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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Bis-propargyl-PEG12

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

  • CAS Number: 1351373-50-6
  • MF: C30H54O13
  • MW: 622.742
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 623.4±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 222.7±30.0 °C

PROTAC AR Degrader-4

PROTAC AR Degrader-4 comprises a cIAP1 ligand binding group, a linker and an androgen receptor (AR) binding group. PROTAC AR Degrader-4 is an AR degrader. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs)[1].

  • CAS Number: 1351169-31-7
  • MF: C43H67N3O9
  • MW: 770.01
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-Boc-cis-4-Hydroxy-D-proline

N-Boc-cis-4-Hydroxy-D-proline is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). N-Boc-cis-4-Hydroxy-D-proline is also a alkyl chain-based PROTAC linker that can be used in the synth

  • CAS Number: 135042-12-5
  • MF: C10H17NO5
  • MW: 231.246
  • Catalog: ADC Linker
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 390.9±42.0 °C at 760 mmHg
  • Melting Point: 145ºC
  • Flash Point: 190.2±27.9 °C

Thalidomide-5,6-Cl

Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.

  • CAS Number: 2648939-40-4
  • MF: C13H8Cl2N2O4
  • MW: 327.12
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Triethylene glycol monodecyl ether

Triethylene glycol monodecyl ether is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 4669-23-2
  • MF: C16H34O4
  • MW: 290.43900
  • Catalog: PROTAC Linker
  • Density: 0.936 g/mL at 20ºC(lit.)
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-(2-(6-chlorohexyloxy)ethoxy)ethanamine hydrochloride

2-(2-(6-chlorohexyloxy)ethoxy)ethanamine (hydrochloride) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1035373-85-3
  • MF: C10H23Cl2NO2
  • MW: 260.20112
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG4-amino-t-Bu-DADPS-C6-azide

Biotin-PEG4-amino-t-Bu-DADPS-C6-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1260247-50-4
  • MF: C43H67N7O9SSi
  • MW: 886.18
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-N-amido-PEG3-azide

Fmoc-N-amido-PEG3-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1172605-58-1
  • MF: C23H28N4O5
  • MW: 440.49200
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG2-CH2COOH

Propargyl-PEG2-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 944561-46-0
  • MF: C9H14O5
  • MW: 202.20
  • Catalog: PROTAC Linker
  • Density: 1.158±0.06 g/cm3(Predicted)
  • Boiling Point: 334.9±27.0 °C(Predicted)
  • Melting Point: N/A
  • Flash Point: 129.8±17.2 °C

Aldehyde-benzyl-PEG5-alkyne

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

  • CAS Number: 1378928-83-6
  • MF: C19H26O6
  • MW: 350.41
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

rel-((1R,8S,9r)-Bicyclo[6.1.0]non-4-yn-9-yl)methyl (4-nitrophenyl) carbonate

exo BCN-O-PNB is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1380006-72-3
  • MF: C17H17NO5
  • MW: 315.32
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-N-Boc-3-hydroxyazetidine

1-N-Boc-3-hydroxyazetidine is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). 1-N-Boc-3-hydroxyazetidine is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs

  • CAS Number: 141699-55-0
  • MF: C8H15NO3
  • MW: 173.210
  • Catalog: ADC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 253.7±33.0 °C at 760 mmHg
  • Melting Point: 42-44°C
  • Flash Point: 107.2±25.4 °C

m-PEG4-phosphonic acid ethyl ester

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

  • CAS Number: 1872433-73-2
  • MF: C13H29O7P
  • MW: 328.34
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-NH-PEG1-CH2CH2COOH

Boc-NH-PEG1-CH2CH2COOH is a cleavable (1 unit PEG) ADC linker and also a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of antibody-drug conjugates (ADCs) or PROTACs[1][2].

