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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Sulfo-NHS-Acetate sodium

Sulfo-NHS-Acetate sodium is an alkyl chain-based PROTAC linker. Sulfo-NHS-Acetate sodium can be used in the synthesis of PROTACs[1].

  • CAS Number: 221222-61-3
  • MF: C6H6NNaO7S
  • MW: 259.17
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

endo-BCN-PEG3-acid

endo-BCN-PEG3-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

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

Boc-C16-COOH

Boc-C16-COOH is a non-cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs). Boc-C16-COOH is also a alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1]

  • CAS Number: 843666-40-0
  • MF: C22H42O4
  • MW: 370.56600
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HJB97

HJB97 is a high-affinity BET inhibitor with Kis of 0.9±0.2 nM (BRD2 BD1), 0.27±0.09 nM (BRD2 BD2), 0.18±0.01 nM (BRD3 BD1), 0.21±0.03 nM (BRD3 BD2), 0.5±0.2 nM (BRD4 BD1), 1.0±0.1 nM (BRD4 BD2), respectively. HJB97 is a PROTAC BET degrader. Antitumor activity[1].

  • CAS Number: 2093391-24-1
  • MF: C26H28N8O3
  • MW: 500.55
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG5-CH2CO2-PFP

Azido-PEG5-CH2CO2-PFP is a PEG- and Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 2144777-92-2
  • MF: C18H22F5N3O7
  • MW: 487.38
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

[4-(Diethoxy-phosphorylamino)-butyl]-phosphoramidic acid diethyl ester

Tetraethyl butane-​1,​4-​diylbis(phosphoramid​ate) is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 720707-93-7
  • MF: C12H30N2O6P2
  • MW: 360.32
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CBZ-NH-PEG4-CH2CH2COOH

Cbz-NH-PEG4-C2-acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 756526-00-8
  • MF: C19H29NO8
  • MW: 399.43546
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG1-Tos

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

  • CAS Number: 4981-83-3
  • MF: C16H18O4S
  • MW: 306.37700
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH2-PEG2-methyl acetate

NH2-PEG2-methyl acetate is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 741235-80-3
  • MF: C7H15NO4
  • MW: 177.20
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH-(PEG4-acid)2

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

  • CAS Number: 2055041-59-1
  • MF: C22H43NO12
  • MW: 513.58
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

THP-PEG1-alcohol

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

  • CAS Number: 2162-31-4
  • MF: C7H14O3
  • MW: 146.184
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 255.3±30.0 °C at 760 mmHg
  • Melting Point: 95ºC 22 mm Hg(lit.)
  • Flash Point: 108.2±24.6 °C

t-boc-N-amido-PEG5-azide

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

  • CAS Number: 911209-07-9
  • MF: C17H34N4O7
  • MW: 406.47
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

2-Amino-1,3-bis(carboxylethoxy)propane HCl

2-Amino-13-bis(carboxylethoxy)propane is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1020112-73-5
  • MF: C9H17NO6
  • MW: 235.23
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG8-ethoxycarbonyl--NHS ester

m-PEG8-ethoxycarbonyl--NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2353409-76-2
  • MF: C25H43NO14
  • MW: 581.61
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG1-NHS ester

m-PEG1-NHS ester is a PEG/Alkyl/ether-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1027371-75-0
  • MF: C8H11NO5
  • MW: 201.18
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NH-bis(PEG4-Boc)

NH-bis(PEG4-C2-NH-Boc) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2182601-75-6
  • MF: C30H61N3O12
  • MW: 655.82
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-PEG1-Boc

Boc-PEG1-Boc is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 727729-33-1
  • MF: C14H26O6
  • MW: 290.35
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tetra(cyanoethoxymethyl) methane

Tetra(cyanoethoxymethyl) methane is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2465-91-0
  • MF: C17H24N4O4
  • MW: 348.39700
  • Catalog: PROTAC Linker
  • Density: 1.13g/cm3
  • Boiling Point: 610.6ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 232ºC

Biotin-PEG6-acid

Biotin-PEG6-acid is a PEG-based PROTAC linker can be used in the synthesis of PROTAC.

  • CAS Number: 1352814-10-8
  • MF: C25H45N3O10S
  • MW: 579.704
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 818.4±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 448.8±34.3 °C

Desthiobiotin-PEG4-DBCO

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

  • CAS Number: 2032788-37-5
  • MF: C39H53N5O8
  • MW: 719.87
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

t-boc-N-amido-PEG7-azide

Boc-NH-PEG7-azide is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 206265-96-5
  • MF: C21H42N4O9
  • MW: 494.58
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC IRAK4 degrader-1

PROTAC IRAK4 degrader-1 is a PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively[1].

  • CAS Number: 2360533-90-8
  • MF: C44H39F3N12O7
  • MW: 904.85
  • Catalog: IRAK
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

heptaethylene glycol

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

  • CAS Number: 5617-32-3
  • MF: C14H30O8
  • MW: 326.383
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 435.0±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 216.9±27.3 °C

m-PEG6-amino-Mal

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

  • CAS Number: 1644231-07-1
  • MF: C20H34N2O9
  • MW: 446.492
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 604.5±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 319.4±31.5 °C

Acid-PEG3-SSPy

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

  • CAS Number: 2088570-69-6
  • MF: C14H21NO5S2
  • MW: 347.45
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

S-acetyl-PEG6-Boc

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

  • CAS Number: 1818294-39-1
  • MF: C21H40O9S
  • MW: 468.602
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 522.5±50.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 242.0±18.1 °C

Vipivotide tetraxetan Linker

Vipivotide tetraxetan Linker is a useful peptide linker for synthesis of Vipivotide tetraxetan (PSMA-617). Vipivotide tetraxetan (PSMA-617) is a ligand used to synthesize 177Lu-PSMA-617, which is a radioactive molecule for the treatment of prostate cancer[1].

  • CAS Number: 1703768-74-4
  • MF: C33H45N5O9
  • MW: 655.74
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SMPH Crosslinker

SMPH Crosslinker is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 367927-39-7
  • MF: C17H21N3O7
  • MW: 379.36500
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG8-ethoxycarbonyl-propanoic acid

m-PEG8-ethoxycarbonyl-propanoic acid is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2353409-75-1
  • MF: C21H40O12
  • MW: 484.54
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

endo-BCN-PEG3-NH-Boc

endo-BCN-PEG3-NH-Boc is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

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