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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Mal-PEG2-alcohol

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

  • CAS Number: 34321-81-8
  • MF: C8H11NO4
  • MW: 185.17700
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Boc-NH-PEG2-C2-amido-C4-acid

PROTAC Linker 30 is a PROTAC linker, which refers to the alkyl/ether composition. PROTAC Linker 30 can be used in the synthesis of a series of PROTACs. PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[1].

  • CAS Number: 1310327-20-8
  • MF: C17H32N2O7
  • MW: 376.45
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Thiol-PEG2-acid

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

  • CAS Number: 1379649-73-6
  • MF: C7H14O4S
  • MW: 194.249
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 329.0±32.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 152.8±25.1 °C

Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Br

Glucocorticoid receptor agonist-1 phosphate Ala-Ala-Br is an ADC linker that can be used as a reaction reagent for the synthesis of anti-CD40 antibody agent conjugates (ADCs)[1].

  • CAS Number: 2345733-40-4
  • MF: C43H49BrF2N3O12P
  • MW: 948.74
  • Catalog: ADC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomid-C6-PEG3-butyl-N3

Pomalidomid-C6-PEG3-butyl-N3 is a click chemistry reagent containing an azide group. Pomalidomid-C6-PEG3-butyl-N3 also is a crosslinker-E3 ligase ligand conjugate, which be used in click reactive protein degrader building block for PROTAC research.Pomalidomid-C6-PEG3-butyl-N3 also can be used in the template for synthesis of targeted protein degrader[1].

  • CAS Number: 2300178-66-7
  • MF: C29H40N6O8
  • MW: 600.663
  • Catalog: PROTAC
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Hydroxy-PEG6-CH2-Boc

Hydroxy-PEG6-CH2-Boc is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 297162-47-1
  • MF: C18H36O9
  • MW: 396.473
  • Catalog: PROTAC Linker
  • Density: 1.1±0.1 g/cm3
  • Boiling Point: 469.5±40.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 151.3±20.8 °C

N-(Azido-PEG3)-N-bis(PEG3-acid) HCl

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

  • CAS Number: 2055042-57-2
  • MF: C26H50N4O13
  • MW: 626.69
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Biotinyl-NH-PEG3-C3-amido-C3-COOH (DIPEA)

Biotinyl-NH-PEG3-C3-amido-C3-COOH (DIPEA) is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1205744-09-7
  • MF: C33H63N5O8S
  • MW: 689.95
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Pomalidomide-6-OH

Pomalidomide-6-OH is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-6-OH can be connected to the ligand for protein by a linker to form PROTAC[1].

  • CAS Number: 1547162-44-6
  • MF: C13H11N3O5
  • MW: 289.24
  • Catalog: Ligand for E3 Ligase
  • Density: 1.7±0.1 g/cm3
  • Boiling Point: 674.7±55.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 361.8±31.5 °C

m-PEG3-CH2COOH

m-PEG3-CH2COOH is a PEG-based based PROTAC linker can be used in the synthesis of PROTACs.

  • CAS Number: 16024-60-5
  • MF: C9H18O6
  • MW: 222.23600
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

m-PEG10-Tos

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

  • CAS Number: 211859-75-5
  • MF: C26H46O12S
  • MW: 582.7
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

N-(Aminooxy-PEG2)-N-bis(PEG3-propargyl)

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

  • CAS Number: 2112737-71-8
  • MF: C24H44N2O9
  • MW: 504.61
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG2-OH

Propargyl-PEG2-OH is a PEG-based PROTAC linker can be used in the synthesis of Thalidomide-O-PEG2-propargyl (HY-126458)[1].

  • CAS Number: 7218-43-1
  • MF: C7H12O3
  • MW: 144.168
  • Catalog: PROTAC Linker
  • Density: 1.0±0.1 g/cm3
  • Boiling Point: 225.6±20.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 90.3±21.8 °C

Thalidomide-5-NH-CH2-COO(t-Bu)

Thalidomide-5-NH-CH2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-5-NH-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-5-NH-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.

