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Linker

The length and composition of the linker play critical roles in the physicochemical properties and bioactivity of PROTACs. While linker design has historically received limited attention, the PROTAC field is evolving rapidly and undergoing an important shift from synthetically tractable alkyl and polyethylene glycol to more sophisticated functional linkers. Equally important, linker-mediated binding cooperativity also represents a potential source of affinity for the POI for PROTACs based on weak affinity warheads. However, the current consensus is that the linker composition, and particularly its length and attachment point to the anchor/warhead, must be optimized for each ligand pair.

Ac4ManNAz
T14093361154-30-5In house
Ac4ManNAz is an azide-containing metabolic glycoprotein labeling reagent that can selectively modify proteins and can be used for cell labeling, tracking, and proteomic analysis.
  • $32
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Deruxtecan
T150981599440-13-7
Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and a maleimide-GGFG peptide linker used in the synthesis of DS-8201 and U3-1402.
  • $139
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DOTA-​NHS-​ester
T17842170908-81-3
DOTA-NHS-ester is a linker for affibody molecules with applications in small animal PET, SPECT, and CT. It can be used to label radiotherapeutic agents or imaging probes for tumor detection.
  • $41
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DSG Crosslinker
T1517179642-50-5
DSG Crosslinker, a cleavable ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs).
  • $39
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DTSSP Crosslinker
T1517981069-02-5
DTSSP Crosslinker, a cleavable ADC linker, is utilized in the synthesis of antibody-drug conjugates (ADCs).
  • $37
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N3-C3-NHS ester
T18466943858-70-6
N3-C3-NHS ester is a noncleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
  • $50
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TCO-NHS ester
T170141191901-33-3
TCO-NHS ester is a alkyl ether-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
  • $52
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Alkynyl Palmitic Acid
T1418599208-90-9
Alkynyl Palmitic Acid is an alkyl chain-based PROTAC linker that can be used in PROTAC synthesis.
  • $122
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Mc-Val-Cit-PAB-Cl
T183211639351-92-0
Mc-Val-Cit-PAB-Cl, a cleavable ADC linker, is utilized in the conjugation of MMAE and antibodies to produce compounds such as antibody-MC-vc-MMAE (e.g., anti-CD22-MC-VC-PABC-MMAE), which demonstrate cytotoxicity with IC50s of 3.3 and 0.95 nM against BJAB and WSU cell lines, respectively.
  • $119
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Biotin-PEG2-CH2CH2N3
T17566945633-30-7
Biotin-PEG2-CH2CH2N3 is a PEG-based PROTAC linker suitable for use in PROTAC synthesis.
  • $30
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Sulfo-SMCC sodium
T1872892921-24-9
Sulfo-SMCC sodium, a widely utilized non-cleavable, hetero-bifunctional crosslinker for antibody-drug conjugates (ADCs), features both N-hydroxysuccinimide (NHS) ester and maleimide groups. These functionalities enable it to specifically react with primary amines and sulfhydryl groups, respectively.
  • $41
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Biotin-PEG3-azide
T14591875770-34-6
Biotin-PEG3-azide is a PEG-based PROTAC linker utilized in the synthesis of PROTACs.
  • $39
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BS3 Crosslinker disodium
T14833L127634-19-9
BS3 Crosslinker disodium, a non-cleavable ADC linker, is employed in the synthesis of antibody-drug conjugates (ADCs).
  • $41
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DBCO-PEG4-NHS ester
T150731427004-19-0
DBCO-PEG4-NHS ester is a PEG-based PROTAC linker utilized in PROTAC synthesis[1].
  • $59
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DSS Crosslinker
T1517668528-80-3
DSS Crosslinker is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). It is a homobifunctional crosslinker that is cell membrane permeable, with amine-reactive NHS esters at both ends of an 8-atom [11.4 angstrom] spacer arm for conjugating proteins, including intracellular proteins.
