PROTACs or Proteolysis Targeting Chimeric Molecules are heterobifunctional nanomolecules that theoretically target any protein for ubiquitination and degradation. In terms of the structure, PROTACs consist of one moiety which is recognized by the E3 ligase. This moiety is then chemically and covalently linked to a small molecule or a protein that recognizes the target protein. The trimeric complex formation leads to the transfer of ubiquitins to the target protein.

By removing target proteins directly rather than merely blocking them, PROTACs can provide multiple advantages over small molecule inhibitors, which can require high systemic exposure to achieve sufficient inhibition, often resulting in toxic side effects and eventual drug resistance. PROTAC molecules possess good tissue distribution and the ability to target intracellular proteins, thus can be directly applied to cells or injected into animals without the use of vectors.

Targeted protein degradation using the PROTAC technology is emerging as a novel therapeutic method to address diseases, such as cancer, driven by the aberrant expression of a disease-causing protein. In addition to the use of PROTACs for the treatment of human disease, these molecules provide a chemical genetic approach to “knock down” proteins to study their function. Currently, there are several small molecule inhibitors that have been found to show good biological activity by specifically targeting BET, estrogen receptor (ER), androgen receptor, etc.

References:
[1] Sakamoto KM. Pediatr Res. 2010 May;67(5):505-8.
[2] Neklesa TK, et al. Pharmacol Ther. 2017 Jun;174:138-144.


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Pomalidomide-piperazine

Pomalidomide-piperazine is an active compound that can be used to synthesis the E3 ligand for PROTAC[1].

  • CAS Number: 2154342-57-9
  • MF: C17H18N4O4
  • MW: 342.35
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3,4-Dibromo-Mal-PEG8-t-butyl ester

3,4-Dibromo-Mal-PEG8-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2055198-02-0
  • MF: C27H45Br2NO12
  • MW: 735.45
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

5-(Biotinamido)pentylamine

5-Biotinamidopentylamine is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 115416-38-1
  • MF: C15H28N4O2S
  • MW: 328.47300
  • Catalog: PROTAC Linker
  • Density: 1.131g/cm3
  • Boiling Point: 652ºC at 760mmHg
  • Melting Point: N/A
  • Flash Point: 348.1ºC

Chloroacetamido-C-PEG3-C3-NHBoc

Chloroacetamido-C-PEG3-C3-NHBoc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 934164-55-3
  • MF: C17H33ClN2O6
  • MW: 396.91
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SCO-PEG8-COOH

SCO-PEG8-COOH is a PROTAC linker and belongs to the PEG class. SCO-PEG8-COOH contains SCO and COOH that can be covalently combined with amino groups, respectively. SCO is often used to react with amino acid residues of proteins or peptides, particularly lysine.

  • CAS Number: 2143968-79-8
  • MF: C28H49NO12
  • MW: 591.69
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(Azido-PEG3)-N-Fluorescein-PEG3-acid

N-(Azido-PEG3)-N-Fluorescein-PEG3-acid is a PEG-based PROTAC linker which contains azide, fluorescein and carboxylic acid moieties.

  • CAS Number: 2100306-50-9
  • MF: C38H45N5O13S
  • MW: 811.85
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-6-O-CH3

Pomalidomide-6-O-CH3 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-6-O-CH3 can be connected to the ligand for protein by a linker to form PROTAC[1].

  • CAS Number: 1547163-08-5
  • MF: C14H13N3O5
  • MW: 303.27
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG4-Amido-tri-(carboxyethoxymethyl)-methane

Azido-PEG4-amido-tri-(carboxyethoxymethyl)-methane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1398044-51-3
  • MF: C24H42N4O14
  • MW: 610.61
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

6-Bromohexylphosphonic acid

6-Bromohexylphosphonic acid is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 133345-66-1
  • MF: C6H14BrO3P
  • MW: 245.051
  • Catalog: PROTAC Linker
  • Density: 1.5±0.1 g/cm3
  • Boiling Point: 374.1±44.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 180.0±28.4 °C

