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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Acid-C1-PEG5-Boc

Acid-C1-PEG5-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2304558-22-1
  • MF: C17H32O9
  • MW: 380.43
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG-acid

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

  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG27-amine

Amino-PEG27-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2252208-09-4
  • MF: C56H116N2O27
  • MW: 1249.52
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Chloro-PEG2-Boc

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

  • CAS Number: 1442085-43-9
  • MF: C10H19ClO4
  • MW: 238.71
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DBCO-PEG1-NH-Boc

DBCO-PEG1-NH-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2364591-77-3
  • MF: C28H33N3O5
  • MW: 491.58
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Carboxy-PEG5-sulfonic acid

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

  • CAS Number: 1817735-38-8
  • MF: C13H26O10S
  • MW: 374.40
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TCO-PEG4-acid

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

  • CAS Number: 1802913-21-8
  • MF: C20H35NO8
  • MW: 417.494
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 574.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 301.2±30.1 °C

Hydroxy-PEG4-O-Boc

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

  • CAS Number: 1807530-05-7
  • MF: C16H32O8
  • MW: 352.421
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 432.4±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 142.6±20.8 °C

Thalidomide-O-C8-NH2

Thalidomide-O-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].

  • CAS Number: 1957235-91-4
  • MF: C21H27N3O5
  • MW: 401.46
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-Boc-Aminooxy-PEG3-thiol

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

  • CAS Number: 1895922-75-4
  • MF: C13H27NO6S
  • MW: 325.42
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC ERRα Degrader-1

PROTAC ERRalpha Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRalpha Degrader-1 is an estrogen-related receptor alpha (ERRa) degrader[1].

  • CAS Number: 2306388-84-9
  • MF: C54H49Cl2F6N7O8
  • MW: 1108.91
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Carboxy-PEG4-sulfonic acid

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

  • CAS Number: 1817735-25-3
  • MF: C11H22O9S
  • MW: 330.35
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG4-propargyl

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

  • CAS Number: 1262681-30-0
  • MF: C15H21NO6
  • MW: 311.33
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-C4-NH2

Pomalidomide-C4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].

  • CAS Number: 1957236-34-8
  • MF: C17H20N4O4
  • MW: 344.37
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-5-O-C6-NH2 hydrochloride

Thalidomide-5-O-C6-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].

  • CAS Number: 2761398-05-2
  • MF: C19H24ClN3O5
  • MW: 409.86
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG2-alcohol

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

  • CAS Number: 57641-66-4
  • MF: C4H9BrO2
  • MW: 169.01700
  • Catalog: PROTAC Linker
  • Density: 1.514±0.06 g/cm3
  • Boiling Point: 228.9±15.0 °C
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-O-amido-C6-NH2 hydrochloride

Thalidomide-O-amido-C6-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs[1].

  • CAS Number: 2376990-31-5
  • MF: C21H27ClN4O6
  • MW: 466.92
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lipoamido-PEG4-acid

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

  • CAS Number: 1314378-10-3
  • MF: C19H35NO7S2
  • MW: 453.614
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 650.7±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 347.3±31.5 °C

THP-PEG4-Pyrrolidine(N-Boc)-CH2OH

THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a PEG-based PROTAC linker can be used in the synthesis of PROTAC K-Ras Degrader-1 (HY-129523)[1].

  • CAS Number: 2378261-80-2
  • MF: C23H43NO9
  • MW: 477.59
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG4-MS

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

  • CAS Number: 2167807-41-0
  • MF: C9H19BrO6S
  • MW: 335.21
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-PEG3-N'-(propargyl-PEG4)-Cy5

N-PEG3-N'-(propargyl-PEG4)-Cy5 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2107273-06-1
  • MF: C42H57ClN2O7
  • MW: 737.36
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-amido-PEG9-NHS ester

Mal-amido-PEG9-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2575631-92-2
  • MF: C32H51N3O16
  • MW: 733.76
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Target Protein-binding moiety 4

Target Protein-binding moiety 4 is a BRD4(1) inhibitor with an IC50 of 7.9 μM.

  • CAS Number: 1300019-38-8
  • MF: C20H17ClN4O3
  • MW: 396.83
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH-(PEG2-acid)2

NH-bis(PEG2-C2-acid) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1919044-99-7
  • MF: C14H27NO8
  • MW: 337.37
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MS177

MS177 (MS-177) is a potent and selective EZH2 degarder (PROTAC) based on EZH2 inhibitor C24 with CRBN ligand pomalidomide with DC50 of 0.2 uM in EOL-1 cells.MS177 effectively degraded cellular EZH2-PRC2, suppressed global H3K27me3 in leukaemia cells.MS177 exhibited half-maximal degradation concentration (DC50) values of 0.2 ± 0.1 μM and 1.5 ± 0.2 μM, and maximum degradation (Dmax) values of 82% and 68%, respectively, in EOL-1 and MV4;11 cells.MS177 efficiently suppresses EZH2-PRC2 functions, also efficiently induces Myc degradation in cancer cells, suppresses EZH2-PRC2 functions.MS177 efficiently induces leukaemia cell growth inhibition, apoptosis and cell cycle progression arrest, which is more effective than EZH2 inhibitors. MS177 (i.p. injection, 50-1 g/kg) represses AML growth without apparent toxicity in PDX models.

  • CAS Number: 2225938-86-1
  • MF: C48H55N11O8
  • MW: 914.037
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG6-alcohol

Biotin-PEG6-alcohol is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 906099-89-6
  • MF: C22H41N3O8S
  • MW: 507.64100
  • Catalog: PROTAC Linker
  • Density: 1.176±0.06 g/cm3(20 °C , 760mmHg)
  • Boiling Point: 754.3±60.0 °C (760 mmHg)
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand-Linker Conjugates 17

E3 ligase Ligand-Linker Conjugates 17 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

  • CAS Number: 1950635-16-1
  • MF: C25H31F3N4O8
  • MW: 572.53
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand-Linker Conjugates 14

E3 ligase Ligand-Linker Conjugates 14 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

  • CAS Number: 1957236-21-3
  • MF: C25H31F3N4O11
  • MW: 620.53
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG6-PFP ester

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

  • CAS Number: 1599486-33-5
  • MF: C25H30F5NO10
  • MW: 599.498
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 623.0±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 330.6±31.5 °C

Pomalidomide-amino-PEG4-NH2

Pomalidomide-amino-PEG4-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Pomalidomide based cereblon ligand and a linker used in PROTAC technology[1].

  • CAS Number: 2331259-44-8
  • MF: C23H30N4O9
  • MW: 506.51
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A