  • $41
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DiZPK
T151361337883-32-5
DiZPK is an analog of pyrrolysine and acts as a photocrosslinker.
  • $108
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Biotin-PEG2-C2-iodoacetamide
T17565292843-75-5
Biotin-PEG2-C2-iodoacetamide (Biotin-PEG2-iodoacetamide) is a PEG-based PROTAC linker that can be used in PROTAC synthesis.
  • $38
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Biotin-PEG4-azide
T175831309649-57-7
Biotin-PEG4-azide, a biotin-labeled, PEG-based PROTAC linker, is utilized in PROTAC synthesis.
  • $66
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SMCC-DM1
T168991228105-51-8
SMCC-DM1 is a drug-coupler coupler consisting of a potent microtubule disrupter, DM1, and a coupler, SMCC, for the preparation of antibody-drug couplers.
  • $97
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m-PEG8-Ms
T159351059588-19-0
m-PEG8-Ms is a PROTAC linker belonging to the PEG class and can be used to synthesize PROTAC compounds.
  • $40
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DBCO-mPEG (MW 5kDa)
T17753
DBCO-mPEG (MW 5kDa) is a PEG-based linker utilized in PROTACs to connect two essential ligands, facilitating selective protein degradation through the ubiquitin-proteasome system.
  • $39
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DBCO-amine
T150581255942-06-3
DBCO-amine is a cleavable ADC linker utilized in the synthesis of antibody-drug conjugates (ADCs)[1].
  • $32
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DSPE-PEG-Biotin (MW 2000)
T17850385437-57-0
DSPE-PEG-Biotin (MW 2000) is a PEG-based PROTAC linker for PROTAC synthesis.
  • $30
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L-Homopropargylglycine
T1569498891-36-2
L-Homopropargylglycine is an alkyl chain-based PROTAC linker utilized in the synthesis of PROTACs[1].
  • $29
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Biotin-PEG4-alkyne
T145981458576-00-5
Biotin-PEG4-alkyne is a biotin-labeled, polyethylene glycol-based (PEG-based) PROTAC linker utilized in PROTAC synthesis.
  • $30
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Aminooxy-PEG3-azide
T142641306615-51-9
Aminooxy-PEG3-azide is an ADC linker belonging to the class of PEGs, as well as three-unit PEGs, which can be used for the synthesis of antibody-coupled reactive molecules (ADCs).
  • $37
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17-ODYA
T1418634450-18-5
Squalane is a lipid found in some fish oils (especially shark liver oil) and some vegetable oils. It has anticancer and antioxidant properties and is used as a skin moisturizer and emollient.
  • $45
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m-PEG9-CH2COOH
T18226405518-55-0
m-PEG9-CH2COOH is a PEG-based PROTAC linker utilized in the synthesis of PROTACs.
  • $30
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(S,R,S)-AHPC-PEG4-N3
T179211797406-81-5
(S,R,S)-AHPC-PEG4-N3 (VHL Ligand-Linker Conjugates 5) is a synthesized ligand-linker for E3 ligase-based systems, comprising the (S,R,S)-AHPC VHL ligand and a 4-unit PEG linker, commonly used in PROTAC technology.
  • $30
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Amino-PEG12-acid
T174051415408-69-3
Amino-PEG12-acid, a PEG-based PROTAC linker, is utilized in PROTAC synthesis.
  • $61
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Cbz-NH-PEG12-C2-acid
T177191334177-88-6
Cbz-NH-PEG12-C2-acid is a PEG-based linker for PROTACs, facilitating the connection of two essential ligands to form PROTAC molecules, thereby enabling selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
  • $30
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Propargyl-C1-NHS ester
T18560132178-37-1
Propargyl-C1-NHS ester (4-Pentynoic Acid Succinimidyl Ester) is a nonclaevable linker used for antibody-drug-conjugation (ADC).
  • $30
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DSP Crosslinker
T1517557757-57-0
DSP Crosslinker, used in antibody-drug conjugates (ADCs) synthesis, is a cleavable ADC linker[1].
