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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Thalidomide-4-C3-NH2 hydrochloride

Thalidomide-4-C3-NH2 hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-4-C3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs[1].

  • CAS Number: 2357110-84-8
  • MF: C16H18ClN3O4
  • MW: 351.78
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amino-PEG3-sulfonic acid HCl

Amino-PEG3-C2-sulfonic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1817735-43-5
  • MF: C8H19NO6S
  • MW: 257.30
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-(23-Hydroxy-3,6,9,12,15,18,21-heptaoxatricosyl)-1H-pyrrole-2,5-dione

Mal-PEG8-alcohol is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2353409-63-7
  • MF: C20H35NO10
  • MW: 449.49
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG4-S-PEG4-acid

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

  • CAS Number: 2055041-20-6
  • MF: C22H40O10S
  • MW: 496.61
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methyltetrazine-propylamine HCl

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

  • CAS Number: 1802978-47-7
  • MF: C12H15N5O
  • MW: 245.28
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG3-propionic hydrazide

Biotin-PEG3-propionic hydrazide is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.

  • CAS Number: 1381861-94-4
  • MF: C19H35N5O6S
  • MW: 461.576
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 813.7±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 445.9±34.3 °C

Acid-PEG4-S-S-PEG4-acid

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

  • CAS Number: 2055015-40-0
  • MF: C22H42O12S2
  • MW: 562.69
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

1-(t-Boc-Aminooxy)-3-aminooxy-propane

1-(t-Boc-Aminooxy)-3-aminooxy-propane is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1352546-80-5
  • MF: C8H18N2O4
  • MW: 206.24
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG3-PFP ester

Mal-PEG3-PFP ester is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1807534-78-6
  • MF: C19H18F5NO7
  • MW: 467.341
  • Catalog: PROTAC Linker
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 531.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 275.3±30.1 °C

Boc-A 410099.1 amide-alkylC4-amine

Boc-A 410099.1 amide-alkylC4-amine is a functionalized IAP ligand for PROTACs that incorporates an IAP ligand and an amide-alkylC4 linker with terminal amine. Boc-A 410099.1 amide-alkylC4-amine can conjugates with target protein ligands.

  • CAS Number: 2415256-18-5
  • MF: C37H58N6O6
  • MW: 682.89
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

THP-PEG7

THP-PEG6-OH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. THP-PEG6-OH is also a non-cleavable 3 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs)[2].

  • CAS Number: 42607-87-4
  • MF: C17H34O8
  • MW: 232.23900
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thiol-PEG3-phosphonic acid

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

  • CAS Number: 1360716-36-4
  • MF: C8H19O6PS
  • MW: 274.27
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-5-PEG4-NH2 hydrochloride

Thalidomide-5-PEG4-NH2 hydrochloride 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: 2743434-24-2
  • MF: C21H28ClN3O8
  • MW: 485.92
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG10-alcohol

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

  • CAS Number: 2378150-09-3
  • MF: C23H44O11
  • MW: 496.59
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG4-5-nitrophenyl carbonate

Propargyl-PEG4-5-nitrophenyl carbonate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1422540-81-5
  • MF: C18H23NO9
  • MW: 397.38
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-7-NH2

Pomalidomide-7-NH2 is the Pomalidomide-based cereblon ligand used in the recruitment of CRBN protein. Pomalidomide-7-NH2 can be connected to the ligand for protein by a linker to form PROTACs[1].

  • CAS Number: 497146-96-0
  • MF: C13H12N4O4
  • MW: 288.26
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG8-amine

Azido-PEG8-amine is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 857891-82-8
  • MF: C18H38N4O8
  • MW: 438.51600
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pyrene-PEG5-alcohol

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

  • CAS Number: 1817735-44-6
  • MF: C27H31NO6
  • MW: 465.54
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thiol-PEG5-alcohol

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

  • CAS Number: 248582-03-8
  • MF: C10H22O5S
  • MW: 254.341
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(Acid-PEG2)-N-bis(PEG3-azide)

N-(Acid-PEG2)-N-bis(PEG3-azide) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2320560-35-6
  • MF: C24H45N7O11
  • MW: 607.65
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-PEG3-NHS ester

Fmoc-PEG3-CH2CH2-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1352827-47-4
  • MF: C28H32N2O9
  • MW: 540.56
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fluorescein-PEG5-NHS ester

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

  • CAS Number: 2353409-62-6
  • MF: C38H41N3O14S
  • MW: 795.81
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

TAMRA-PEG4-acid

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

  • CAS Number: 1909223-02-4
  • MF: C36H43N3O10
  • MW: 677.80
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Acid-PEG4-S-PEG4-acid

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

  • CAS Number: 2055041-21-7
  • MF: C22H42O12S
  • MW: 530.63
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG3-acid chloride

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

  • CAS Number: 66722-87-0
  • MF: C8H15ClO4
  • MW: 210.66
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-acetyl-PEG4-Boc

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

  • CAS Number: 1818294-26-6
  • MF: C17H32O7S
  • MW: 380.497
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 452.0±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 207.2±15.4 °C

m-PEG9-phosphonic acid

m-PEG9-phosphonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 2055016-25-4
  • MF: C19H41O12P
  • MW: 492.50
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tos-O-C4-NH-Boc

Tos-O-C4-NH-Boc is an alkyl ether-based PROTAC linker can be used in the synthesis of PROTACs, such as BSJ-03-204 (HY-136250)[1].

  • CAS Number: 180851-50-7
  • MF: C16H25NO5S
  • MW: 343.43800
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bromo-PEG2-C2-Boc

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

  • CAS Number: 1381861-91-1
  • MF: C11H21BrO4
  • MW: 297.18604
  • Catalog: PROTAC Linker
  • Density: 1.240±0.06 g/cm3
  • Boiling Point: 332.0±22.0 °C
  • Melting Point: N/A
  • Flash Point: N/A

Acid-PEG3-PFP ester

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

  • CAS Number: 1835759-67-5
  • MF: C16H17F5O7
  • MW: 416.29
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A