Biotin-PEG4-allyl

Biotin-PEG4-allyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1643661-79-3
  • MF: C21H37N3O6S
  • MW: 459.60
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-aminooxy-PEG5-propargyl

Boc-aminooxy-PEG5-propargyl is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2086688-98-2
  • MF: C18H33NO8
  • MW: 391.46
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-N-amido-PEG6-Tos

t-Boc-N-amido-PEG6-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1264015-76-0
  • MF: C24H41NO10S
  • MW: 535.65
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG3-amine

Benzyl-PEG3-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 86770-75-4
  • MF: C13H21NO3
  • MW: 239.31100
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

H-cis-Hyp-OMe hydrochloride

H-cis-Hyp-OMe hydrochloride is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). H-cis-Hyp-OMe hydrochloride is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PR

  • CAS Number: 40126-30-5
  • MF: C6H12ClNO3
  • MW: 181.617
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: 282.3ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 124.5ºC

HS-PEG3-CH2CH2N3

HS-PEG3-CH2CH2N3 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1347750-79-1
  • MF: C8H17N3O3S
  • MW: 235.30400
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC BET Degrader-1

PROTAC BET Degrader-1 is a potent BET degrader based on PROTAC, decreasing BRD2, BRD3, and BRD4 protein levels at low concentration.

  • CAS Number: 2093386-22-0
  • MF: C44H45N11O9
  • MW: 871.9
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG4-sulfonic acid

m-PEG4-sulfonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 787524-78-1
  • MF: C9H20O7S
  • MW: 272.316
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tos-PEG12-Tos

Tos-PEG12-Tos is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1456708-45-4
  • MF: C38H62O17S2
  • MW: 855.019
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 833.3±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 457.8±34.3 °C

Acid-PEG2-C2-Boc

Acid-PEG2-C2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2086688-99-3
  • MF: C12H22O6
  • MW: 262.3
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG24-NHS ester

Mal-PEG24-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2226733-37-3
  • MF: C16H19N3O8
  • MW: 381.34
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Cl-PEG6-acid

Cl-PEG6-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2365309-92-6
  • MF: C14H27ClO8
  • MW: 358.81
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(+)-Biotin-ONP

(+)-Biotin-ONP is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 33755-53-2
  • MF: C16H19N3O5S
  • MW: 365.404
  • Catalog: PROTAC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 642.9±50.0 °C at 760 mmHg
  • Melting Point: 163-165ºC
  • Flash Point: 342.6±30.1 °C

Bromo-PEG3-THP

Bromo-PEG3-THP is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 220568-33-2
  • MF: C11H21BrO4
  • MW: 297.19
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG7-4-nitrophenyl carbonate

m-PEG7-4-nitrophenyl carbonate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 678150-56-6
  • MF: C20H31NO11
  • MW: 461.46
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand 6

Protein degrader 1 TFA is a small molecule ligand for VHL, an E3 ligase which has been targeted in numerous PROTACs.

  • CAS Number: 1631137-51-3
  • MF: C24H31F3N4O5S
  • MW: 544.59
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG5-azide

Benzyl-PEG5-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 86770-72-1
  • MF: C17H27N3O5
  • MW: 353.413
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG3-C-Boc

Azido-PEG3-C-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 172531-36-1
  • MF: C12H23N3O5
  • MW: 289.32800
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

(2R)-2-Azetidinecarboxylic acid

(R)-Azetidine-2-carboxylic acid is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). (R)-Azetidine-2-carboxylic acid is also a alkyl chain-based PROTAC linker that can be

  • CAS Number: 7729-30-8
  • MF: C4H7NO2
  • MW: 101.104
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 242.0±33.0 °C at 760 mmHg
  • Melting Point: 209-211ºC
  • Flash Point: 100.1±25.4 °C

Lenalidomide-4-aminomethyl hydrochloride

Lenalidomide-4-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC[1]

  • CAS Number: 444289-05-8
  • MF: C14H16ClN3O3
  • MW: 309.75
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG6-amine

Azido-PEG6-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Azido-PEG6-amine is also a non-cleavable 6 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 957486-82-7
  • MF: C14H30N4O6
  • MW: 350.41100
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A