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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m-PEG9-CH2COOH

m-PEG9-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 405518-55-0
  • MF: C21H42O12
  • MW: 486.55100
  • Catalog: PROTAC Linker
  • Density: 1.122
  • Boiling Point: 557.372ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 175.904ºC

Amino-PEG5-amine

Amino-PEG5-amine is a PEG-based (5 units) PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 72236-26-1
  • MF: C12H28N2O5
  • MW: 280.36100
  • Catalog: PROTAC Linker
  • Density: 1.055g/cm3
  • Boiling Point: 379.915ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 181.118ºC

(S,R,S)-AHPC-amido-C5-acid

(S,R,S)-AHPC-amido-C5-acid incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. (S,R,S)-AHPC-amido-C5-acid can be used to design XY028-133 (HY-129180)[1].

  • CAS Number: 2162120-87-6
  • MF: C29H40N4O6S
  • MW: 572.72
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-NMe-PEG4-acid

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

  • CAS Number: 2170240-98-7
  • MF: C27H35NO8
  • MW: 501.57
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG8-CH2CH2-NHS ester

m-PEG8-CH2CH2-NHS ester is a PEG--based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 1316189-13-5
  • MF: C24H43NO13
  • MW: 553.597
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 598.3±60.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 315.7±32.9 °C

N-Me-N-(PEG4-acid)2

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

  • CAS Number: 2055014-77-0
  • MF: C23H45NO12
  • MW: 527.60
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Nonylbenzene-PEG8-OH

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

  • CAS Number: 41506-14-3
  • MF: C31H56O9
  • MW: 572.77100
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG8-acid

Biotin-PEG8-acid is a biotin-labeled, PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2143964-62-7
  • MF: C29H53N3O12S
  • MW: 667.81
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-propargyl-PEG5

Bis-propargyl-PEG5 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG5 is used for the synthesis of carbohydrate receptors (SCRs) with anti-Zika activity[1].

  • CAS Number: 185378-83-0
  • MF: C16H26O6
  • MW: 314.374
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 381.7±37.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 147.7±26.4 °C

JPS016

JPS016 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS016 degrades class I histone deacetylase (HDAC). JPS016 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells[1].

  • CAS Number: 2669785-77-5
  • MF: C48H63N7O8S
  • MW: 898.12
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Acid-PEG13-NHS ester

Acid-PEG13-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2152679-62-2
  • MF: C34H61NO19
  • MW: 787.84
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride

Thalidomide-O-amido-PEG3-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology[1].

  • CAS Number: 2245697-84-9
  • MF: C23H31ClN4O9
  • MW: 542.97
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG3-azide

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

  • CAS Number: 932741-18-9
  • MF: C9H15N3O3
  • MW: 213.234
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

E3 ligase Ligand-Linker Conjugates 11

E3 Ligase Ligand-Linker Conjugate 11 is a synthesized compound which incorporates a ligand for the E3 ubiquitin ligase and a PROTAC linker to bring together target protein and ubiquitinating machinery.

  • CAS Number: 1835705-61-7
  • MF: C39H61ClN4O6S
  • MW: 749.44
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydroxy-PEG2-C2-sulfonic acid

Hydroxy-PEG2-C2-sulfonic acid is a PEG-based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 112724-27-3
  • MF: C6H14O6S
  • MW: 214.23700
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

A 410099.1, amine-Boc

A 410099.1, amine-Bocis a functionalized IAP ligand and can be used for the synthesis of PROTACs, such as PROTACs targeting BTK (PROTACs 4 and 5)[1].

  • CAS Number: 1613552-03-6
  • MF: C32H49N5O5
  • MW: 583.76
  • Catalog: E3 Ligase Ligand-Linker Conjugate
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Protac linker 5

Protac Linker 5 is a PROTAC linker utilized to connect the respective tyrosine kinase inhibitor (TKI) to the E3 recruiting ligand.

  • CAS Number: 2245697-83-8
  • MF: C27H40ClN5O4S
  • MW: 566.16
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PEG1-Boc

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

  • CAS Number: 810677-16-8
  • MF: C13H19NO5
  • MW: 269.294
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 390.5±22.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 190.0±22.3 °C

N-Boc-PEG10-alcohol

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

  • CAS Number: 2238844-74-9
  • MF: C25H51NO12
  • MW: 557.67
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Diethoxy-phosphorylethyl-PEG5-ethylphosphonic acid

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

  • CAS Number: 1446282-17-2
  • MF: C16H36O11P2
  • MW: 466.4
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG4-beta-D-glucose

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

  • CAS Number: 1397682-63-1
  • MF: C17H30O10
  • MW: 394.41
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-propargyl-PEG6

Bis-propargyl-PEG6 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG6 can be used to synthesize the polymer linked multimers of guanosine-3', 5'-cyclic monophosphates[1].

  • CAS Number: 400775-35-1
  • MF: C18H30O7
  • MW: 358.427
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 421.9±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 162.5±27.2 °C

JPS014

JPS014 is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). JPS014 degrades class I histone deacetylase (HDAC). JPS014 is potent HDAC1/2 degrader correlated with greater total differentially expressed genes and enhanced apoptosis in HCT116 cells[1].

  • CAS Number: 2669785-76-4
  • MF: C46H59N7O7S
  • MW: 854.07
  • Catalog: HDAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BCL6 PROTAC 1

BCL6 PROTAC 1 is a selective B-cell lymphoma 6 (BCL6) PROTAC. BCL6 PROTAC 1 inhibits BCL6 cell reporter with an IC50 value of 8.8 µM. BCL6 PROTAC 1 significantly degrades BCL6 in diffuse large B-cell lymphoma (DLBCL) cell lines. BCL6 PROTAC 1 can be used in tumor related research[1].

  • CAS Number: 2257479-54-0
  • MF: C45H52ClN9O12
  • MW: 946.40
  • Catalog: Bcl-2 Family
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG3-C3-OH

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

  • CAS Number: 1807512-36-2
  • MF: C9H19N3O4
  • MW: 233.265
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotin-PEG3-OH

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

  • CAS Number: 1263044-40-1
  • MF: C16H29N3O5S
  • MW: 375.48
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG3-SH

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

  • CAS Number: 31521-83-2
  • MF: C7H16O3S
  • MW: 180.26500
  • Catalog: PROTAC Linker
  • Density: 1.017
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Benzyl-PEG24-alcohol

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

  • CAS Number: 2218463-19-3
  • MF: C55H104O25
  • MW: 1165.40
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(Ac-PEG3)-N'-(azide-PEG3)-Cy7 chloride

N-(Ac-PEG3)-N'-(azide-PEG3)-Cy7 (chloride) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 2107273-00-5
  • MF: C43H58ClN5O7
  • MW: 792.40
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Amine-PEG4-Desthiobiotin

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

  • CAS Number: 2306109-91-9
  • MF: C20H40N4O6
  • MW: 432.55
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A