  • CAS Number: 1260092-44-1
  • MF: C10H19NO5
  • MW: 233.262
  • Catalog: ADC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 385.0±27.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 186.7±23.7 °C

Benzyl-PEG6-THP

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

  • CAS Number: 230620-73-2
  • MF: C24H40O8
  • MW: 456.57
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG9-alcohol

Azido-PEG9-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1984776-37-5
  • MF: C18H37N3O9
  • MW: 439.50
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand 16

E3 ligase Ligand 16 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 16 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins[1].

  • CAS Number: 2249750-27-2
  • MF: C32H32Cl2N4O6
  • MW: 639.53
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

A947

A947 is a potent and selective SMARCA2 proteolysis-targeting chimera molecule (PROTAC). A947 also is a potent and moderately selective SMARCA2 degrader. A947 has binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM. A947 can be used for the research of cancer[1].

  • CAS Number: 2378056-80-3
  • MF: C61H76N12O7S
  • MW: 1121.40
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG4-t-butyl ester

Bis-PEG4-t-butyl ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2100306-53-2
  • MF: C20H38O8
  • MW: 406.51
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-NH-PEG12-CH2COOH

Fmoc-NH-PEG12-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2291257-76-4
  • MF: C41H63NO16
  • MW: 825.94
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH2-PEG5-C6-Cl hydrochloride

NH2-PEG5-C6-Cl hydrochloride is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2241669-16-7
  • MF: C16H35Cl2NO5
  • MW: 392.36
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG3-alcohol

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

  • CAS Number: 57641-67-5
  • MF: C6H13BrO3
  • MW: 213.07000
  • Catalog: PROTAC Linker
  • Density: 1.411±0.06 g/cm3
  • Boiling Point: 276.3±20.0 °C
  • Melting Point: N/A
  • Flash Point: N/A

E3 Ligase Ligand-Linker Conjugates 21

E3 Ligase Ligand-Linker Conjugates 21 is a synthesized compound that incorporates an E3 ligase ligand and a linker used in PROTAC technology.

  • CAS Number: 1957236-20-2
  • MF: C23H30N4O9
  • MW: 506.51
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MD13

MD13 is a macrophage migration inhibitory factor (MIF)-directed PROTAC with a Ki of 71 nM. MD13 can be used for cancer research[1].

  • CAS Number: 2758431-97-7
  • MF: C35H35N5O8
  • MW: 653.68
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-PEG10-acid

Bis-PEG10-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 2055023-26-0
  • MF: C24H46O14
  • MW: 558.61
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC IRAK4 degrader-4

PROTAC IRAK4 degrader-4 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-127[1].

  • CAS Number: 2360528-45-4
  • MF: C41H38F3N11O10
  • MW: 901.80
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

hexaethyleneglycol

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

  • CAS Number: 2615-15-8
  • MF: C12H26O7
  • MW: 282.331
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 378.3±0.0 °C at 760 mmHg
  • Melting Point: 5-7 °C(lit.)
  • Flash Point: 193.7±26.5 °C

SJFα

SJFα is a 13-atom linker PROTAC. SJFα degrades p38α with a DC50 of 7.16  nM, but is far less effective at degrading p38δ (DC50=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 µM[1].

  • CAS Number: 2254609-27-1
  • MF: C59H67F2N7O11S
  • MW: 1120.27
  • Catalog: p38 MAPK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Lenalidomide-C5-amido-Boc

Lenalidomide-C5-amido-Boc is the Lenalidomide-based Cereblon ligand used in the recruitment of CRBN protein. Lenalidomide-C5-amido-Boc can be connected to the ligand for protein by a linker to form PROTAC[1].

  • CAS Number: 2138441-25-3
  • MF: C23H31N3O5
  • MW: 429.51
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-5'-C8-acid

Pomalidomide-5'-C8-acid (Compound 3d') is an E3 ligase ligand-linker conjugate containing a Pomalidomide (HY-10984) based cereblon (CRBN) ligand and a linker. Pomalidomide-5'-C8-acid can be used in the synthesis of PROTACs[1].

  • CAS Number: 2682112-09-8
  • MF: C22H27N3O6
  • MW: 429.47
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A