  • $30
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Biotin-PEG12-NHS ester
T175611934296-88-4
Biotin-PEG12-NHS ester is a PEG-based PROTAC linker used in the synthesis of PROTACs.
  • $40
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m-PEG9-SH
T18229651042-84-1
m-PEG9-SH, a PEG-based linker for PROTACs, facilitates the formation of PROTAC molecules by joining two essential ligands and enables selective protein degradation through the ubiquitin-proteasome system within cells.
  • $29
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N3-C5-NHS ester
T18468866363-70-4
N3-C5-NHS ester, a noncleavable ADC linker, can be used in the synthesis of antibody-drug conjugates (ADCs).
  • $53
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DBCO-S-S-PEG3-biotin
T150761430408-09-5
DBCO-S-S-PEG3-biotin is a cleavable reagent for the introduction of a biotin moiety to azide-containing biomolecules using copper-free Click Chemistry. The disulfide bond in this linker can be cleaved with reducing agents such as DTT, BME, and TCEP to remove the biotin label. PEG linkers can also be used in the synthesis of PROTACs.
  • $36
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Azido-PEG4-azide
T39268182760-73-2
Azido-PEG4-azide is a PEG-based PROTAC linker used for synthesizing PROTACs.
  • $50
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5-(Biotinamido)pentylamine
T38543115416-38-1
5-(Biotinamido)pentylamine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs.
  • $43
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MC-Gly-Gly-Phe
T183081599440-15-9
MC-Gly-Gly-Phe is a cleavable linker used for antibody-drug conjugates (ADC).
  • $29
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Val-Cit-PAB-MMAE
T18867644981-35-1
Val-Cit-PAB-MMAE is a drug-linker conjugate for ADC. Val-Cit-PAB-MMAE contains the ADCs linker (peptide Val-Cit-PAB) and a potent tubulin inhibitor MMAE . MMAE a potent mitotic inhibitor by inhibiting tubulin polymerization[1].
  • $50
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Mc-MMAE
T18312863971-24-8
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) is a drug-linker conjugate for ADC. Mc-MMAE is a maleimidocaproyl-conjugated monomethyl auristatin E, which is a potent tubulin inhibitor.
  • $163
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Pomalidomide-PEG4-C2-NH2 hydrochloride
T400322357105-92-9
Pomalidomide-PEG4-C2-NH2 hydrochloride is a PEG-based PROTAC linker used for synthesizing PROTACs[1].
  • $31
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(S,R,S)-AHPC-PEG3-N3
T179091797406-80-4
(S, R, S)-AHPC-PEG3-N3 (VHL Ligand-Linker Conjugates 8) is a synthesized E3 ligase ligand-linker conjugate. (S, R, S)-AHPC-PEG3-N3 incorporates the (S, R, S)-AHPC based VHL ligand and 3-unit PEG linker used in PROTAC technology.
  • $37
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Pomalidomide-PEG4-C2-NH2
T179162225940-52-1
Pomalidomide-PEG4-C2-NH2 (E3 Ligase Ligand-Linker Conjugates 22) is a synthesized E3 ligase ligand-linker conjugate incorporating the Pomalidomide-based cereblon ligand and 4-unit PEG linker.
  • $30
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MC-Gly-Gly-Phe-Gly
T86672413428-36-9
MC-Gly-Gly-Phe-Gly (DSN28369) is a heterobifunctional linker, and useful to make antibody drug conjuate (ADC).
  • $30
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L-Azidohomoalanine hydrochloride
T41090942518-29-8
L-Azidohomoalanine hydrochloride (H-L-Aha-OH hydrochloride) is an alkyl chain-based PROTAC linker.
  • $30
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Mal-amido-PEG8-NHS ester
T15962756525-93-6
Mal-amido-PEG8-NHS ester, a PEG-based PROTAC linker, is utilized in the synthesis of PROTACs.
  • $33
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