  • CAS Number: 2412056-28-9
  • MF: C19H21N3O6
  • MW: 387.39
  • Catalog: Ligand for E3 Ligase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DSPE-PEG5-azide

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

  • CAS Number: 2112737-73-0
  • MF: C54H105N4O14P
  • MW: 1065.40
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-aminooxy-PEG4-acid

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

  • CAS Number: 1895922-70-9
  • MF: C26H33NO9
  • MW: 503.54
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-PFP ester

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

  • CAS Number: 138194-55-5
  • MF: C13H6F5NO4
  • MW: 335.18
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Fmoc-NH-PEG10-acid

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

  • CAS Number: 2101563-45-3
  • MF: C38H57NO14
  • MW: 751.857
  • Catalog: PROTAC Linker
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 826.4±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 453.6±34.3 °C

t-Butoxycarbonyl-PEG4-NHS ester

Boc-PEG4-C2-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1835759-75-5
  • MF: C20H33NO10
  • MW: 447.48
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Bis-Tos-PEG6

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

  • CAS Number: 42749-27-9
  • MF: C26H38O11S2
  • MW: 590.70300
  • Catalog: PROTAC Linker
  • Density: 1.24g/cm3
  • Boiling Point: 687.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 369.5ºC

TGN-020 sodium

TGN-020 sodium is a selective Aquaporin 4 (AQP4) inhibitor with an IC50 of 3.1 μM[1][2]. TGN-020 sodium is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[3]. TGN-020 sodium alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats[4].

  • CAS Number: 1313731-99-5
  • MF: C8H5N4NaOS
  • MW: 228.21
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Tetrazine-Ph-NHCO-C3-NHS ester

Tetrazine-Ph-NHCO-C3-NHS ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1244040-64-9
  • MF: C18H18N6O5
  • MW: 398.37300
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PROTAC BRD4 Degrader-3

PROTAC BRD4 Degrader-3 (compound 1004.1) is an efficacious PROTAC BRD4 degrader[1].

  • CAS Number: 2313234-00-1
  • MF: C55H65F2N9O9S2
  • MW: 1098.29
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

111-Trifluoroethyl-PEG4-azide

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

  • CAS Number: 1817735-35-5
  • MF: C10H18F3N3O4
  • MW: 301.26
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Methylamino-PEG5-azide

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

  • CAS Number: 2055046-24-5
  • MF: C13H28N4O5
  • MW: 320.39
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Azido-PEG12-alcohol

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

  • CAS Number: 1111239-69-0
  • MF: C26H53N3O13
  • MW: 615.71
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Propargyl-PEG1-NH2

Propargyl-PEG1-NH2 is a PEG-based PROTAC linker can be used in the synthesis of PROTACs[1].

  • CAS Number: 122116-12-5
  • MF: C5H9NO
  • MW: 99.13110
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: 50 °C

FKBP12 PROTAC dTAG-13

FKBP12 PROTAC dTAG-13 (dTAG-13) is an in vivo-active heterobifunctional adation tag (dTAG) small molecule that engage FKBP12F36V and CRBN, selectively degrade FKBP12F36V in a CRBN-dependent manner in cells; causes rapid degradation of nuclear and cytoplasmic FKBP12F36V fusion chimeras, and an unexpected superior antiproliferative effect of pan-BET bromodomain degradation over selective BRD4 degradation, characterize immediate effects of KRASG12V loss on proteomic signaling, and demonstrate rapid degradation in vivo.

  • CAS Number: 2064175-41-1
  • MF: C57H68N4O15
  • MW: 1049.168
  • Catalog: Epigenetic Reader Domain
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 1134.0±65.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 639.6±34.3 °C

DSPE-PEG4-acid

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

  • CAS Number: 2112738-58-4
  • MF: C52H100NO15P
  • MW: 1010.32
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Mal-NH-PEG6-CH2CH2COOPFP ester

Mal-NH-PEG6-CH2CH2COOPFP ester is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1].

  • CAS Number: 1599432-34-4
  • MF: C28H35F5N2O11
  • MW: 670.58
  • Catalog: PROTAC Linker
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A