osimertinib.
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SMARCA2 Ligand-Linker Conjugate-4
T2152053033001-29-2
SMARCA2 Ligand-Linker Conjugate-4 is a Target Protein Ligand-Linker Conjugate that consists of a SMARCA2 ligand and a PROTAC linker, enabling the recruitment of E3 ligase. This conjugate is utilized in the synthesis of PROTACSMARCA2 degrader-35.
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MRTX849 ethoxypropanoic acid
T401902561529-98-2
MRTX849 ethoxypropanoic acid is a compound that contains a ligand for KRAS G12C and a PROTAC linker. It is commonly employed in the synthesis of PROTAC LC-2, which is a highly effective and innovative PROTAC. LC-2 has been proven to degrade endogenous KRAS G12C with remarkable potency, exhibiting DC50 values ranging from 0.25 to 0.76 μM.
  • $5,450
10-14 weeks
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Ahx-DM1 TFA
T2082071702356-22-6
Ahx-DM1 (TFA) (compound 2A) is a conjugate of proteins/peptides that can combine with therapeutic, diagnostic, or labeling agents.
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3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid
T2123662230826-10-3
3-Fluoro-desmethyl-cabozantinib-C3-O-C3-PEG-acid is a target protein ligand-linker conjugate combining a c-Met ligand with a PROTAC linker to recruit E3 ligase. It is applicable for synthesizing PROTACs, such as SJF-8240.
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10-14 weeks
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SMARCA2 ligand-12-3-methylazetidine
T203685
SMARCA2 ligand-12-3-methylazetidin is a target protein ligand-linker conjugate that includes a ligand for SMARCA2 and a PROTAC linker, capable of recruiting E3 ligase. It is utilized in the synthesis of PROTAC SMARCA2 degrader-25.
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JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222
T204183
JQ-1 (carboxylic acid)-NH-C2-NH-AMPRO-222 incorporates a BRD4 ligand and a PROTAC linker, and is used in the synthesis of PROTAC BRD4 Degrader-29.
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Ad-JQ1
T2120542497485-14-8
Ad-JQ1 (Compound 16) is a Target Protein Ligand-Linker Conjugate incorporating a BRD4 ligand and a PROTAC linker capable of recruiting E3 ligase. It is utilized in the synthesis of PROTACβ-NF-JQ1.
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10-14 weeks
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HPK1 ligand 3-dimethylph tetrahydropyridine
T211091
HPK1 ligand 3-dimethylph tetrahydropyridine is a Target Protein Ligand-Linker Conjugate. It is utilized in the synthesis of PROTACHPK1 Degrader-4.
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